November 2012, VOL 1, NO 5

Page 1

The official publication of

November 2012 Volume 1 • Number 5 A Peer-Reviewed Journal

PM O

PERSONALIZED MEDICINE IN ONCOLOGY TM

INTERVIEW WITH THE INNOVATORS Cultivating Personalized Medicine Clinical Acumen in the Management of Breast Cancer: An Interview With Edith Perez, MD.....................................Page 17

CONTINUING MEDICAL EDUCATION Clinical Approaches to Targeted Technologies: Implementing the Promise of Prognostic Precision Into Personalized Cancer Care....................... Page 26

MULTIPLE MYELOMA The Role of Personalized Therapy in the Management of Multiple Myeloma: Case Study of a Patient With a Cytogenetic Abnormality...................... Page 41

IMMUNOTHERAPY The Cancer Immunotherapy Trials Network: A National Strategy for the Development and Implementation of Immunotherapy for the Treatment of Cancer...................................... Page 46

ALSO IN THIS ISSUE… • The Last Word by Robert E. Henry................ Page 56

IMPLEMENTING THE PROMISE OF PROGNOSTIC PRECISION INTO PERSONALIZED CANCER CARE

TM

www.PersonalizedMedOnc.com © 2012 Green Hill Healthcare Communications, LLC

In partnership with



Linker Antibody Specific for a tumor-associated antigen that has restricted expression on normal cells.4,8

Cytotoxic agent Designed to kill target cells when internalized and released.4,8

Attaches the cytotoxic agent to the antibody. Newer linker systems are designed to be stable in circulation and release the cytotoxic agent inside targeted cells.4,8,9


T

he Global Biomarkers Consortium™ (GBC) is a community of worldrenowned healthcare professionals who will convene in multiple educational forums in order to better understand the clinical application of predictive molecular biomarkers and advanced personalized care for patients.

PM O

November 2012 Volume 1 • Number 5

PERSONALIZED MEDICINE IN ONCOLOGY ™

CONFERENCE NEWS News From ESMO

PAGE 12

Frontline Therapy of Metastatic Renal Cell Carcinoma: Pazopanib as Effective as Sunitinib Crizotinib Extends Survival Versus Chemotherapy in Advanced NSCLC

Save the date for the Second Annual Conference, October 4-6, 2013 Visit www.globalbiomarkersconsortium.com to register

Professional Experience of GBC Attendees

EGFR Mutations, Not KRAS Mutations, May Be Predictive for Sorafenib Response in Advanced NSCLC Whole Genome Testing Moves Forward in Breast Cancer

INTERVIEW WITH THE INNOVATORS Cultivating Personalized Medicine Clinical Acumen in the Management of Breast Cancer: An Interview PAGE 17 With Edith Perez, MD PMO speaks with the Deputy Director of Mayo Clinic Cancer Center in Florida to discuss the strategy and tactics that she and her fellow colleagues are employing in the fight against breast cancer.

56.7%

26.7%

CONTINUING MEDICAL EDUCATION Clinical Approaches to Targeted Technologies: Implementing the Promise of Prognostic Precision Into Personalized Cancer Care

6.7% 3.3% 6.7%

1-3 years 3-5 years

PAGE 26

Evolving regional standards of care and emerging data on molecular markers impact treatment strategies for specific tumor types. This continuing medical education activity brings together highlights, summaries, and expert commentary on the application of biomarkers in personalized care for patients with solid tumors.

5-10 years 10-20 years >20 years

4

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PERSONALIZED MEDICINE

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November 2012


CARIS TARGET NOW ™ JUST GOT SMARTER

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The use of the Caris Target Now service, the use or interpretation of any information provided as part of su s ch servic vice, e, and and/or /or th the e sele selecti ct on of any dr drug ug age agents nts is so solel lelyy at a and within h n th the e disc discret retion ion of the treating physician’s independent medical judgment. The Caris Target Now services are performed by Cariss Li Life fe Sci Scienc ences, es, a CLI CLIA-c A-certifi fied ed lab labora orator toryy oper operati ating ng und under er the U. U.S. S. Cli Clinic nical al Laboratory Amendment Act of 1988 and in compliance with all relevant U.S. state and federal regulations. None off the Ca Caris ris Ta Targe rgett Now Now ser servic vices es hav have e been been re revie viewed wed by th the e Unit United ed Sta States tes Fo Food od and Drug Administration. Persons depicted are models and used for illustrative purposes only. ©2012 Caris Life Sciences an and d affi affilia liates tes.. All ri right ghtss rese reserve rved. d. CT CTN06 N06131 1312PM 2PMO O


PUBLISHING STAFF SENIOR VICE PRESIDENT, SALES AND MARKETING Philip Pawelko phil@greenhillhc.com PUBLISHERS John W. Hennessy john@greenhillhc.com Russell Hennessy russell@greenhillhc.com DIRECTOR, CLIENT SERVICES Lou Lesperance Jr lou@greenhillhc.com MANAGING DIRECTOR Pam Rattananont Ferris

The Role of Personalized Therapy in the Management of Multiple Myeloma: Case Study of a Patient With a Cytogenetic Abnormality

STRATEGIC EDITOR Robert E. Henry

PAGE 41

A report from the 2012 conference of the Global Biomarkers Consortium.

SENIOR COPY EDITOR BJ Hansen PRODUCTION MANAGER Marie RS Borrelli

IMMUNOTHERAPY

QUALITY CONTROL DIRECTOR Barbara Marino BUSINESS MANAGER Blanche Marchitto CIRCULATION DEPARTMENT circulation@greenhillhc.com Personalized Medicine in Oncology, ISSN 2166-0166 (print); ISSN applied for (online) is published 6 times a year by Green Hill Healthcare Communications, LLC, 1249 South River Road, Suite 202A, Cranbury, NJ 08512. Telephone: 732.656.7935. Fax: 732.656.7938. Copyright ©2012 by Green Hill Healthcare Communications, LLC. All rights reserved. Personalized Medicine in Oncology logo is a trademark of Green Hill Healthcare Communications, LLC. No part of this publication may be reproduced or transmitted in any form or by any means now or hereafter known, electronic or mechanical, including photocopy, recording, or any informational storage and retrieval system, without written permission from the publisher. Printed in the United States of America. EDITORIAL CORRESPONDENCE should be addressed to EDITORIAL DIRECTOR, Personalized Medicine in Oncology (PMO), 1249 South River Road, Suite 202A, Cranbury, NJ 08512. YEARLY SUBSCRIPTION RATES: United States and possessions: individuals, $50.00; institutions, $90.00; single issues, $5.00. Orders will be billed at individual rate until proof of status is confirmed. Prices are subject to change without notice. Correspondence regarding permission to reprint all or part of any article published in this journal should be addressed to REPRINT PERMISSIONS DEPARTMENT, Green Hill Healthcare Communications, LLC, 1249 South River Road, Suite 202A, Cranbury, NJ 08512. The ideas and opinions expressed in PMO do not necessarily reflect those of the editorial board, the editorial director, or the publishers. Publication of an advertisement or other product mention in PMO should not be construed as an endorsement of the product or the manufacturer’s claims. Readers are encouraged to contact the manufacturer with questions about the features or limitations of the products mentioned. Neither the editorial board nor the publishers assume any responsibility for any injury and/or damage to persons or property arising out of or related to any use of the material contained in this periodical. The reader is advised to check the appropriate medical literature and the product information currently provided by the manufacturer of each drug to be administered to verify the dosage, the method and duration of administration, or contraindications. It is the responsibility of the treating physician or other healthcare professional, relying on independent experience and knowledge of the patient, to determine drug dosages and the best treatment for the patient. Every effort has been made to check generic and trade names, and to verify dosages. The ultimate responsibility, however, lies with the prescribing physician. Please convey any errors to the editorial director.

Volume 1 • No 5

PERSONALIZED MEDICINE IN ONCOLOGY ™

MULTIPLE MYELOMA

EDITORIAL DIRECTOR Kristin Siyahian kristin@greenhillhc.com

6

PM O

The Cancer Immunotherapy Trials Network: A National Strategy for the Development and Implementation of Immunotherapy for the Treatment of Cancer

PAGE 46

Holbrook E. Kohrt, MD, PhD; Howard L. Kaufman, MD; Mary L. Disis, MD The Cancer Immunotherapy Trials Network was established to address the lack of widespread clinical expertise with immunotherapy and to promote the rapid development of new immunotherapy agents and combination therapy using an integrated national network.

THE LAST WORD A Personal Introduction and Invitation to Join My Journey Through the World of Personalized Medicine

PAGE 56

Robert E. Henry The Strategic Editor of PMO offers thoughts on a variety of topics in personalized medicine.

OUR MISSION The mission of Personalized Medicine in Oncology is to deliver practice-changing information to clinicians about customizing healthcare based on molecular profiling technologies, each patient’s unique genetic blueprint, and their specific, individual psychosocial profile, preferences, and circumstances relevant to the process of care. OUR VISION Our vision is to transform the current medical model into a new model of personalized care, where decisions and practices are tailored for the individual – beginning with an incremental integration of personalized techniques into the conventional practice paradigm currently in place.

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November 2012


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Editorial Board Editor in Chief AL B. BENSON III, MD Northwestern University Chicago, Illinois

SECTION EDITORS Breast Cancer EDITH PEREZ, MD Mayo Clinic Jacksonville, Florida

Gastrointestinal Cancer EUNICE KWAK, MD Massachusetts General Hospital Cancer Center Harvard Medical School Boston, Massachusetts

Drug Development IGOR PUZANOV, MD Vanderbilt University Vanderbilt-Ingram Cancer Center Nashville, Tennessee

Hematologic Malignancies GAUTAM BORTHAKUR, MD The University of Texas MD Anderson Cancer Center Houston, Texas

Lung Cancer VINCENT A. MILLER, MD Foundation Medicine Cambridge, Massachusetts

Pathology DAVID L. RIMM, MD, PHD Yale Pathology Tissue Services Yale University School of Medicine New Haven, Connecticut

Melanoma DOUG SCHWARTZENTRUBER, MD Indiana University Simon Cancer Center Indianapolis, Indiana

Predictive Modeling MICHAEL KATTAN, PHD Case Western Reserve University Cleveland, Ohio

Prostate Cancer OLIVER SARTOR, MD Tulane University New Orleans, Louisiana

EDITORIAL BOARD SANJIV S. AGARWALA, MD St. Luke’s Hospital Bethlehem, Pennsylvania

K. PETER HIRTH, PHD Plexxikon, Inc. Berkeley, California

HOPE S. RUGO, MD University of California, San Francisco San Francisco, California

GREGORY D. AYERS, MS Vanderbilt University School of Medicine Nashville, Tennessee

HOWARD L. KAUFMAN, MD Rush University Chicago, Illinois

DANIELLE SCELFO, MHSA Genomic Health Redwood City, California

LYUDMILA BAZHENOVA, MD University of California, San Diego San Diego, California

KATIE KELLEY, MD UCSF School of Medicine San Francisco, California

LEE SCHWARTZBERG, MD The West Clinic Memphis, Tennessee

LEIF BERGSAGEL, MD Mayo Clinic Scottsdale, Arizona

MINETTA LIU, MD Georgetown University Hospital Washington, DC

JOHN SHAUGHNESSY, PHD University of Arkansas for Medical Sciences Little Rock, Arkansas

KENNETH BLOOM, MD Clarient Inc. Aliso Viejo, California

KIM MARGOLIN, MD University of Washington Fred Hutchinson Cancer Research Center Seattle, Washington

LAWRENCE N. SHULMAN, MD Dana-Farber Cancer Institute Boston, Massachusetts

MARK S. BOGUSKI, MD, PHD Harvard Medical School Boston, Massachusetts GILBERTO CASTRO, MD Instituto do Câncer do Estado de São Paulo São Paulo, Brazil MADELEINE DUVIC, MD The University of Texas MD Anderson Cancer Center Houston, Texas

STEVEN D. GORE, MD The Johns Hopkins University School of Medicine Baltimore, Maryland

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AFSANEH MOTAMED-KHORASANI, PHD Radient Pharmaceuticals Tustin, California NIKHIL C. MUNSHI, MD Dana-Farber Cancer Institute Boston, Massachusetts

BETH FAIMAN, PHD(C), MSN, APRN-BC, AOCN Cleveland Clinic Taussig Cancer Center Cleveland, Ohio STEPHEN GATELY, MD TGen Drug Development (TD2) Scottsdale, Arizona

GENE MORSE, PHARMD University at Buffalo Buffalo, New York

JAMIE SHUTTER, MD South Beach Medical Consultants, LLC Miami Beach, Florida DARREN SIGAL, MD Scripps Clinic Medical Group San Diego, California DAVID SPIGEL, MD Sarah Cannon Research Institute Nashville, Tennessee MOSHE TALPAZ, MD University of Michigan Medical Center Ann Arbor, Michigan

STEVEN O’DAY, MD John Wayne Cancer Institute Santa Monica, California

SHEILA D. WALCOFF, JD Goldbug Strategies, LLC Rockville, Maryland

DAVID A. PROIA, PHD Synta Pharmaceuticals Lexington, Massachusetts

ANAS YOUNES, MD The University of Texas MD Anderson Cancer Center Houston, Texas

RAFAEL ROSELL, MD, PHD Catalan Institute of Oncology Barcelona, Spain STEVEN T. ROSEN, MD, FACP Northwestern University Chicago, Illinois

PERSONALIZED MEDICINE

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November 2012


THIRD ANNUAL

Association for Value-Based Cancer Care Conference Influencing the Patient-Impact Factor May 2-5, 2013 • Westin Diplomat • Hollywood, Florida CONFERENCE CO-CHAIRS

AGENDA* THURSDAY, MAY 2, 2013 8:00 am - 5:00 pm

Registration

FRIDAY, MAY 3, 2013

Craig K. Deligdish, MD Hematologist/Oncologist Oncology Resource Networks

Gary M. Owens, MD President Gary Owens Associates

Burt Zweigenhaft, BS President and CEO OncoMed

PROGRAM OVERVIEW Following on the success of our Second Annual Conference, AVBCC will be coming to Hollywood, Florida, on May 2-5, 2013. We continue to be guided by the expertise of leaders in these fields providing attendees with a thorough understanding of the evolution of the value equation as it relates to cancer therapies. Our goal is to be able to assist them in implementing, improving, and sustaining their organizations and institutions, while improving access for patients and ultimately quality patient care.

7:00 am - 8:00 am

Simultaneous Symposia/Product Theaters

8:15 am - 9:15 am

Session 1: Welcome, Introductions, and Opening Remarks Conference Co-Chairs - Craig K. Deligdish, MD; Gary M. Owens, MD; Burt Zweigenhaft, BS

9:15 am - 10:15 am

Keynote Address

10:15 am - 10:30 am

Break

10:30 am - 11:45 am

Session 2: Trends in Treatment Decision-Making: Pathways and Stakeholder Collaborations Roy A. Beveridge, MD; Michael Kolodziej, MD

12:00 pm - 1:00 pm

Exclusive Lunch Symposium/Product Theater

1:15 pm - 2:00 pm

Session 3: Cost of Cure: When, How, and How Much? John Fox, MD; John Hennessy

2:00 pm - 2:45 pm

Session 4: Where Is Oncology Care Headed in the Future? Jayson Slotnick, JD, MPH (Moderator); Barbara L. McAneny, MD

Upon completion of this activity, the participant will be able to: • Discuss the current trends and challenges facing all stakeholders in optimizing value in cancer care delivery. • Define the barriers associated with cost, quality, and access as they relate to healthcare reform and what solutions are currently being considered. • Compare and contrast the different approaches/tools providers and payers are utilizing to manage and deliver care collaboratively. • Examine the current trends in personalized care and companion diagnostics. • Analyze the patient issues around cost, quality, and access to care.

2:45 pm - 3:30 pm

Session 5: What Will the Cancer Delivery System Look Like in 2015? Linda Bosserman, MD, FACP; John D. Sprandio, MD

3:30 pm - 3:45 pm

Break

3:45 pm - 4:30 pm

Session 6: Employers and Oncology Care F. Randy Vogenberg, PhD, RPh (Moderator); Bridget Eber, PharmD; Patricia Goldsmith; Darin Hinderman

4:30 pm - 5:15 pm

Session 7: The Role of Government in the Future of Oncology Care Jayson Slotnick, JD, MPH

TARGET AUDIENCE

5:15 pm - 5:45 pm

Summary/Wrap-Up of Day 1

This conference is intended for medical oncologists, practice managers/administrators, and managed care professionals. Stakeholders in a position to impact cancer patient care, such as advanced practice nurses, pharmacists, and medical directors, are also invited to join this exciting forum.

6:00 pm - 8:00 pm

Cocktail Reception in the Exhibit Hall

SATURDAY, MAY 4, 2013 7:00 am - 8:00 am

Simultaneous Symposia/Product Theaters

DESIGNATION OF CREDIT STATEMENTS

8:15 am - 8:30 am

Opening Remarks

8:30 am - 9:15 am

Session 8: Advanced Care Directives: Palliative Care, Hospice, Ethics J. Russell Hoverman, MD, PhD Thomas J. Smith, MD, FACP, FASCO

9:15 am - 10:00 am

Session 9: Medicaid: A Healthcare Delivery System Review Matthew Brow

LEARNING OBJECTIVES

SPONSORS This activity is jointly sponsored by Medical Learning Institute Inc, the Association for Value-Based Cancer Care, Inc., Center of Excellence Media, LLC, and Core Principle Solutions, LLC.

COMMERCIAL SUPPORT ACKNOWLEDGMENT

10:00 am - 10:15 am

Break

Grant requests are currently being reviewed by numerous supporters. Support will be acknowledged prior to the start of the educational activities.

10:15 am - 11:00 am

Session 10: Payer, Government, and Industry Insights: Balancing Cost and Quality

11:00 am - 11:45 am

Session 11: National Coalition for Cancer Survivorship: Medication Nonadherence Issues Pat McKercher

12:00 pm - 1:00 pm

Exclusive Lunch Symposium/Product Theater

1:15 pm - 3:00 pm

Session 12: Meet the Experts Networking Roundtable Session

3:00 pm - 3:45 pm

Session 13: Personalized Medicine, Companion Diagnostics, Molecular Profiling, Genome Sequencing—The Impact on Cost, Treatment, and the Value Proposition Mark S. Boguski, MD, PhD

3:45 pm - 4:15 pm

Summary/Wrap-Up of Day 2

4:30 pm - 6:30 pm

Cocktail Reception in the Exhibit Hall

PHYSICIAN CREDIT DESIGNATION The Medical Learning Institute Inc designates this live activity for a maximum of 17.25 AMA PRA Category 1 Credits™. Physicians should claim only the credit commensurate with the extent of their participation in the activity. This activity has been planned and implemented in accordance with the Essential Areas and policies of the Accreditation Council for Continuing Medical Education through the joint sponsorship of the Medical Learning Institute Inc and the Center of Excellence Media, LLC. The Medical Learning Institute Inc is accredited by the Accreditation Council for Continuing Medical Education to provide continuing medical education for physicians.

REGISTERED NURSE DESIGNATION Medical Learning Institute Inc. Provider approved by the California Board of Registered Nursing, Provider Number 15106, for 17.25 contact hours.

SUNDAY, MAY 5, 2013 7:00 am - 8:00 am

Simultaneous Symposia/Product Theaters

REGISTERED PHARMACY DESIGNATION

8:15 am - 8:30 am

Opening Remarks

The Medical Learning Institute Inc is accredited by the Accreditation Council for Pharmacy Education as a provider of continuing pharmacy education. Completion of this knowledge-based activity provides for 17.25 contact hours (1.725 CEUs) of continuing pharmacy education credit. The Universal Activity Number for this activity is (To be determined).

8:30 am - 9:15 am

Session 14: Cancer Rehabilitation: The Next Frontier in Survivorship Care Julie Silver, MD

9:15 am - 10:00 am

Session 15: Current and Future Considerations for the Oncology Practice Manager Dawn Holcombe, MBA, FACMPE, ACHE; Leonard Natelson

10:00 am - 10:15 am

Break

10:15 am - 11:00 am

Session 16: Access to Drugs—Shortages, Biosimilars Douglas Burgoyne, PharmD; James T. Kenney, Jr., RPh, MBA

11:00 am - 11:45 am

Session 17: Perspectives from Large Oncology Group Practices—Successes, Issues, and Challenges

11:45 am - 12:00 pm

Summary and Conclusion of Conference

CONFERENCE REGISTRATION Discounted Pricing Available!

$375.00 until January 15, 2013 $475.00 until March 15, 2013 $675.00 after March 15, 2013

REGISTER TODAY AT

www.regonline.com/avbcc2013

*Agenda is subject to change.


Letter From the Board

PMO and the PM Initiative: Value, Time, and Talent Dear Reader,

W

elcome to the 5th issue of Personalized Medicine in Oncology (PMO) – a journal dedicated to informing practicing oncologists and other providers on the clinical application of personalized medicine (PM) research discoveries, and so guiding them in the appropriate usage of the biologicals and diagnostics so integral to PM. The healthcare system demands value, the balance of cost, quality, and access that requires skillful resource allocation. PMO imparts to practicing oncologists the skills needed for value-based utilization of biologicals that are changing the Oliver Sartor, MD face of cancer care. This includes knowing when and how to use the biologicals that help drive the PM process of care and cause it to prosper. Their gratuitous usage, however, eliminates the value they bring and would threaten their continued usage. Never has “less is more” meant so much. Translating research into action is the tactical completion of the PM mission. Opposing this, however, is a long-standing trend of delaying the application of new research, as stated in the Institute of Medicine report, Crossing the Quality Chasm: A New Health System for the 21st Century: “In the current health care system, scientific knowledge about best care is not applied systematically or expeditiously to clinical practice. An average of about 17 years is required for new knowledge generated by randomized controlled trials to be incorporated into practice, and even then application is highly uneven.” Such inefficiency is incompatible with today’s healthcare system, especially where biologicals and diagnostics are concerned. Their usage must be tied to value. PMO helps providers master value-based usage of biologicals and diagnostics, thereby aligning PM with healthcare’s rules of engagement. To disseminate information on the principles of PM, we offer the oncology community our print and online media as well as live events. Please save the date for the 2nd Annual Conference of the Global Biomarkers Consortium (GBC) on October 4-6, 2013, in Boston, Massachusetts. The GBC is a community of world-renowned healthcare professionals who convene to discuss the clinical application of predictive molecular biomarkers and advanced personalized care for patients. To register or for more information, please visit www.globalbiomarkersconsortium.com. We are pleased to join you in the PM community. Sincerely,

Oliver Sartor, MD Tulane University PMO Board Member

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November 2012


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To learn more, visit us at millennium.com. ©2012 Millennium Pharmaceuticals, Inc. All rights reserved.


2012 ESMO Congress

Frontline Therapy of Metastatic Renal Cell Carcinoma: Pazopanib as Effective as Sunitinib Phoebe Starr

A

ccording to a phase 3 noninferiority trial, pazopanib is similarly effective as sunitinib, with some advantages in its side effect profile. The COMPARZ trial, reported at the 2012 ESMO Congress, met its primary end point by demonstrating that pazopanib was noninferior to sunitinib, a standard frontline therapy in this setting. The distinct side effect profiles of these drugs should be considered when selecting frontline therapy, according to experts. Lead author Robert Motzer, MD, Memorial SloanKettering Cancer Center (MSKCC), New York City, said that the study showed similar efficacy for pazopanib and sunitinib.

The QOL analysis showed greater patient satisfaction with pazopanib therapy, with less fatigue and physical symptoms compared with sunitinib. “The differentiated safety profile of pazopanib shows a lower incidence of hand-foot syndrome, fatigue, stomatitis, and mucositis. Higher liver function abnormalities were observed with pazopanib,” Motzer said. A benefit in quality of life (QOL) was also reported for pazopanib in the COMPARZ study, which is the largest randomized trial conducted in metastatic renal cell carcinoma (mRCC) thus far. COMPARZ randomized 1110 patients with mRCC to either pazopanib or sunitinib. Baseline demographic and disease characteristics were well balanced between the 2 arms. Median age was 61years, about 72% were male, and

We’re just a

83% had prior nephrectomy. Patients from all risk groups were allowed in the trial; the majority had good and intermediate risk according to MSKCC criteria. Median progression-free survival was 8.4 months with pazopanib versus 9.5 months with sunitinib, a nonsignificant difference for noninferiority, with a hazard ratio of 1.047. Adverse events differed according to treatment. More frequent elevations in liver enzymes and whitening of the hair were reported in patients treated with pazopanib, while those treated with sunitinib had higher rates of fatigue, hand-foot syndrome, taste alteration, and thrombocytopenia. In Motzer’s opinion, the side effect profiles “tip the scale in favor of pazopanib” as firstline treatment for mRCC. The QOL analysis showed greater patient satisfaction with pazopanib therapy, with less fatigue and physical symptoms compared with sunitinib. Earlier this year at the 2012 ASCO Annual Meeting, Escudier and colleagues reported results of a patient preference study called PISCES. In this study, 70% of patients preferred pazopanib and 22% preferred sunitinib (Abstract CRA4502). Formal discussant of this trial, Tim Eisen, MD, University of Cambridge, UK, said that he found the data on similar efficacy for the 2 drugs more convincing than the QOL data. He pointed out that QOL assessments were made every 28 days, which favors pazopanib; 28 days is at peak exposure to sunitinib, which is given on a 4 weeks on, 2 weeks off schedule, while pazopanib is given continuously. He said the QOL from PISCES were more convincing in favor of pazopanib. u

click

away!

Please visit us at www.PersonalizedMedOnc.com

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2012 ESMO Congress

Crizotinib Extends Survival Versus Chemotherapy in Advanced NSCLC Phoebe Starr

T

he PROFILE 1007 trial, reported at the 2012 ESMO Congress, showed positive results for a targeted therapy in patients whose tumors expressed that target. The first-in-class ALK inhibitor crizotinib prolonged progression-free survival (PFS) and improved response rates compared with single-agent chemotherapy in patients with advanced, previously treated, ALK-positive (ALK+), non–small cell lung cancer (NSCLC). Patients treated with crizotinib had greater improvement in lung cancer symptoms and quality of life (QOL) compared with patients receiving chemotherapy. PROFILE 1007 is the first trial to compare crizotinib head-to-head with chemotherapy in ALK+ NSCLC. ALK rearrangements are found in about 5% of lung cancers. Even though this is a small percentage, lung cancer is so prevalent that ALK positivity accounts for about 50,000 new cases each year. Studies show that younger patients, those who never smoked, and adenocarcinoma cases are more likely to be ALK+. “These results establish crizotinib as the standard of care for patients with advanced previously treated ALK+ NSCLC,” stated lead author Alice Shaw, MD, Dana-Farber Cancer Institute/Harvard Cancer Center, Boston, Massachusetts. Crizotinib is approved for the treatment of ALK+ NSCLC in the United States. The international PROFILE 1007 trial randomized 347 patients with ALK+, stage IIIb or IV NSCLC to crizotinib 250 mg bid, pemetrexed 500 mg/m2, or docetaxel 75 mg/m2 on a 21-day cycle. Patients treated with crizotinib received a median of 11 cycles, while those treated with chemotherapy received a median of 4 cycles. For the primary end point, median PFS was 7.7 months with crizotinib versus 3 months with chemotherapy, reducing the risk of progression by 51% with crizotinib (P<.0001). Median PFS was 7.7 months

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with crizotinib versus 4.2 months with pemetrexed (P=.0004) and 2.6 months with docetaxel (P<.0001). Overall response rate was tripled in the crizotinib group: 65.3% versus 19.3% for single-agent chemotherapy (P<.0001). No overall survival (OS) benefit was seen with crizotinib in an interim analysis. However, longer follow-up is needed so the data can mature, Shaw said. OS will likely be confounded by crossover, she said, since patients were allowed to cross over to crizotinib if progression occurred.

The first-in-class ALK inhibitor crizotinib prolonged PFS and improved response rates compared with single-agent chemotherapy in patients with advanced, previously treated, ALK-positive NSCLC. Adverse events associated with crizotinib were mild and manageable in the study. The rate of toxicities grade 3 or higher was under 5% for most toxicities; in the crizotinib arm, elevated transaminases were reported in 16% of patients and pulmonary embolism in 5%. Myelosuppression was more frequent in the chemotherapy arms compared with crizotinib. Patient-reported outcomes suggested that QOL was superior on crizotinib compared with chemotherapy. Time to deterioration in lung cancer symptoms was a median of 5.6 months with crizotinib versus 1.4 months with chemotherapy (P<.0001). As with other targeted therapies, patients with advanced cancers will develop resistance to crizotinib. Investigational drugs such as LBK 178, AB6 273, and heat shock protein inhibitors may be able to overcome resistance that develops with crizotinib. u

WWW.PERSONALIZEDMEDONC.COM

November 2012

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2012 ESMO Congress

EGFR Mutations, Not KRAS Mutations, May Be Predictive for Sorafenib Response in Advanced NSCLC Phoebe Starr

T

reatment with sorafenib did not improve overall survival (OS) in patients with heavily pretreated advanced non–small cell lung cancer (NSCLC) in the overall analysis of the MISSION trial reported at the 2012 ESMO Congress. A post hoc companion biomarker study of MISSION presented at the same meeting suggested that EGFR mutated status may be predictive of a benefit with sorafenib treatment; however, KRAS mutations were not predictive of response. “The biomarker analysis hinted that mutated EGFR may be predictive for sorafenib, but interpret these data with caution,” stated lead author Tony S. Mok, MD, Chinese University of Hong Kong. He pointed out that this analysis was based on a small sample size and was exploratory.

The global multicenter, randomized, phase 3 MISSION trial compared sorafenib plus best supportive care with best supportive care alone as third- or fourth-line therapy in 703 patients with advanced NSCLC. The global multicenter, randomized, phase 3 MISSION trial compared sorafenib plus best supportive care with best supportive care alone as third- or fourth-line therapy in 703 patients with advanced NSCLC. Patients were not preselected or prestratified according to EGFR or KRAS status. After the trial was completed, mutational analysis was performed on 347 patients. EGFR mutations were detected in 26% and KRAS mutations in 20%. Mutational status was balanced between the 2 treatment arms. Mutated EGFR was identified in tumor tissue or plasma in 44 patients treated with sorafenib and 45 re-

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ceiving placebo. Wild-type EGFR was found in 122 of sorafenib-treated patients and in 136 in the group receiving placebo. Sorafenib demonstrated a significant progression-free survival (PFS) benefit in patients with mutated EGFR: median PFS was 2.7 months with sorafenib versus 1.4 months with placebo (P<.001). PFS was also significantly better with sorafenib in the wild-type EGFR patients: median of 2.7 months versus 1.5 months, respectively (P<.001). Sorafenib-treated patients with EGFR mutations had significantly superior OS compared with placebo; OS was 13.9 months on sorafenib versus 6.5 months for those receiving placebo (P=.002). However, no OS difference was found between groups in patients with wildtype EGFR; median OS was 8.3 months with sorafenib and 8.4 months with placebo. The biomarker treatment interaction analysis had a P value of .015 for PFS and .023 for OS. The interaction analysis suggests that EGFR status is a potential biomarker for sorafenib response, Mok noted. No significant PFS or OS benefit was observed for sorafenib in either KRAS mutated or KRAS wild-type NSCLC. For KRAS mutation, the biomarker treatment interaction analysis had a P value of .696; for KRAS wild-type, the biomarker interaction analysis had a P value of .743. “KRAS mutation status did not appear to influence response to sorafenib. The interaction analysis was negative for both PFS and OS,” Mok said. “Based on current data, we hypothesize that EGFR mutation is a predictive biomarker for sorafenib in treatment of patients with advanced NSCLC,” Mok stated. He added that the search for biomarkers that predict response is critical for progress. “Otherwise we are treating blindly in the dark,” he commented. u

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2012 ESMO Congress

Whole Genome Testing Moves Forward in Breast Cancer Phoebe Starr

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esearchers presented the first large study to test the entire genome of individualized breast cancers to help personalize cancer at the 2012 ESMO Congress. They found that this approach is feasible and enables identification of genetic alterations that can be targeted by available drugs. They also saw early signs of clinical activity with this approach. “Now that a number of drugs are available that target specific genetic alterations in cancers, genetic testing is usually performed. In most of these cases, these genetic testing approaches analyze only a limited number of genes,” said lead author of the study, Fabrice André, MD, Institut Gustav Roussy, Villejuif, France. Theoretically, whole genome testing can identify both frequent and rare genetic alterations. “In addition, this approach allows us to quantify the level of genomic instability, and to detect whether driver mutations are associated with genomic alterations involved in resistance to specific targeted agents,” André explained. Also, whole genome approaches could reduce expenditures related to genetic testing, because new bioassays would not need to be developed for each new targetable genetic alteration discovered in cancer. “An all-in-one assay could substitute for multiple tests,” explained Monica Arnedos, MD, one of the study coauthors. The SAFIR01 trial analyzed the entire genome from a biopsy of a metastatic lesion prospectively. “We sought to identify molecular alterations and try to match these with a targeted therapy for each patient,” Arnedos said. The investigators also wanted to determine the best technology for looking at the whole genome, and the best algorithm for identifying potential therapeutic targets. Most important, they plan to evaluate whether whole genome testing improves outcomes. “First we did a pilot study in 108 patients where we performed whole genome analysis to determine feasibility. The techniques we used were array CGH and Sanger sequencing. Once feasibility was determined, we initiated

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the French national program, funded by French NCI and sponsored by UNICANCER,” Arnedos told listeners. SAFIR01 was performed at 18 centers. As of September 23, 2012, biopsies were obtained from a metastatic lesion in 402 breast cancer patients, including 26 patients whose biopsies were under study. A genomic result was generated in 276 patients, including whole genome analysis in 251 patients. A targetable genomic alteration was identified in 172 (69%) of those patients. No patients had any evidence of disease progression while on treatment. “Seventy-six genetic alterations were considered rare, low-frequency alterations. These alterations are unexpected, highlighting the need for whole genome approaches,” she said. At the time of the ESMO Congress, 26 patients had received therapy targeted to their specific genetic alterations. Evidence of activity was observed in 8 of these patients. The data are still quite preliminary. “In the next 3 years, we expect to have treated 80 patients with metastatic breast cancer using matched therapy selected from whole genome analysis,” Arnedos said. The researchers plan to develop approaches to decrease biopsy failure and to improve access to targeted therapies. Arnedos said these biopsies and tests are challenging. In 105 cases, the tumor sample was not sufficient for analysis, and in 19 cases the whole genome analysis was not interpretable. The next trial, called SAFIR 2, will be a randomized trial comparing treatment based on whole genome testing versus treatment not driven by tumor biology. “This approach is extremely important. It will identify patients who could benefit from a targeted drug not necessarily approved for that type of cancer. This approach will change the way we approve drugs. We have seen surprising compounds emerge that are effective. This will affect the regulatory process,” stated the press conference moderator, Christoph Zielinski, MD, Medical University of Vienna, Austria, who was not involved in these studies. u

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PMPM O C

ERSONALIZED EDICINE IN ONCOLOGY

ALL FOR PAPERS

Personalized Medicine in Oncology’s mission is to deliver practice-changing information to clinicians about customizing healthcare based on molecular profiling technologies and each patient’s unique genetic blueprint. Our vision is to transform the old medical model of stratified medicine into a new model of personalized care where all decisions and practices are tailored to the individual. The goal of Personalized Medicine in Oncology is to sensitize practitioners to the performance realities of new diagnostic and treatment discoveries and to clarify molecular profiling technologies as they relate to diagnostic, prognostic, and predictive medicine. PMO will feature diagnostic and clinical treatment information concerning these 3 root aspects of personalized medicine in oncology. Readers are invited to submit articles for consideration in the following categories:

Biologicals in Trial •

Exploring the challenges of clinical trial design and patient enrollment

Presentation of emerging clinical data

Genetic Profiling Technologies •

What technologies are available to clinicians and consumers and their impact on diagnostic, prognostic, and predictive medicine

In Practice Predictive Models and Diagnostics •

Genetics and Biomarkers •

A practical guide for community-based oncologists discussing clinical applications and strategies for incorporating personalized medicine techniques into practice

Development of treatment algorithms

A look at available diagnostic technologies and implementation in the community practice setting

Exploring genetic discoveries and impact on predictors of disease and therapeutic response

The Cost of Personalized Medicine •

Personalized medicine policy drivers

Payer coverage of diagnostics and biologics

N=1 •

Case studies, patient-reported outcomes, defining treatment goals, partnering with patients and caregivers

Submit the entire manuscript and a cover letter stating the objectives of the article to PMO@greenhillhc.com. Manuscripts should follow the Author Guidelines available at www.PersonalizedMedOnc.com. "


Interview With the Innovators

Cultivating Personalized Medicine Clinical Acumen in the Management of Breast Cancer: An Interview With Edith Perez, MD Edith Perez, MD Deputy Director Mayo Clinic Cancer Center, Florida

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f any cancer can be said to have launched personalmedicine in breast cancer, she mentions not the adized medicine into orbit and establish it as the stanvances in science but the lives that will be saved dard for all cancer therapy to aspire toward, it is through a new understanding and application of its scibreast cancer. The discovery of the esence. Asked about the “competing” trogen receptor (ER) and HER2 biomodel of predictive modeling versus markers has astonished healthcare biomarkers, she instantly embraces it professionals and the public alike and as a welcome and helpful adjunct to raised forever the bar of cancer care. biomarkers. This same inclusiveness What conditions have arisen to make extends to wellness-based healthcare, breast cancer the envy of other cancer to patient-reported outcomes, to the researchers, and how is this field levlink between the clinical, business, eraging its discoveries to unlock new and policy sectors of healthcare in opportunities for researchers and making breast cancer research get tracclinicians alike? And most important, tion and stay on course. how can today’s practicing oncologists And what is that course? Without Edith Perez, MD put into practice the lifesaving techhesitation, she advances the translaniques of breast cancer personalized tional research goal: a new molecular medicine, ally them with the conventional medicine classification of breast cancer that identifies the relethat still dominates the field, and cultivate a base of vance of types of breast cancer to drive treatment deciknowledge of this burgeoning, data-heavy field of medsions. For Dr Perez, it’s all about treatment. As one of ical science? the leading researchers in the area of cancer research To capture the essence of the breast cancer treatthat other cancer experts look to as a model of success, ment revolution, we interview Dr Edith Perez. Transwe sought her out to give not only an empirical view of lational research is the soul of Dr Perez’s work. Asked the principles and drivers of breast cancer success and what she sees as the vision statement of personalized future research goals, but also to help define the issues

Dr Perez is Deputy Director, Mayo Clinic Cancer Center in Florida, and director of the Breast Program and the Serene M. and Frances C. Durling Professor of Medicine at Mayo Medical School. She is a cancer specialist and an internationally known translational researcher at Mayo Clinic. Her roles extend nationally, including chairing the Breast Committee for the North Central Cancer Treatment Group, as well as other positions within the American Association for Cancer Research, the American Society of Clinical Oncology, and the National Cancer Institute. Dr Perez has developed and is involved in a wide range of clinical trials exploring the use of new therapeutic agents for the treatment and prevention of breast cancer. She also has developed studies to evaluate the role of genetic biomarkers in the development, aggressiveness, and therapeutic efficacy for breast cancer.

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helpful to all cancers. Above all, she applauds the principle of personalized medicine in oncology: to cultivate an understanding by practicing oncologists of the biological basis of cancer and the pharmacodynamic basis of the drugs – biologicals and conventional alike – used to combat it. Asked what the practicing oncologist must glean from the informational overload of this new science to keep up, her advice was immediate and precise:

“The practicing oncologist needs to understand genes, the regulation of genes, protein expression, and then metabolomics.” We turn now to a tour of personalized medicine for the practicing oncologist by Dr Edith Perez, who describes the strategy and tactics that she and her fellow colleagues are employing to transform what was once a universal killer into a manageable, nonlethal condition.

PMO How would you define or otherwise describe personalized medicine and its role in the clinical management of breast cancer? Dr Perez It’s our ability to identify markers of the tumor of the host that impact pathogenesis so that we can target them to optimize treatments for the individual patients. PMO How does predictive modeling assist in this process, compared with the more specific matter of biomarkers?

we need a fairly large number of patients with appropriate molecular testing to reach definite conclusions. I’m very enthusiastic, though, about the way the field is moving, but at the same time I’m concerned about the volume of reports that are published in abstract form or peer-reviewed manuscripts every month in this field that may not have a robust number of patients to reach definite conclusions. PMO Yes, and that’s what you’re looking for: an enriched patient population. Dr Perez Yes, and we’ll get to that, but another area that is tremendously important in terms of interpretation of the literature is that it has become easier for journals to prominently publicize and publish material that reflects a possible relationship between a biomarker and patient outcome. It remains difficult to print data of negative associations. For the needs of patients, reports of negative associations are as important, so that researchers don’t have to keep repeating the same work, as well as acknowledge the work that is done by not only the patients volunteering tumor specimens but also the investigators who have done the calculation work. I would like to ask for a call to analyze and publicize the data, even if they are negative, because that is the way to advance the field. PMO Yes, everyone from the public to the research community is getting this skewed, overly positive perspective on the degree of success – and the ease of success – that’s present in personalized medicine. Without sufficient recognition of the research failures, we will lose the impetus to continue pursuing research areas that are going to overcome these setbacks.

It’s our ability to identify markers of the tumor of the host that impact pathogenesis so that we can target them to optimize treatments for the individual patients. Dr Perez Predictive modeling can be really fascinating and provide us with some guide of the path that we want to follow. The same applies to preclinical modeling, utilizing cell lines or newer models. In the area of predictive medicine for patients, or personalized medicine, we have realized that all of these models really need to be validated with a robust number of patients who have been followed for an adequate time, along with having appropriate tumor specimens to test these biomarkers. We can chase a lot of ideas with theoretical concepts and preclinical models, and even studies in a small number of patients. But in the area of oncology, certainly in the area of breast cancer, we have come to a realization that these tumors are heterogeneous. There are many genes and proteins that impact the pathogenesis. Thus,

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Dr Perez Yes, but I wouldn’t actually use the word failure. When we have hypotheses, it’s our job as scientists and translational investigators to validate the hypothesis or not, and so our obligation is to be able to publish, to report on the information we have provided. That’s the way I look at the field. But I am very enthusiastic about the way we’re moving because we are all learning about better ways to do the analysis. We have started to look more carefully at the way the specimens are collected and stored, the need to validate any laboratory testing that we do with appropriate controls, and potentially even have more than 1 pathologist look at stains or results of gene analysis. And also how carefully we have to analyze the data from these markers in a blinded way in the context of patient outcomes, so that the results that we obtain truly could relate with patient performance. PMO You’re seeing basically a success in changing not just prognostic expectations that personalized medicine provides, but even changing the culture of medicine regarding prevention, diagnosis, and treatment? Dr Perez Well stated. Let me phrase the situation in this way. It is clear that we have made advances over the past 30 to 40 years, but at this time I think we are in a position for the advances to be of much greater magnitude than what we have been able to accomplish. Second, the 2 basic stories that are most positive in the setting of breast cancer are following the only 2 targets that we currently use for therapeutic decisions, which include the ER and HER2. At the same time we know that we have to move beyond these 2 markers in the context of 24,000 genes, validation of the expression of these genes, then posttranslational modification approaches. PMO What is the degree of the proliferation, if you will, of personalized care in breast cancer compared with other cancers, and what would be the reason for the differences in the degree of personalized medicine proliferation across these cancers? Dr Perez I think there’s a wide interest in the field of personalized medicine for all malignancies. The 1 issue in the setting of breast cancer that makes it unique is

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An avid runner, Dr Perez, among her many contributions to breast cancer research, participates in a race for the finish.

composed of 2 things. Number 1, breast cancer is a common disease, and we have had some good therapies that have allowed many patients to survive for longer times than other tumor types, which has then led to an advocacy coming from the patient’s standpoint to get researchers to do research in the setting of breast cancer.

It is clear we have made advances over the past 30 to 40 years, but at this time I think we’re in a position for the advances to be of much greater magnitude... Also a positive for breast cancer has been the fact that some of these therapies that we have found to be beneficial really have impacted the lives of so many, so essentially we have used the low-hanging fruit. Some things have worked very well, so we have a lot of impetus to keep moving in that direction. But clearly at the same time I’m really very happy that this field of personalized medicine has started to pan out in the setting of some lung cancers and also some other cancers, especially melanoma, where we’re starting to see some really fascinating data. But the issue is going to be, are these new data going to impact the 5-year survival

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of those diseases, which remain way below 20%. So although the data with the EGFR inhibitors for lung cancer, for the ALK inhibitors for lung cancer, and the data for the BRAF inhibition in the setting of melanoma, look very interesting, we need a little bit longer follow-up, whereas in breast cancer, we know that targeting ER, targeting HER2, truly impacts the longterm outcome of patients in addition to having an impact on short-term response or progression-free survival. Initially it seems like the group of individuals involved in breast cancer is quite cohesive at the global level, but this is happening also with other tumor types. But we have had long-term meetings where research data are discussed on an ongoing basis so that we don’t duplicate work, and at the same time we collaborate with each other to make important data available.

In the area of microRNAs, there are hundreds of RNAs that have now been identified, and RNAs appear to modulate the function of about a third of our genes. PMO What would be some of the important examples of personalized medicine algorithms of this type as they’re generally understood? And next, what are some examples of such algorithms that have been discovered by researchers but have failed to be adopted by oncologists expeditiously, and how can we expedite the uptake of that kind of progress for breast cancer patients? Dr Perez First of all, one of the issues that we have to deal with, and I deal with this all the time, is how to convey the message of the work that is currently being done, as well as the complexity of the work being done, to the physicians who are mainly involved in practice, or to physicians or to philanthropists who we absolutely need for support of some of this innovative work. We have to distill the technical jargon to understandable concepts that can be conveyed to people because they have to be part of the team as we try to solve this puzzle of breast cancer. PMO Yes, including the investors. Dr Perez Absolutely. Then we as scientists also have

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to keep in mind that the honesty related to our research findings is something that cannot be underestimated. We have to be judicious in the way we report our own data and just absolutely always, always tell the truth, not make more than what we have, not make less than what we have. We’ll always be 100% honest and accurate related to the information we share with others. We cannot compromise on this issue because we may send confusing messages to all of these stakeholders as well as all the researchers. In terms of personalized medicine algorithms, I think probably the most important thing I can say is that we have to work with our pathologists to be able to collect the tumor specimens in a consistent way, and for pathologists to follow algorithms and recommendations that have been generated by expert panels related to exposure of tissues to various elements so that the tissue remains appropriate for testing of these markers. At the same time it is very important to realize that at least from the treatment standpoint, depending on the data that we get from these molecular profiles, the clinical condition of the patient is also very important. So we don’t manage patients only based on laboratory results. We manage patients based on the prior therapy they may have had, the patient’s overall condition, and organ function. We have to put all the pieces together, but I hope that in the next few years we’re going to learn so much about the molecular profile of these tumors that we’ll be able to be a lot smarter related to putting together molecular profiles with patient profiles to come up with the best treatments. When we think about personalized medicine and molecular markers, there are so many different things that we can look at. We can look at whole genome. We can look at exomes. We can look at RNA. We can look at proteins. We can look at microRNAs, RNAs that modulate function of genes. So this is a very vast field that speaks to the complexity of what we need to elucidate. In the area of microRNAs, there are hundreds of RNAs that have now been identified, and RNAs appear to modulate the function of about a third of our genes. PMO Given the limitations of personalized medi-

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cine, empirical science continues to play a predominant role in cancer care and in research, and we won’t be abandoning this approach anytime soon. Because of the need for personalized medicine and empirical medicine to coexist, we’d welcome your comments to put personalized medicine into an operational perspective. Dr Perez I think in order to provide personalized medicine there will always be a portion of empiricism, because I don’t know if we are going to be able to devise a treatment that will target all molecular abnormalities that may be driving a tumor for each individual patient. I think what we’re going to be able to do is subclassify patients based on pathways, and I hope that will give us enough information to be able to have maybe 10 types of breast cancer and guide therapy based on that. Ideally, if a tumor is found to have 3 abnormalities and we can find 3 drugs that address those abnormalities, then obviously we will be able to provide individualized care to each patient. But I think the way things are going, each breast cancer may have many more than 3 abnormalities, so we may not be able to treat a patient with 20 drugs. A realistic approach means that, while most of what we do now is empiric, the balance will change. But we’re going to have to be realistic related to whether we will address every target in the tumor. Think about this: It’s more than just being able to identify the abnormalities in the tumor with genomic analysis. We need to identify whether they are drivers of tumor growth or metastatic potential. PMO Is there any strategic guidance that you might offer practicing oncologists to give appropriate emphasis to personalized medicine in order to integrate it into their clinical strategic process? Dr Perez I think the guidance is going to be that we are going to need more access to more specimens in the evolution of the disease process to be able to manage patients in an optimal way. Right now we’ve been practically relying on the limited molecular testing that we can do on the original tumor and expect that that will provide us the guide on how to manage patients when they develop relapse, when they go into a metastatic setting, when they develop further progression, so I think that has to be the guide.

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Dr Perez and her team are focusing on developing a new molecular classification for breast cancer.

Dr Perez with E. Aubrey Thompson, PhD, Professor of Biochemistry and Molecular Biology at the Mayo Clinic in Florida. We may need to be much more attentive and consistent in our recommendations to obtain biopsies so that we can do this molecular analysis at the different stages of the disease process. Then people like me and others will figure out the best tools with which to evaluate the molecular changes. But without tissue that can be collated with patient outcome, we will not be able to advance as quickly as we should. PMO How would you advise oncologists so that

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they could develop a sophistication in their understanding of personalized medicine techniques to distinguish real innovation from just novelty? Dr Perez Very good point. I think it’s going to be up to all of us. I think it’s our responsibility to educate physicians, because the terminology is different from what they learned in medical school. So we need different specimens to do different types of gene sequencing. We need to help them understand the difference between doing an exome analysis versus a whole genome sequencing and the data that we can get. There’s a realization that we’ll need to work together to educate practicing oncologists, and it will be done. PMO Can you describe breast cancer patient subgroup risk stratification as part of the personalized medicine revolution? What are the different categories of breast cancer prognostic expression signature sets?

Right now the best we can do when we have a patient with advanced cancer is to choose any of the drugs that have been approved by regulatory agencies. Dr Perez They’re currently being defined. That’s actually 1 of the challenges in the field. Different people are using different technologies to come up with signatures, and the genes from one signature do not correlate with the genes found with the other mechanisms, so these signatures seem to be nonconsistent, in my opinion. That’s because the platforms used to develop the signatures are different. So I think as we get more and more into understanding the exome, and we get to understand the whole genome sequencing, this will get better, because right now we just have a smatter of signatures and no real clear-cut relation between one versus the other. To complicate matters even more, not many studies have been done in which a specific set of tumors has been tested using different techniques to see if the signatures that are derived are the same or different. PMO How do they reflect tumor status? Dr Perez Well, right now we and others are working

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on redeveloping signatures for what’s ER-positive versus ER-negative breast cancer. I think we will eventually develop signatures for patients with HER2-positive breast cancer that will have a likelihood of responding to trastuzumab or lapatinib or other agents. Right now the status of the signature is that no one can tell me whether it’s a primary tumor or a metastatic site. That’s not the area that we are going to be pursuing. We’re just going to take a tumor wherever it is, try to understand the biology so that we can offer the best therapy for our patients. PMO Drilling down 1 step further. These signature sets, how do they help delineate outcome? Dr Perez When we find mutations in the signature sets that are important for the pathophysiology of the breast cancer, then we’ll be able to really devise therapeutic strategies using combinations of agents, and that will be directly correlated with improved patient outcome. At least that’s the way I envision this. PMO Historically, how reliable are they? Dr Perez Well, we haven’t had the tools in the past. Right now the best we can do when we have a patient with advanced cancer is to choose any of the drugs that have been approved by regulatory agencies. Each drug has approximately a 20% to 30% activity, and that’s just not good enough. I hope that we’ll get to the point where we’ll be able to do the analysis of the tumors and tell the patient, “hey, your tumor has an 80% chance of benefiting.” Even with that I’m going to be very happy. PMO Are these codified in algorithms by the National Comprehensive Cancer Network or American Society of Clinical Oncology? Dr Perez Not yet, because there are so many signatures that are being published, based on what I consider to be evolving technologies, that they have not been validated by others enough to really have big names yet. PMO What are the specific breast cancer patient types – and tumor types? Is the revelation of personalized medicine processes in breast cancer leading to subspecialization based on these patient types and tumor types? Dr Perez This will happen, but right now they’re really not validated enough for me to tell you that there

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are going to be 4 subtypes of breast cancer, or 10. I think this is going to require a little bit more work. Right now we’re still using ER/PR [progesterone receptor] and HER2 to make the decisions for patients. Everything else is to be validated. PMO In what way would this profiling aid the oncologist in risk stratification, in establishing prognostic expectations, and in identifying personalized medicine diagnostic tests and treatment? Dr Perez Just to give you an example of how this is going to be revolutionized: Right now when a new patient is diagnosed with breast cancer, we do surgery and take the tumor out, and then we give adjuvant therapy, or we may decide to give neoadjuvant therapy. But there are essentially about 5 drugs that are used where I think there may be 40 abnormalities in the breast cancer that may be important to drive pathogenesis. I think in the future we’re going to have many more agents that are really directed toward their normal targets. Instead of having 1 general recommendation for adjuvant therapy, we may have 10. Because right now everybody’s treated the same way, bottom line. Everybody gets chemotherapy, that is anthracycline, taxane-based chemotherapy. That’s it. That is the backbone of treatment for patients with cancer, even with early-stage breast cancer, and we need to be much more specific than you’re seeing, you know, 2 classes of drugs that are most effective. PMO If you could, please discuss the discovery and advancement of the approved biomarkers for breast cancer, and the investigational ones. Dr Perez In terms of a routine management of patients with breast cancer, there are only 3 markers that are done: ER, PR, and HER2. And it’s not even HER2/neu. HER2/neu refers to the HER2 gene, so we prefer to call it HER2 because HER2 addresses evaluation of the protein or the gene, and we can do either for a therapeutic decision. We don’t have to do both. EGFR has been looked at, and it has not panned out yet as a marker to drive therapy in patients with breast cancer. Regarding p53, certainly we know it’s expressed as abnormal in a majority of tumors, but it’s not tumor-

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Offering patients optimal therapies with minimal side effects is at the heart of Dr Perez’s work. specific enough to guide therapy, and people have tried to look at p53 in the context of anthracyclines, but again nothing specific. So we just wonder when looking at AKT, looking at PA3 kinase, looking at IGF, are those markers going to be important, but right now we don’t know. MET may be a very important marker in breast cancer. Protein kinase D1 may be important, but again, all these things are a part of research right now. Nodule may be important. But we need to figure out what those markers mean in the context of the physiology of this disease. PMO Why are these attracting the most interest and research? Dr Perez One of the reasons is that companies have drugs that target a particular marker, because the other markers that we haven’t talked a lot about today are the microRNAs, which may control 30% of our genome, and theoretically they could be extremely important. But more work needs to be done in that area.

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Another area certainly is phosphorylated proteins, but that is very difficult to test for because phosphorylation occurs, and in 1 minute it’s gone, so you cannot assay for the impact of phosphorylated proteins in the context of tumors. We can do that very well in cell lines, but that’s very different than in humans, so I think that’s going to be a very challenging area to conquer. The other biomarker of interest has been circulating tumor cells. Before we can really explore this more, we need to first understand if the genomic markers in circulating tumor cells are equivalent to the genomic markers of the tumors that are invading different organs. And second, can we assay for a variety of molecular markers in circulating tumor cells when we may have just 5 cells per mL? When is the technology going to be good enough that we can take 2 cells and do enough biomarkers in those 2 cells to be able to drive a better understanding of breast cancer? If we can avoid having to do invasive biopsies and just assay the circulating tumor cells, that would be great. But before we do this we again need to address those 2 issues: are they the same cells, or is there something different about the cells that decide to shed and be in the circulation compared with the tumors that are invading the liver and causing death? PMO What would you regard as landmark research in personalized medicine in breast cancer and the clinical basis for its significance? Dr Perez The term “personalized medicine” is a very broad term, but essentially the most important biomarker in addition to ER really has been HER2. HER2 was identified, and then we developed a strategy in the metastatic setting to target HER2, clearly improving survival. And then we were able to take that marker and use these agents in the adjuvant setting, and we decreased relapse by 50%, and we are improving survival by 38%. So now by using this biomarker, this is part of personalized medicine. We’ve been able to change the natural history of HER2-positive breast cancer from a very aggressive type of breast cancer to one that is very manageable and potentially curable. PMO Are there any particular clinical, business, or

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policy factors impeding progress in breast cancer, especially involving personalized medicine? Dr Perez It’s really time and money, because we need to put enough resources not only to have sequencing machines but to have the patient resources to have enough tumor specimens to not only put the specimens in a machine but also to have the bioinformatics personnel to put the story together. There has to be a focused and concerted effort to devote enough resources to this area in a timely fashion to really get the answers. PMO Are there particular areas of consensus and particular areas of controversy concerning biomarkers in particular and personalized medicine in general involving breast cancer that you see as standing out, very obvious ones? Dr Perez The controversy is, in my opinion, that some people feel a lot of gene work has been done and “it hasn’t translated into anything yet.” Some people have become naysayers because they’re not as involved as some of us are, trying to really make specific advances on this. I think that is the main controversy. This is a new field, and people don’t understand it. Breast cancer is a genetic disease, and we really need to unravel the genetics of this disease, what drives gene function, what is the product of those genes, so that we can realize this dream, going back to the dream of personalized medicine for our patients with breast cancer. PMO In your research priorities, are you going to focus in 1 area? Dr Perez Absolutely, although our interests are very vast. I hope that our work will eventually lead to a new molecular classification of breast cancer and we’ll identify the relevance of types of breast cancer to drive treatment decisions. Along those lines, this finding of fusion genes in breast cancer may be very important. But first of all, we need to identify what the redundant fusion genes are, and number 2, do they have any associated protein products, and can they be utilized for the development of new treatments. PMO That gives us a perfect place to end our discussion today. Thank you for your time. Dr Perez My pleasure. u

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• Melanoma • Basal Cell Carcinoma • Cutaneous T-Cell Lymphoma • Squamous Cell Carcinoma • Merkel Cell Carcinoma

July 26-28, 2013 Hyatt Regency La Jolla • San Diego, California

PROGRAM OVERVIEW

CONFERENCE CO-CHAIRS

A 2-day congress dedicated to informing, educating, and fostering the exchange of clinically relevant information in the field of cutaneous malignancies on topics in melanoma, basal cell carcinoma, cutaneous T-cell lymphoma, squamous cell carcinoma, and Merkel cell carcinoma, including: • Epidemiology and genetic/environmental factors • Molecular biology and cytogenetics related to the pathogenesis of cutaneous malignancies • Risk stratification based on patient and tumor characteristics • Principles of cancer prevention of melanoma and basal cell carcinoma • Current treatment guidelines • Emerging treatment options for personalized therapy • Future strategies in management based on translational data from current clinical trials and basic research

LEARNING OBJECTIVES Upon completion of this activity, the participant will be able to: • Review the molecular biology and pathogenesis of cutaneous malignancies as they relate to the treatment of cutaneous T-cell lymphoma, basal cell carcinoma, Merkel cell tumors, and malignant melanoma • Compare risk stratification of patients with cutaneous malignancies, and how to tailor treatment based on patient and tumor characteristics • Summarize a personalized treatment strategy that incorporates current standards of care and emerging treatment options for therapy of patients with cutaneous malignancies

TARGET AUDIENCE This activity was developed for medical and surgical oncologists, dermatologists, radiation oncologists, and pathologists actively involved in the treatment of cutaneous malignancies. Advanced practice oncology or dermatololgy nurses, oncology pharmacists, and researchers interested in the molecular biology and management of cutaneous malignancies are also encouraged to participate.

DESIGNATION OF CREDIT STATEMENTS SPONSORS This activity is jointly sponsored by Medical Learning Institute Inc, Center of Excellence Media, LLC, and Core Principle Solutions, LLC.

COMMERCIAL SUPPORT ACKNOWLEDGMENT Grant requests are currently being reviewed by numerous supporters. Support will be acknowledged prior to the start of the educational activities.

Sanjiv S. Agarwala, MD Professor of Medicine Temple University School of Medicine Chief, Oncology & Hematology St. Luke’s Cancer Center Bethlehem, Pennsylvania

REGISTERED NURSE DESIGNATION Medical Learning Institute Inc Provider approved by the California Board of Registered Nursing, Provider Number 15106, for 12.0 contact hours.

REGISTERED PHARMACY DESIGNATION The Medical Learning Institute Inc is accredited by the Accreditation Council for Pharmacy Education as a provider of continuing pharmacy education. Completion of this knowledge-based activity provides for 12.0 contact hours (1.2 CEUs) of continuing pharmacy education credit. The Universal Activity Number for this activity is (To be determined).

Professor Dr. Med. Axel Hauschild Professor, Department of Dermatology University of Kiel Kiel, Germany

AGENDA* FRIDAY, JULY 26, 2013 3:00 pm – 7:00 pm

Registration

5:30 pm – 7:30 pm

Welcome Reception/Exhibits

SATURDAY, JULY 27, 2013 7:00 am – 8:00 am

Breakfast Symposium/Product Theater/Exhibits

8:00 am – 8:15 am

BREAK

8:15 am – 8:30 am

Welcome to the Second Annual World Cutaneous Malignancies Congress — Setting the Stage for the Meeting - Sanjiv S. Agarwala, MD

8:30 am – 11:45 am General Session I: A Clinician’s Primer on the Molecular Biology of Cutaneous Malignancies • Keynote Lecture Understanding the Basic Biology and Clinical Implications of the Hedgehog Pathway • Keynote Lecture Pathogenesis of Merkel Cell Carcinoma: An Infectious Etiology? - Paul Nghiem, MD, PhD 12:00 pm – 1:00 pm Lunch Symposium/Product Theater/Exhibits 1:00 pm – 1:15 pm

BREAK

1:15 pm – 4:30 pm

General Session II: Current Treatment Guidelines in Cutaneous Malignancies • Case Studies Optimal, Value-Based Therapy of Cutaneous Malignancies: The Expert’s Perspective on How I Treat My Patients • Panel Discussion Management Controversies and Accepted Guidelines for the Personalized Management of Cutaneous Malignancies • Keynote Lecture New Combinations in Melanoma: A Role for MEK + BRAF and Anti–PD-1

4:30 pm – 6:30 pm

Meet the Experts/Networking/Exhibits

PHYSICIAN CREDIT DESIGNATION The Medical Learning Institute Inc designates this live activity for a maximum of 12.0 AMA PRA Category 1 Credits ™. Physicians should claim only the credit commensurate with the extent of their participation in the activity. This activity has been planned and implemented in accordance with the Essential Areas and policies of the Accreditation Council for Continuing Medical Education through the joint sponsorship of the Medical Learning Institute Inc and the Center of Excellence Media, LLC. The Medical Learning Institute Inc is accredited by the Accreditation Council for Continuing Medical Education to provide continuing medical education for physicians.

Steven J. O’Day, MD Hematology/Oncology Director of Clinical Research Director of Los Angeles Skin Cancer Institute at Beverly Hills Cancer Center Clinical Associate Professor of Medicine USC Keck School of Medicine Los Angeles, California

SUNDAY, JULY 28, 2013 7:00 am – 8:00 am

Breakfast Symposium/Product Theater/Exhibits

8:00 am – 8:15 am

BREAK

8:15 am – 8:30 am

Review of Saturday’s Presentations and Preview of Today’s Sessions

8:30 am – 11:45 am General Session III: Review of Emerging Treatment Options for Cutaneous Malignancies General Session IV: Challenges for the Cutaneous Malignancies Clinician • Panel Discussion How Can the Healthcare Team Work Best Together to Deliver Value-Based Care in Cutaneous Malignancies? 12:00 pm – 1:00 pm Lunch Symposium/Product Theater/Exhibits

CONFERENCE REGISTRATION

1:00 pm – 1:15 pm

BREAK

1:15 pm – 2:45 pm

General Session V: “Hot Data” — What I Learned at Recent Meetings: Focus on Cutaneous Malignancies

2:45 pm – 3:00 pm

Closing Remarks - Steven J. O’Day, MD

EARLY BIRD REGISTRATION NOW OPEN! $175.00 UNTIL APRIL 30, 2013

www.CutaneousMalignancies.com

*Agenda is subject to change.

For complete agenda please visit www.CutaneousMalignancies.com


Continuing Medical Education To receive credit, complete the posttest at www.mlicme.org/P12038E.html.

Clinical Approaches to Targeted Technologies: Implementing the Promise of Prognostic Precision Into Personalized Cancer Care An ancillary educational symposium, Clinical Approaches to Targeted Technologies: Implementing the Promise of Prognostic Precision Into Personalized Cancer Care, was held June 2, 2012, in conjunction with the 2012 American Society of Clinical Oncology (ASCO) Annual Meeting in Chicago, Illinois. The symposium focused on evolving regional standards of care and cutting-edge information and emerging data on molecular markers that can impact treatment strategies for specific tumor types. This continuing medical education activity brings together highlights, summaries, and expert commentary from the symposium on the current and future direction of the application of biomarkers in personalized care for patients with solid tumors.

The Evolution of Personalized Biomarker-Based Therapy for Advanced Non–Small Cell Lung Cancer Roy S. Herbst, MD, PhD, from the Yale Comprehensive Cancer Center and Yale School of Medicine in New Haven, Connecticut, began the symposium by

Sponsors This activity is jointly sponsored by Medical Learning Institute Inc, Core Principle Solutions, LLC, and Center of Excellence Media, LLC. Commercial Support Acknowledgment This activity is supported by educational grants from Boehringer Ingelheim and Eisai Pharmaceuticals. Target Audience This educational activity is directed toward medical oncologists, pathologists, geneticists, advanced practice oncology nurses, research nurses, clinical oncology pharmacists, genetic counselors, and other healthcare providers involved in the management of patients with solid tumors and interested in the use of molecular tumor biomarkers to help optimize patient care. Purpose Statement The purpose of this activity is to enhance competence of medical oncologists, pathologists, geneticists, advanced practice oncology nurses, research nurses, clinical oncology pharmacists, genetic counselors, and other healthcare providers concerning the application of biomarkers in personalized care for patients with solid tumors. Physician Credit Designation The Medical Learning Institute Inc designates this enduring material for a maximum of 1.25 AMA PRA Category 1 Credits™. Physicians should claim only the credit commensurate with the extent of their participation in the activity. This activity has been planned and imple-

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discussing the magnitude of the problem of non–small cell lung cancer (NSCLC). Lung cancer (both small cell and non–small cell) is the second most common cancer in both men and women (not counting skin cancer). In men, prostate cancer is more common, while in women breast cancer is more common. In the United States alone, approximately

mented in accordance with the Essential Areas and policies of the Accreditation Council for Continuing Medical Education through the joint sponsorship of the Medical Learning Institute Inc, Core Principle Solutions, LLC, and the Center of Excellence Media, LLC. The Medical Learning Institute Inc is accredited by the Accreditation Council for Continuing Medical Education to provide continuing medical education for physicians. Registered Nurse Designation Medical Learning Institute Inc. Provider approved by the California Board of Registered Nursing, Provider Number 15106, for 1.25 contact hours. Registered Pharmacy Designation The Medical Learning Institute Inc is accredited by the Accreditation Council for Pharmacy Education as a provider of continuing pharmacy education. Completion of this knowledge-based activity provides for 1.25 contact hours (0.125 CEUs) of continuing pharmacy education credit. The Universal Activity Number for this activity is 0468-9999-12-032-H01-P. Learning Objectives Upon completing this activity, the participants will be able to: • Assess emerging data and recent advances in the discovery of solid tumor biomarkers, their impact on the treatment of patients with solid tumors, and how to integrate key findings into clinical practice • Discuss the role of tumor biomarkers in designing personalized therapy for patients with solid tumor cancers, including management of treatment-related adverse events

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To receive credit, complete the posttest at www.mlicme.org/P12038E.html.

Figure 1. Five-Year Survival Rates for Patients With NSCLC by Stage2

5-Year Survival Rate (%)

226,160 new cases of lung cancer (116,470 in men and 109,690 in women) will be diagnosed in 2012.1 Lung cancer is by far the leading cause of cancer death among both men and women. Each year, more people die of lung cancer than of colon, breast, and prostate cancers combined. In the United States, an estimated 160,340 deaths will occur in 2012 from lung cancer (87,750 in men and 72,590 among women).1 Five-year survival rates for patients with advanced NSCLC are extremely low (Figure 1),2 indicating an urgent need for better therapies. However, the development of new therapies is fraught with challenges, including long timelines, great attrition, and huge expense. As illustrated in Figure 2, it takes approximately 24 drug candidates and a period of 14 or more years of research and development to result in the launch of just 1 new drug.3,4 According to Herbst, “The goal is to identify a biomarker early on, so we can test the right drug

60 50

49 45

40 31

30

30 20

14

10 0

5

IA

IB

IIA

IIB Stage

IIIA

IIIB

NSCLC indicates non–small cell lung cancer.

in the right patient at the right time, thus decreasing the amount of time the drug takes in clinical trials.”

Disclosures Before the activity, all faculty and anyone who is in a position to have control over the content of this activity and their spouse/life partner will disclose the existence of any financial interest and/or relationship(s) they might have with any commercial interest producing healthcare goods/services to be discussed during their presentation(s): honoraria, expenses, grants, consulting roles, speakers bureau membership, stock ownership, or other special relationships. Presenters will inform participants of any off-label discussions. All identified conflicts of interest are thoroughly vetted by Medical Learning Institute Inc for fair balance, scientific objectivity of studies mentioned in the materials or used as the basis for content, and appropriateness of patient care recommendations.

related to the content of this CME/CPE/CE activity for any amount during the past 12 months.

Planners and Managers Disclosures Karen Cooksey, Medical Writer, has nothing to disclose. William J. Wong, MD, MLI Reviewer, has nothing to disclose. Teresa Haile, RPh, MBA, MLI Reviewer, has nothing to disclose. Kathryn Gada, MSN, MLI Reviewer, has nothing to disclose.

Instructions for Credit

Faculty Disclosures Roy S. Herbst, MD, PhD, Professor of Medicine and Pharmacology, receives grant support/research funding from Amgen, AstraZeneca, Bristol-Myers Squibb, Genentech, Geron, Imclone, Novartis, Oncothyreon, OSI Pharmaceuticals, Pfizer, and Sanofi Aventis; is a paid consultant for Allos Therapeutics, Argennix Inc, Boehringer Ingelheim, Genentech, and OSI Pharmaceuticals; and is on scientific advisory boards for Biothera, DiaTech Oncology, Genetics Squared, MedTrust, N-of-One, SynDevRx, and Targeted Molecular Diagnostics. The associates of Medical Learning Institute Inc, the accredited provider for this activity, Core Principle Solutions, LLC, and Center of Excellence Media, LLC, do not have any financial relationships or relationships to products or devices with any commercial interest

Volume 1 • No 5

1

IV

Disclaimer The information provided in this CME/CPE/CE activity is for continuing education purposes only and is not meant to substitute for the independent medical judgment of a healthcare provider relative to diagnostic and treatment options of a specific patient’s medical condition. Recommendations for the use of particular therapeutic agents are based on the best available scientific evidence and current clinical guidelines. No bias toward or promotion for any agent discussed in this program should be inferred.

There is no fee for this activity. To receive credit after reading this CME/CPE/CE activity in its entirety, participants must complete the pretest, posttest, and evaluation. The pretest, posttest, and evaluation can be completed online at www.mlicme.org/P12038E.html. Upon completion of the evaluation and scoring 70% or better on the posttest, you will immediately receive your certificate online. If you do not achieve a score of 70% or better on the posttest, you will be asked to take it again. Please retain a copy of the Certificate for your records. For questions regarding the accreditation of this activity, please contact Medical Learning Institute Inc at 609-333-1693 or cgusack@mlicme.org. Estimated time to complete this activity: 1.25 hours Date of initial release: November 13, 2012 Valid for CME/CPE/CE credit through: November 13, 2013

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Continuing Medical Education

Figure 2. Drug Development Timeline =#+#$"0>!

?#@#1'4A#(%!

!"#$%&'()$(*)%#+%&(,) )'-)*".,)+./+%$(0#!

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567)8"+!

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p(TS) indicates probability of technical success of that phase; WIP, work in progress, ie, the number of projects (targets) pursued. ) ) ) $ $ $ $ ! " $$$%$&'()*$+,$-)(.)/0012$+3/3$45/$,678/)$(9$-)(:/;40$<4=)./40>$-6)06/?$ Reprinted by permission from Macmillan Publishers Ltd: Paul SM, Mytelka DS, Dunwiddie CT, et al. How the pharmaceutical ) )to improve ) R&D productivity: ) •" $ $ $ $ $ $ $ $ ! industry’s grand challenge. Nat Rev Drug Discov. 2010;9:203-214. Copyright 2010.

Evolution of Chemotherapy Modern chemotherapy was born in 1942 at Yale University, when the first oncology patient received treatment with nitrogen mustard.5 A timeline showing other key developments in the war against cancer is presented in Figure 3.6 Lung cancer chemotherapy reached the modern age in the mid 1990s, when a number of promising new agents, including the taxanes, gemcitabine, and vinorelbine, became available for the treatment of metastatic NSCLC. However, a study by Schiller and colleagues in 2002 compared the survival rates achieved by 4 chemotherapy regimens (cisplatin plus paclitaxel, cisplatin plus gemcitabine, cisplatin plus docetaxel, or carboplatin plus paclitaxel) in the treatment of advanced NSCLC and found that none of the 4 chemotherapy regimens offered a significant advantage over the others (Figure 4).7 These results indicated that a ceiling had been reached in efficacy with these chemotherapy regimens, and a paradigm shift was needed.

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Targeting the Tyrosine Kinase Inhibitors Because of this need for novel therapeutic approaches, research began using small-molecule tyrosine kinase inhibitors to target lung cancer. In 1997, the first orally administered epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors – gefitinib and erlotinib – entered clinical studies. In 2002, phase 1 results from a study with gefitinib showed antitumor activity at all doses in both chemotherapy-naive and heavily pretreated patients.8 Gefitinib was granted accelerated approval by the FDA in May 2003 for the treatment of patients with NSCLC who were refractory to established cancer treatments (ie, both a platinum drug and docetaxel) on the basis of a surrogate end point, tumor response rate, for clinical efficacy. The response rate in patients taking the drug was approximately 10%.9 In November 2004, the FDA approved erlotinib for the treatment of patients with locally advanced or metastatic NSCLC after failure of at least 1 prior chemotherapy regimen. Unlike gefitinib, erlotinib was approved based on improved overall survival.10

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Figure 3. Timeline Showing the History of Chemotherapy Louis Goodman and Alfred Gilman use nitrogen mustard to treat a patient with non-Hodgkin’s lymphoma and demonstrate for the first time that chemotherapy can induce tumor regression.

1942

1948

Sidney Farber uses antifolates to successfully induce remissions in children with acute lymphoblastic leukemia (ALL).

The National Chemotherapy Program begins at the National Cancer Institute (NCI); a systematic program for drug screening commences.

1955

1958

Roy Hertz and Min Chiu Li demonstrate that methotrexate as a single agent can cure choriocarcinoma, the first solid tumor to be cured by chemotherapy.

The Food and Drug Administration (FDA) approves the alkylating agent cyclophosphamide.

1959

1965

Vincent DeVita and colleagues cure lymphomas with combination chemotherapy.

1970

Combination chemotherapy (POMP regimen) is able to induce long-term remissions in children with ALL.

1972

A combination of cyclophosphamide, methotrexate, and fluorouracil (CMF) was shown to be effective as adjuvant treatment for node-positive breast cancer.

1975

Emil Frei and colleagues demonstrate that chemotherapy given after surgical removal of osteosarcoma can improve cure rates (adjuvant chemotherapy).

The NCI introduces “disease oriented” screening using 60 cell lines derived from different types of human tumor.

1978

The FDA approves cisplatin for the treatment of ovarian cancer, a drug that would prove to have activity across a broad range of solid tumors.

George Hitchings and Gertude Elion synthesize the purine analogue 6-mercaptopurine.

1989

Studies by Brian Druker lead to FDA approval of imatinib mesylate (Gleevec) for chronic myelogenous leukemia, a new paradigm for targeted therapy in oncology.

1992

The FDA approves paclitaxel (Taxol), which becomes the first “blockbuster” oncology drug.

2001

The FDA approves bevacizumab (Avastin), the first clinically proven antiangiogenic agent, for the treatment of colon cancer.

2004

Researchers at Harvard University define mutations in the epidermal growth factor receptor that confer selective responsiveness to the targeted agent gefitinib, indicating that molecular testing might be able to prospectively identify subsets of patients that will respond to targeted agents.

Reprinted by permission from Macmillan Publishers Ltd: Chabner BA, Roberts TG Jr. Timeline: chemotherapy and the war on cancer. Nat Rev Cancer. 2005;5:65-72. Copyright 2005.

Studies found that the EGFR gene is mutated in many NSCLCs, and that these mutations are associated with increased sensitivity to gefitinib or erlotinib. In addition, EGFR gene mutations were found to be more common among females, patients from Japan, never smokers, and patients with adenocarcinomas, which are the same groups that have the highest response rates to tyrosine kinase inhibitors.11-13 In 2005, a study by Shigematsu and colleagues found that mutations in either of 2 genes (EGFR or KRAS) are involved in the development of lung cancer.14 They found that, in lung cancer patients, mutations in the tyrosine kinase domain of the EGFR gene were more common in never smokers than in smokers or nonsmokers

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(51% vs 10%), adenocarcinomas versus other types of lung cancer (40% vs 3%), patients of East Asian ancestry versus other ethnicities (30% vs 8%), and females

In 1997, the first orally administered EGFR tyrosine kinase inhibitors entered clinical studies. versus males (42% vs 14%). Mutation status was not associated with age at diagnosis, clinical stage, the presence of certain histologic features, or overall survival, and mutations were not found in any normal tissue or tissue from other cancer types. EGFR tyrosine kinase

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Figure 4. Overall Survival by Treatment Group 1.0 0.8

Cisplatin/Paclitaxel Cisplatin/Gemcitabine Cisplatin/Docetaxel Carboplatin/Paclitaxel

0.6 0.4 0.2 0 0

5

10

15 Months

20

25

30

From Schiller JH, Harrington D, Belani CP, et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med. 2002;346:92-98. Copyright Š 2002 Massachusetts Medical Society. Reprinted with permission from Massachusetts Medical Society.

domain mutations are the first known mutations to occur in never smokers. In addition, they found mutations in the KRAS gene, an EGFR signaling pathway gene, in 8% of lung cancers but not in any that had an EGFR gene mutation.

EGFR tyrosine kinase domain mutations are the first known mutations to occur in never smokers. Based on these and other data, in 2011, ASCO issued a provisional clinical opinion recommending EGFR mutation testing for patients with advanced NSCLC.15 Also in 2011, the National Comprehensive Cancer Network (NCCN) similarly called for EGFR testing of NSCLC patients with tumors of all histologies except squamous cell carcinoma.16 Targeting Anaplastic Lymphoma Kinase Inhibitors The benefit of testing for mutations of the anaplastic lymphoma kinase (ALK) gene, such as the EML4-ALK fusion, was demonstrated in a phase 1 study17 and a phase 2 study18 of the ALK inhibitor crizotinib. In these studies,

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patients with the EML4-ALK fusion, nearly all of whom had progressed despite at least 1 prior line of therapy, showed response rates of 50% to 60% with crizotinib.17,18 Based on the results of these 2 studies, in August 2011, the FDA granted accelerated approval to crizotinib for the treatment of patients with locally advanced or metastatic NSCLC that is ALK-positive as detected by a concurrently FDA-approved diagnostic test. In addition, based on a retrospective, nonrandomized analysis comparing overall survival of patients enrolled in the 2 trials with historical controls to estimate the clinical benefit of crizotinib therapy,19 the NCCN recommends testing for ALK rearrangement in patients with metastatic NSCLC adenocarcinoma, and treatment with the ALK inhibitor crizotinib is recommended for ALKpositive patients.16 Multiple Pathways of Lung Cancer Pathogenesis Lung cancer is a heterogeneous disease. Because lung cancer tumors differ from one another pathologically and molecularly, personalized lung cancer therapy is critical in the battle against this disease. Multiple pathways of lung cancer pathogenesis have been uncovered, much due to the work done in the Tumor Sequencing Project (TSP). The TSP team sequenced 623 genes that were known or suspected to contribute to cancer formation in 188 lung cancer patients and matched controls.20 By combining mutation information with copy number and expression data for 41 lung adenocarcinomas, they were also able to determine whether specific mutations affected gene activity and/or copy number. The researchers detected 1013 nonsynonymous somatic mutations in 163 of these lung tumors. Most (>900) were point mutations, although insertions, deletions, and dinucleotide mutations were also detected. Overall, they found 26 genes that were most often mutated in lung adenocarcinoma (Figure 5). Among them were some genes that had not previously been tied to lung cancer but which have been linked to other types of cancer. These findings shed further light on several important signaling pathways involved in lung adenocarcinoma and suggest new molecular targets for treatment.

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Figure 5. Mutation Analysis Shows That Multiple Mutations Along Multiple Pathways Drive the Pathogenesis of Lung Cancer 70

60

Significant on the basis of 3 methods Significant on the basis of 2 methods Significant on the basis of 1 method

Number of Mutations

50

40

30

20

10

SLC38A3

NRAS

ZMYND10

PAK3

INHBA

LTK

GNAS

PDGFRA

EPHA5

NTRK3

RB1

NTRK1

FGFR4

KDR

ERBB4

CDKN2A

PTPRD

EPHA3

APC

ATM

NF1

LRP1B

EGFR

STK11

KRAS

TP53

0

Reprinted by permission from Macmillan Publishers Ltd: Ding L, Getz G, Wheeler DA, et al. Somatic mutations affect key pathways in lung adenocarcinoma. Nature. 2008;455:1069-1075. Copyright 2008.

Latest Clinical Data on Molecular Biomarkers and Their Impact on the Management of Patients With Solid Tumors Biomarkers in Colorectal Cancer Leonard B. Saltz, MD, from the Memorial SloanKettering Cancer Center in New York, New York, presented data along with his personal opinions about the usefulness of biomarkers in the management of colorectal cancer. He began by stating, “most biomarkers that are currently available for patients with colorectal cancer do not provide actionable information and therefore should not be used in routine practice.” One clinical or surrogate “biomarker” that Saltz said is useful in predicting survival in patients receiving the

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EGFR-targeted monoclonal antibodies cetuximab and panitumumab is the presence of a skin rash (Figure 6). In a number of studies, the presence of an acne-like skin rash, predominantly on the face and upper torso, correlates with survival in patients treated with cetuximab and may serve as a clinical biomarker to identify patients likely to respond to cetuximab therapy (Figure 7).21-25 Said Saltz, “Absence of skin rash with cetuximab or panitumumab at 4 weeks strongly suggests lack of activity of the anti-EGFR agent, and the clinician should consider cessation of the agent.” The KRAS mutation, which may be present in 35% to 45% of patients with colorectal cancer, has emerged as a predictive marker of resistance to panitumumab or cetuximab treatment.26-29 For example, in a study by

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Figure 6. Cetuximab-Associated Skin Rash

Figure 7. Correlation of Severity of Skin Rash With Survival of Cetuximab-Treated Patients21

Median Survival (months)

10

9.5

9 8 6.4

7 6 5 4 3 2

1.9

1 0

Grade 0

Grade 1 or 2

Grade 3

Severity of Skin Rash Saltz LB, Meropol NJ, Loehrer PJ Sr, et al. Phase II trial of cetuximab in patients with refractory colorectal cancer that expresses the epidermal growth factor receptor. J Clin Oncol. 2004;22:1201-1208. Reprinted with permission. © 2004 American Society of Clinical Oncology. All rights reserved.

Amado and colleagues, a strong correlation was demonstrated between the KRAS mutation and response to panitumumab (Figure 8).27 In a study by Bokemeyer and colleagues, a strong correlation was demonstrated between the KRAS mutation and response to cetuximab (Figure 9).29 These results

32

show compelling evidence that KRAS mutation is a biomarker that predicts lack of response to both panitumumab and cetuximab; therefore, KRAS genotyping has been incorporated into clinical practice.26 In addition, among colorectal tumors carrying wildtype KRAS, mutation of BRAF or PIK3CA oncogenes or loss of PTEN tumor suppressor gene expression may be associated with resistance to EGFR-targeted monoclonal antibody treatment.26 BRAF mutations are responsible for an additional 12% to 15% of patients who fail to respond to anti-EGFR treatment. Because the Ras-Raf-MAPK pathway lies just downstream of EGFR, a mutation in KRAS could render cells independent of upstream EGFR activation or inhibition of the receptor through anti-EGFR therapies. Recent studies now show a strong correlation of KRAS and BRAF mutations with response to panitumumab and cetuximab. These studies show compelling evidence that KRAS and BRAF mutations are biomarkers of nonresponse to either of these drugs in patients with metastatic colorectal cancer. This finding suggests that genotyping for the BRAF V600E mutation complements KRAS mutation analysis and may be as important as KRAS testing for treatment decisions.30

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Biomarkers in Prostate Cancer Oliver Sartor, MD, from the Tulane Cancer Center and Tulane Medical School in New Orleans, Louisiana, explained that “the brave new era of biomarker-driven therapeutic decision making has yet to arrive for prostate cancer, as clinically useful biomarkers other than prostate-specific antigen (PSA) have been slow to develop in this common malignancy.” PSA screening has led to a significant rise in the number of men diagnosed with prostate cancer and an associated increase in biopsies performed. Despite its limitations, including a positive predictive value of only 25% to 40%, PSA remains the only generally accepted biomarker for prostate cancer.31 In recent years, studies have shown that a change in circulating tumor cell (CTC) count could indicate whether a therapy for metastatic breast,32-34 colorectal,35

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Figure 8. Increased Progression-Free Survival Observed With Panitumumab in Patients With (A) KRAS Mutant Tumors Versus Those With (B) KRAS Wild-Type Tumors

BSC indicates best supportive care; HR, hazard ratio; Panit., panitumumab. Amado RG, Wolf M, Peeters M, et al. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J Clin Oncol. 2008;26:1626-1634. Reprinted with permission. Š 2008 American Society of Clinical Oncology. All rights reserved.

or prostate cancer36,37 is effective.38-40 A semiautomated system, the CellSearch Circulating Tumor Cell Kit, has been developed using an ep-

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ithelial cell adhesion molecule (EpCAM) antibodybased immunomagnetic capture and automated staining methodology for the enumeration of CTCs of

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Progression-Free Survival (proportion)

Progression-Free Survival (proportion)

Figure 9. Increased Progression-Free Survival Observed in Patients Receiving Cetuximab With KRAS Wild-Type Tumors Versus Those With KRAS Mutant Tumors

Time (months)

Time (months)

Cens. indicates censored; Cet., cetuximab; FOLFOX-4, oxaliplatin, leucovorin, and fluorouracil; HR, hazard ratio; mo., months; pts., patients; Progr., progression. Bokemeyer C, Bondarenko I, Makhson A, et al. Fluorouracil, leucovorin, and oxaliplatin with and without cetuximab in the first-line treatment of metastatic colorectal cancer. J Clin Oncol. 2009;27:663-671. Reprinted with permission. © 2009 American Society of Clinical Oncology. All rights reserved.

epithelial origin (CD45–, EpCAM+, and cytokeratins 8, 18+, and/or 19+) in whole blood.41 The system and reagents have been approved by the FDA for predicting progression-free and overall survival in patients with metastatic breast, colorectal, or prostate cancer. In a pivotal trial, the detection of >5 CTCs per 7.5 mL of blood at the start of chemotherapy and after each cycle of therapy was associated with shorter progression-free

The molecular subtypes display highly significant differences in prediction of overall survival as well as relapse-free survival. and overall survival in patients with metastatic breast cancer. CTC counts were more predictive of the outcomes than were standard clinical parameters.42,43 For prostate cancer, preliminary analysis of the correlation of CTC counts with mRNAs for PSA or prostatespecific membrane antigen and available clinical predictors have been encouraging.41,44,45 However, since published literature has yet to demonstrate that the use of CTC measurements improves quality of life or in-

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creases survival, ASCO does not recommend use of CTC measurements for diagnostic or treatment decision making.34 Sartor concluded his discussion of CTCs with this remark, “CTCs are FDA approved but not yet demonstrably useful.” Biomarkers in Breast Cancer Lisa A. Carey, MD, from the Lineberger Comprehensive Cancer Center at the University of North Carolina at Chapel Hill, North Carolina, presented a discussion of the molecular classification and profiling of breast cancer. Breast cancer is a heterogeneous disease; the recent identification of molecular subtypes of breast cancer has led to a paradigm shift in the way we think about breast cancer and may increase our ability to predict response to current and novel therapies and ultimately improve outcomes for breast cancer patients (Figure 10).46 In the past decade, genomic studies have identified several breast cancer intrinsic subtypes (luminal A, luminal B, HER2-enriched, claudin-low, basal-like) and a normal breast-like group.47-52 The molecular subtypes display highly significant differences in prediction of overall survival, as well as re-

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Figure 10. Molecular Classification of Breast Cancer46

ER–, Claudin-3/4/7low, vimentin+, E-cadherinlow, Zeb1+

Breast Cancer

Claudin-low (12%-14%)

ER–, PR–, HER2–, K5/14+, EGFR+

Luminal B (~20%)

Basal-like (15%-20%)

ERlow, HER2low, proliferationhigh

ERhigh, HER2low

Luminal A (~40%) HER2-enriched (10%-15%)

Normal Breast Like Adipose tissue gene signature+

HER2+ ER–

Overall Survival

Relapse-Free Survival

Figure 11. Differences in Prognosis Among the Various Molecular Subtypes of Breast Cancer

Basal-like Claudin-low HER2-enriched Luminal A Luminal B

p=7.67e-06

p=4.67e-06

Months

Months

Reprinted from Prat A, Perou CM. Deconstructing the molecular portraits of breast cancer. Mol Oncol. 2011;5:5-23. Copyright 2011, with permission from Elsevier.

lapse-free survival, with the luminal A subtype having the longest survival (Figure 11).47 Harrell and colleagues recently found that, in addition to differences in survival among the various subtypes of breast cancer, differences occur in the overall risk of relapse, the timing of relapse, and the organs to which the tumors metastasize.53 For example, basal-like and claudin-low breast cancers both exhibit a high probabil-

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ity to metastasize to the brain and lung, while HER2-enriched subtype tumors preferentially colonize the liver.53 Overall, the authors concluded that, depending on the organ of relapse, a combination of gene expression signatures most accurately predicts metastatic behavior. Using gene expression profiling, van ’t Veer and colleagues at The Netherlands Cancer Institute developed a 70-gene signature (MammaPrint) that accurately dis-

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Table 1. Kaplan-Meier Estimates of the Rate of Distant Recurrence at 10 Years, According to Recurrence Score Risk Categories Among Node-Negative, Tamoxifen-Treated Breast Cancer Patients*

consortium.56 Their analyses confirmed that the 70-gene signature is a strong prognostic factor for time to distant metastases and overall survival in untreated patients with node-negative breast cancer, with unadjusted HRs of 2.32 (95% CI, Rate of Distant 1.35-4.00) and 2.79 (95% CI, 1.60-4.87), respecRisk Category Percentage of Patients Recurrence at 10 Years tively. In addition, when adjusted for the clinical Low 51% 6.8% risk groups based on 10-year survival probability Intermediate 22% 14.3% as calculated by the Adjuvant! Online software, High 27% 30.5% the gene signature HRs were 2.13 (95% CI, 1.19*A low risk was defined as a recurrence score of <18, an intermediate risk as a score of 18-<31, and a high risk as a score of ≥31. 3.82) for time to distant metastases, 2.63 (95% From Paik S, Shak S, Tang G, et al. A multigene assay to predict recurrence of tamoxifen-treated, nodeCI, 1.45-4.79) for overall survival, and 1.36 negative breast cancer. N Engl J Med. 2004;351:2817-2826. Copyright © 2004 Massachusetts Medical (95% CI, 0.91-2.03) for disease-free survival. Society. Reprinted with permission from Massachusetts Medical Society. These results indicate that the gene signature adds independent prognostic information to that provided by a risk assessment based solely on clinicotinguished breast cancer patients who were likely to repathologic factors. main free of distant metastases (good profile) from breast MammaPrint is being evaluated in a clinical trial cancer patients at high risk of developing distant metas54 known as MINDACT (Microarray In Node-negative and tases (poor profile). The first validation of the 70-gene 1-3 node-positive Disease may Avoid ChemoTherapy), profile was performed by van de Vijver and colleagues which is a randomized European study comparing on a consecutive series of 295 breast cancer tumors; 144 MammaPrint with clinical assessment.57 MINDACT has tumors from lymph node–positive and 151 tumors from lymph node–negative breast cancer patients.55 Among enrolled over 6000 patients, who have been classified into high or low genomic risk by MammaPrint and clinicothe 295 patients, 180 had a poor-prognosis signature and pathologic risk through Adjuvant! Online. Patients with 115 had a good-prognosis signature, and the mean overboth genomic and clinical high risks are offered adjuvant all 10-year survival rates were 55% and 95%, respecchemotherapy; those with both genomic and clinical low tively. At 10 years, the probability of remaining free of risks do not receive chemotherapy; patients with discordant risk are randomized for the decision of adjuvant The researchers developing Oncotype DX chemotherapy based on genomic or clinical risk.57 MINtook a different approach from that used DACT is due to complete data collection in 2019. by the developers of MammaPrint. The researchers developing the Oncotype DX assay took a different approach from that used by the developers of MammaPrint. Carey explained, “They started distant metastases was 51% in the group with a poorwith 250 candidate genes and then they tailored it down prognosis signature and 85% in the group with a goodto 16. Once they found the best genes, they then valiprognosis signature. The estimated hazard ratio (HR) dated it prospectively.” Paik and colleagues at the Nafor distant metastases in the group with a poor-prognosis tional Surgical Adjuvant Breast and Bowel Project signature, compared with the group with the good-prog(NSABP) tested whether the results of a reverse-trannosis signature, was 5.1 (95% CI, 2.9-9.0; P<.001). scriptase polymerase chain reaction assay of 21 prospecThe 70-gene MammaPrint signature was later valitively selected genes in paraffin-embedded tumor tissue dated by an independent multinational collaborative would correlate with the likelihood of distant recurrence team conducted under the aegis of the TRANSBIG

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Figure 12. Kaplan-Meier Plots for Distant Recurrence Comparing Treatment With Tamoxifen (Tam) Alone Versus Treatment With Tamoxifen Plus Chemotherapy (Tam + chemo)

A, all patients; B, low risk (Recurrence Score [RS] <18); C, intermediate risk (RS 18-30); D, high risk (RS ≥31). Paik S, Tang G, Shak S, et al. Gene expression and benefit of chemotherapy in women with node-negative, estrogen receptor–positive breast cancer. J Clin Oncol. 2006;24:37263734. Reprinted with permission. © 2006 American Society of Clinical Oncology. All rights reserved.

in patients with node-negative, tamoxifen-treated breast cancer who were enrolled in the NSABP study B-14.58 The levels of expression of 16 cancer-related genes and 5 reference genes were used in a prospectively defined algorithm to calculate a “Recurrence Score” (RS) and to determine a risk group (low, intermediate, or high) for each patient (Table 1). Low risk was defined as an RS <18, intermediate risk as a score of ≥18 but <31, and high risk as a score of ≥31. There were 28 recurrences

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in the low-risk group, 25 in the intermediate-risk group, and 56 in the high-risk group. The difference among the groups is significant (P<.001). In addition to quantifying breast cancer recurrence risk, the Oncotype DX assay also assesses the benefit from chemotherapy. Node-Negative, ER-Positive Breast Cancer The data from which the assay was developed were

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Table 2. Timeline of Pivotal Events in the Cancer Field and Relative Survival Rates for Patients With Cancer in the United States* Year 1863 1889 1914 1937 1944 1950 1953 1961 1970 1971 1975 1976 1979 1981 1984 1986 1990 1991 1994 2000 2002

Relative Discovery or Event Survival Rate Cellular origin of cancer (Virchow) Seed-and-soil hypothesis (Paget) Chromosomal mutations in cancer (Boveri) Founding of NCI Transmission of cellular information by DNA (Avery) Availability of cancer drugs through Cancer Chemotherapy National Service Center Report on structure of DNA 35% Breaking of the genetic code Reverse transcriptase Restriction enzymes Passage of National Cancer Act Hybridomas and monoclonal antibodies 50% Tracking of cancer statistics by SEER program Cellular origin of retroviral oncogenes Epidermal growth factor and receptor Suppression of tumor growth by p53 G proteins and cell signaling Retinoblastoma gene First decrease in cancer incidence and mortality Association between mutation in APC gene and colorectal cancer Genetic cancer syndromes Association between BRCA1 and breast cancer Sequencing of the human genome Epigenetics in cancer MicroRNAs in cancer First decrease in total number of deaths 68% from cancer Tumor stromal interaction

hormonal therapy (ie, tamoxifen) with hormonal therapy alone in 651 women with lymph node– negative, estrogen receptor (ER)-positive breast cancer (Figure 12).59 Node-Positive, ER-Positive, Postmenopausal Breast Cancer For lymph node–positive, ER-positive postmenopausal patients treated with tamoxifen, the Oncotype DX report form now includes data retrospectively analyzed from the prospective randomized Southwest Oncology Group (SWOG) 8814 study, which evaluated the risk of recurrence or death versus the RS result (both prognosis and likelihood of chemotherapy benefit). In the SWOG 8814 study, 1477 women were randomized to receive either tamoxifen alone for 5 years (n=361), or 6 cycles of chemotherapy with cyclophosphamide, doxorubicin, and fluorouracil (CAF) with concurrent tamoxifen (n=550), or 6 cycles of CAF followed by tamoxifen (CAF-T).60 In women in the low-risk or intermediate-risk groups, CAF-T offered no significant advantage over the 10-year diseasefree or overall survival rates seen among those who received tamoxifen alone. In contrast, among the women in the high-risk group, the 10year disease-free and overall survival rates were significantly greater with CAF-T than with tamoxifen alone.

Prospective, Randomized Trials Under Way While the Oncotype DX is currently based upon retrospective data from the aforementioned 2006 2 prospective randomized clinical trials, prospec*Data are from the National Cancer Institute Surveillance, Epidemiology, and End Results program. tive studies are ongoing. One prospective study, From DeVita VT Jr, Rosenberg SA. Two hundred years of cancer research. N Engl J Med. 2012;366:22072214. Copyright © 2012 Massachusetts Medical Society. Reprinted with permission from Massachusetts known as TAILORx (Trial Assigning IndividualMedical Society. ized Options for Treatment [Rx]) is examining retrospectively analyzed from a prospective randomized whether chemotherapy is required for the intermediatetrial, the NSABP study B-20, which compared the comrisk group defined by the RS.61 Another prospective ranbination of chemotherapy (ie, 6 cycles of cyclophosdomized trial, known as RxPONDER (Rx for Positive Node, Endocrine Responsive Breast Cancer study, or phamide, methotrexate, and 5-fluorouracil [CMF]) plus

2005

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SWOG S1007), opened in January 2011 and will assess whether chemotherapy benefits patients with node-positive breast cancer who have a low to intermediate RS. The trial will also examine whether there is an optimal RS cutoff point for these patients, above which chemotherapy should be recommended. This study includes women with RS ≤25 who have early-stage, hormone receptor–positive, HER2-negative breast cancer that has been found to involve 1 to 3 lymph nodes. Carey concluded her presentation by saying that genomic signatures have augmented clinical decision making in hormone receptor–positive/HER2-negative breast cancer. An emerging body of evidence indicates that genomic signatures can be used to tailor (and reduce) chemotherapy use in early breast cancer. However, there are no signatures in ER-negative or HER2-positive breast cancer yet.

Summary and Future Directions In June 2012, the 200th anniversary issue of the New England Journal of Medicine featured an article by DeVita and Rosenberg that reviewed the history of cancer research and how these events affected patient outcomes (Table 2).62 Increased understanding of tumor heterogeneity, as well as technical advances such as the identification of markers, mutations, and genomic signatures, will continue to improve clinical outcomes in patients with cancer. Predictive markers identify groups of patients who are likely to have increased sensitivity or resistance to a given therapy; for example, recent findings in lung cancer demonstrate that tumor-related molecular markers, such as EGFR mutations or mutations of the EML4ALK fusion gene, can be used to define subsets of patients who will benefit from particular treatments. In colorectal cancer, one clinical or surrogate “biomarker” that is useful in predicting survival in patients receiving the EGFR-targeted monoclonal antibodies cetuximab and panitumumab is the presence of a skin rash. Tumor KRAS mutations have emerged as a predictive marker of resistance to these same treatments. In prostate cancer, clinically useful biomarkers other than PSA have

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been slow to develop. In breast cancer, genomic signatures have augmented clinical decision making in patients with hormone receptor–positive/HER2-negative tumors. u

References 1. American Cancer Society. Cancer Facts & Figures 2012. www.cancer. org/acs/groups/content/@epidemiologysurveilance/documents/document/a cspc-031941.pdf. Accessed September 19, 2012. 2. American Cancer Society. Non-small cell lung cancer survival rates by stage. www.cancer.org/Cancer/LungCancer-Non-SmallCell/DetailedGuide /non-small-cell-lung-cancer-survival-rates. Accessed September 20, 2012. 3. Paul SM, Mytelka DS, Dunwiddie CT, et al. How to improve R&D productivity: the pharmaceutical industry’s grand challenge. Nat Rev Drug Discov. 2010;9:203-214. 4. Tessier-Lavigne M. Newsmaker interview. Genentech scientist to take the helm at Rockefeller University. Interview by Greg Miller. Science. 2010;329:1456. 5. Christakis P. The birth of chemotherapy at Yale. Bicentennial lecture series: Surgery Grand Round. Yale J Biol Med. 2011;84:169-172. 6. Chabner BA, Roberts TG Jr. Timeline: chemotherapy and the war on cancer. Nat Rev Cancer. 2005;5:65-72. 7. Schiller JH, Harrington D, Belani CP, et al. Comparison of four chemotherapy regimens for advanced non-small-cell lung cancer. N Engl J Med. 2002;346:92-98. 8. Herbst RS, Maddox AM, Rothenberg ML, et al. Selective oral epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 is generally welltolerated and has activity in non-small-cell lung cancer and other solid tumors: results of a phase I trial. J Clin Oncol. 2002;20:3815-3825. 9. National Cancer Institute. Cancer Drug Information: FDA Approval for Gefitinib. www.cancer.gov/cancertopics/druginfo/fda-gefitinib. Accessed September 20, 2012. 10. National Cancer Institute. Cancer Drug Information: FDA Approval for Erlotinib Hydrochloride. www.cancer.gov/cancertopics/druginfo/fdaerlotinib-hydrochloride. Accessed September 20, 2012. 11. Lynch TJ, Bell DW, Sordella R, et al. Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med. 2004;350:2129-2139. 12. Paez JG, Jänne PA, Lee JC, et al. EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science. 2004;304: 1497-1500. 13. Pao W, Miller V, Zakowski M, et al. EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A. 2004;101:13306-13311. 14. Shigematsu H, Lin L, Takahashi T, et al. Clinical and biological features associated with epidermal growth factor receptor gene mutations in lung cancers. J Natl Cancer Inst. 2005;97:339-346. 15. Keedy VL, Temin S, Somerfield MR, et al. American Society of Clinical Oncology provisional clinical opinion: epidermal growth factor receptor (EGFR) mutation testing for patients with advanced non-small-cell lung cancer considering first-line EGFR tyrosine kinase inhibitor therapy. J Clin Oncol. 2011;29:2121-2127. 16. National Comprehensive Cancer Network (NCCN). NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines). Non-Small Cell Lung Cancer. Version 3.2012. www.nccn.org/professionals/physician_gls/pdf/nscl. pdf. Accessed September 20, 2012. 17. Kwak EL, Bang YJ, Camidge DR, et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med. 2010;363:1693-1703. 18. Crinò L, Kim D, Riely GJ, et al. Initial phase II results with crizotinib in advanced ALK-positive non-small cell lung cancer (NSCLC): PROFILE 1005. J Clin Oncol. 2011;29(suppl). Abstract 7514. 19. Shaw AT, Yeap BY, Solomon BJ, et al. Impact of crizotinib on survival in patients with advanced, ALK-positive NSCLC compared with historical controls. J Clin Oncol. 2011;29(suppl). Abstract 7507. 20. Ding L, Getz G, Wheeler DA, et al. Somatic mutations affect key pathways in lung adenocarcinoma. Nature. 2008;455:1069-1075. 21. Saltz LB, Meropol NJ, Loehrer PJ Sr, et al. Phase II trial of cetuximab

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in patients with refractory colorectal cancer that expresses the epidermal growth factor receptor. J Clin Oncol. 2004;22:1201-1208. 22. Raoul JL, Van Laethem JL, Peeters M, et al. Cetuximab in combination with irinotecan/5-fluorouracil/folinic acid (FOLFIRI) in the initial treatment of metastatic colorectal cancer: a multicentre two-part phase I/II study. BMC Cancer. 2009;9:112. 23. Tol J, Koopman M, Cats A, et al. Chemotherapy, bevacizumab, and cetuximab in metastatic colorectal cancer. N Engl J Med. 2009;360:563-572. 24. Su X, Lacouture ME, Jia Y, et al. Risk of high-grade skin rash in cancer patients treated with cetuximab – an antibody against epidermal growth factor receptor: systemic review and meta-analysis. Oncology. 2009;77:124-133. 25. Saridaki Z, Tzardi M, Papadaki C, et al. Impact of KRAS, BRAF, PIK3CA mutations, PTEN, AREG, EREG expression and skin rash in ≥ 2 line cetuximab-based therapy of colorectal cancer patients. PLoS One. 2011;6:e15980. 26. Siena S, Sartore-Bianchi A, Di Nicolantonio F, et al. Biomarkers predicting clinical outcome of epidermal growth factor receptor-targeted therapy in metastatic colorectal cancer. J Natl Cancer Inst. 2009;101: 1308-1324. 27. Amado RG, Wolf M, Peeters M, et al. Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer. J Clin Oncol. 2008;26:1626-1634. 28. Van Cutsem E, Lang I, Folprecht G, et al. Cetuximab plus FOLFIRI: final data from the CRYSTAL study on the association of KRAS and BRAF biomarker status with treatment outcome. J Clin Oncol. 2010; 28(suppl). Abstract 3570. 29. Bokemeyer C, Bondarenko I, Makhson A, et al. Fluorouracil, leucovorin, and oxaliplatin with and without cetuximab in the first-line treatment of metastatic colorectal cancer. J Clin Oncol. 2009;27:663-671. 30. Di Nicolantonio F, Martini M, Molinari F, et al. Wild-type BRAF is required for response to panitumumab or cetuximab in metastatic colorectal cancer. J Clin Oncol. 2008;26:5705-5712. 31. Wright JL, Lange PH. Newer potential biomarkers in prostate cancer. Rev Urol. 2007;9:207-213. 32. Gaforio JJ, Serrano MJ, Sanchez-Rovira P, et al. Detection of breast cancer cells in the peripheral blood is positively correlated with estrogen-receptor status and predicts for poor prognosis. Int J Cancer. 2003;107:984-990. 33. Dawood S, Cristofanilli M. Integrating circulating tumor cell assays into the management of breast cancer. Curr Treat Options Oncol. 2007;8:89-95. 34. Harris L, Fritsche H, Mennel R, et al. American Society of Clinical Oncology 2007 update of recommendations for the use of tumor markers in breast cancer. J Clin Oncol. 2007;25:5287-5312. 35. Cohen SJ, Alpaugh RK, Gross S, et al. Isolation and characterization of circulating tumor cells in patients with metastatic colorectal cancer. Clin Colorectal Cancer. 2006;6:125-132. 36. Olmos D, Arkenau HT, Ang JE, et al. Circulating tumour cell (CTC) counts as intermediate end points in castration-resistant prostate cancer (CRPC): a single-centre experience. Ann Oncol. 2009;20:27-33. 37. Okegawa T, Nutahara K, Higashihara E. Prognostic significance of circulating tumor cells in patients with hormone refractory prostate cancer. J Urol. 2009;181:1091-1097. 38. Budd GT. Let me do more than count the ways: what circulating tumor cells can tell us about the biology of cancer. Mol Pharm. 2009;6:1307-1310. 39. Allard WJ, Matera J, Miller MC, et al. Tumor cells circulate in the peripheral blood of all major carcinomas but not in healthy subjects or patients with nonmalignant diseases. Clin Cancer Res. 2004;10:6897-6904. 40. Beerepoot LV, Mehra N, Vermaat JS, et al. Increased levels of viable circulating endothelial cells are an indicator of progressive disease in cancer patients. Ann Oncol. 2004;15:139-145.

41. CellSearch Circulating Tumor Cell Kit (Epithelial) [package insert]. Raritan, NJ: Veridex LLC; 2009. 42. Cristofanilli M, Budd GT, Ellis MJ, et al. Circulating tumor cells, disease progression, and survival in metastatic breast cancer. N Engl J Med. 2004;351:781-791. 43. Cristofanilli M, Hayes DF, Budd GT, et al. Circulating tumor cells: a novel prognostic factor for newly diagnosed metastatic breast cancer. J Clin Oncol. 2005;23:1420-1430. 44. Shaffer DR, Leversha MA, Danila DC, et al. Circulating tumor cell analysis in patients with progressive castration-resistant prostate cancer. Clin Cancer Res. 2007;13:2023-2029. 45. Chen BT, Loberg RD, Neeley CK, et al. Preliminary study of immunomagnetic quantification of circulating tumor cells in patients with advanced disease. Urology. 2005;65:616-621. 46. Malhotra GK, Zhao X, Band H, et al. Histological, molecular and functional subtypes of breast cancers. Cancer Biol Ther. 2010;10:955-960. 47. Prat A, Perou CM. Deconstructing the molecular portraits of breast cancer. Mol Oncol. 2011;5:5-23. 48. Perou CM, Sørlie T, Eisen MB, et al. Molecular portraits of human breast tumours. Nature. 2000;406:747-752. 49. Sørlie T, Perou CM, Tibshirani R, et al. Gene expression patterns of breast carcinomas distinguish tumor subclasses with clinical implications. Proc Natl Acad Sci U S A. 2001;98:10869-10874. 50. Sorlie T, Tibshirani R, Parker J, et al. Repeated observation of breast tumor subtypes in independent gene expression data sets. Proc Natl Acad Sci U S A. 2003;100:8418-8423. 51. Herschkowitz JI, Simin K, Weigman VJ, et al. Identification of conserved gene expression features between murine mammary carcinoma models and human breast tumors. Genome Biol. 2007;8:R76. 52. Prat A, Parker JS, Karginova O, et al. Phenotypic and molecular characterization of the claudin-low intrinsic subtype of breast cancer. Breast Cancer Res. 2010;12:R68. 53. Harrell JC, Prat A, Parker JS, et al. Genomic analysis identifies unique signatures predictive of brain, lung, and liver relapse. Breast Cancer Res Treat. 2012;132:523-535. 54. van ’t Veer LJ, Dai H, van de Vijver MJ, et al. Gene expression profiling predicts clinical outcome of breast cancer. Nature. 2002;415:530-536. 55. van de Vijver MJ, He YD, van ’t Veer LJ, et al. A gene-expression signature as a predictor of survival in breast cancer. N Engl J Med. 2002; 347:1999-2009. 56. Buyse M, Loi S, van ’t Veer L, et al. Validation and clinical utility of a 70-gene prognostic signature for women with node-negative breast cancer. J Natl Cancer Inst. 2006;98:1183-1192. 57. Rutgers E, Piccart-Gebhart MJ, Bogaerts J, et al. The EORTC 10041/BIG 03-04 MINDACT trial is feasible: results of the pilot phase. Eur J Cancer. 2011;47:2742-2749. 58. Paik S, Shak S, Tang G, et al. A multigene assay to predict recurrence of tamoxifen-treated, node-negative breast cancer. N Engl J Med. 2004;351:2817-2826. 59. Paik S, Tang G, Shak S, et al. Gene expression and benefit of chemotherapy in women with node-negative, estrogen receptor-positive breast cancer. J Clin Oncol. 2006;24:3726-3734. 60. Albain KS, Barlow WE, Shak S, et al. Prognostic and predictive value of the 21-gene recurrence score assay in postmenopausal women with nodepositive, oestrogen-receptor-positive breast cancer on chemotherapy: a retrospective analysis of a randomised trial. Lancet Oncol. 2010;11:55-65. 61. Sparano JA, Paik S. Development of the 21-gene assay and its application in clinical practice and clinical trials. J Clin Oncol. 2008;26:721-728. 62. DeVita VT Jr, Rosenberg SA. Two hundred years of cancer research. N Engl J Med. 2012;366:2207-2214.

THIRD ANNUAL CONFERENCE Influencing the Patient-Impact Factor

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The Role of Personalized Therapy in the Management of Multiple Myeloma: Case Study of a Patient With a Cytogenetic Abnormality At the 2012 conference of the Global Biomarkers Consortium, which took place March 9-11, 2012, in Orlando, Florida, Sagar Lonial, MD, from the Winship Cancer Institute and Emory University in Atlanta, Georgia, discussed the use of personalized therapy in the management of multiple myeloma.

C

ertain chromosomal abnoryour newly diagnosed MM patients, malities are associated with then the lab is not using a plasma cell prognosis in multiple myeloma enrichment technique, and it is not (MM). The translocations t(4;14) and giving you reliable data. t(14;16), or deletion del(13), are poor Prognosis for Patients prognostic factors in MM. Patients With t(4;14) with these abnormalities are considThe patient in our case was found by ered high risk. cIg-FISH to have t(4;14), which indiGenetic abnormalities are assessed cates a poor prognosis. This genetic aberboth by routine cytogenetic karyotyping and by fluorescence in situ hyration occurs in about 15% of MM bridization (FISH). FISH detects patients.1 Results from a 2005 study by Sagar Lonial, MD Jaksic and colleagues2 showed that pagenetic abnormalities on both dividing and nondividing cells, while conventional cytogenetics only detects abnormalities in dividing cells. Case While FISH is more sensitive than conventional • A 55-year-old woman presents with new-onset anemia karyotyping in detecting genetic aberrations, it is im(Hb 9.6 g/dL) portant to note that not all laboratories perform FISH • Skeletal survey is normal the same way. Detection of genetic abnormalities by • Chemistries are normal except for an elevated total protein FISH can be limited by the percentage of plasma cells (10.2 g/dL) in the specimen. If all the lab is doing is looking at 200 • Albumin is 3.9 g/dL; β2-microglobulin is 4.4 mg/L random cells under a microscope and doing FISH, you • Marrow shows 55% clonal plasma cells may receive false-negative FISH results in the case of low • Serum protein electrophoresis shows IgA kappa protein of monoclonal plasma cell tumor burden. A more reliable 3.6 g/dL FISH test is one in which the lab uses a plasma cell en• Free light chain ratio is abnormal (20:1) richment technique, such as cytoplasmic immunoglob• 24-hour urine protein electrophoresis shows 350 mg of ulin FISH (cIg-FISH), which uses light chain–specific kappa light chains immunofluorescence, or by using CD138 magnetic mi• Conventional cytogenetic results are normal crobeads to sort the plasma cells. • FISH performed at outside laboratory was negative for One way to do a quality control check on the lab cytogenetic abnormalities; however, FISH performed at that’s doing your FISH tests is to request an analysis for Emory is positive for t(4;14) del(13). This marker is present in about 50% of all newly diagnosed MM patients. If your lab does not return a result showing 50% expression of del(13) in all

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FISH indicates fluorescence in situ hybridization; Hb, hemoglobin.

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Figure 1. PFS and OS for Patients With t(4;14) Are Quite Poor

OS indicates overall survival; PFS, progression-free survival. Jaksic W, Trudel S, Chang H, et al. Clinical outcomes in t(4;14) multiple myeloma: a chemotherapy-sensitive disease characterized by rapid relapse and alkylating agent resistance. J Clin Oncol. 2005;23:7069-7073. Reprinted with permission. © 2005 American Society of Clinical Oncology. All rights reserved.

# #

# # ##

##

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Figure 2. Left Panel: OS of Patients With Versus Without t(4;14). Right Panel: OS of Patients with t(4;14) According to Hb and β2-Microglobulin Values at Diagnosis

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t(4;14) pos: 100 patients, t(4;14) neg: 616 patients; median 41.4 vs 65 months

Overall survival according to t(4;14) positivity

Overall survival of patients with t(4;14) according to hemoglobin and β2-microglobulin values at diagnosis

Hb indicates hemoglobin; OS, overall survival. Reprinted by permission from Macmillan Publishers Ltd: Moreau P, Attal M, Garban F, et al. Heterogeneity of t(4;14) in multiple myeloma. Long-term follow-up of 100 cases treated with tandem transplantation in IFM99 trials. Leukemia. 2007;21:2020-2024. Copyright 2007.

tients identified with t(4;14) by cIg-FISH who received induction followed by autologous stem cell transplantation (ASCT) had a median progression-free survival (PFS)

from the time of ASCT of only 14.1 months (Figure 1).2 This was significantly shorter than for t(4;14)-negative pa7# # # # 0 # # # F# # # #of 25.8 months # # tients, who had a median# PFS (P=.0003). 7# #

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Figure 3. EFS and OS in Patients With and Without t(4;14) Treated With BortezomibDexamethasone Induction Therapy

EFS indicates event-free survival; OS, overall survival. Avet-Loiseau H, Leleu X, Roussel M, et al. Bortezomib plus dexamethasone induction improves outcome of patients with t(4;14) myeloma but not outcome of patients with del(17p). J Clin Oncol. 2010;28:4630-4634. Reprinted with permission. © 2010 American Society of Clinical Oncology. All rights reserved.

The median overall survival (OS) for t(4;14)-positive patients from the time of ASCT was only 24.2 months.2 Results from a study by Moreau and colleagues in 2007 shows, however, that genetics alone does not tell the whole story. In this study, researchers identified a subgroup of t(4;14) patients with both low β2-microglobulin (<4 mg/L) and high hemoglobin (Hb; ≥10 g/dL) who experienced prolonged survival (median OS of 54.6 months and median PFS of 26 months) after tandem transplant and benefited from high-dose therapy (Figure 2).3

Novel Therapies in the Treatment of Patients With t(4;14) In the Intergroupe Francophone du Myélome 200501 trial, newly diagnosed MM patients with t(4;14) who received short-term induction with 4 cycles of bortezomib-dexamethasone before high-dose melphalan experienced significantly improved survival compared with those treated with vincristine, doxorubicin, and dexamethasone induction therapy (Figure 3).4 Cavo and colleagues from the GIMEMA Italian

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Myeloma Network compared thalidomide plus dexamethasone (TD) versus bortezomib plus TD (VTD) as induction therapy before, and consolidation therapy after, double ASCT in 480 patients with newly diagnosed MM.5 Results showed that while TD failed to overcome the poor prognosis related to the presence of t(4;14), VTD completely overcame the poor prognosis related to the presence of t(4;14).

Specific targeted maintenance holds the promise for better long-term disease control while still taking advantage of the combination effect when patients are initially diagnosed. In the area of personalized medicine for myeloma, it may be different from other solid tumors. In myeloma, with good induction therapy, most patients will respond, and thus the challenge remains how to keep them in a major response. Because combinations of agents are so successful for newly diagnosed patients, the real person-

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alization occurs in the maintenance setting, where we can use novel methods of keeping disease in control, such as stratified maintenance. This appears to be the future, as specific targeted maintenance holds the promise for better long-term disease control while still taking advantage of the combination effect when patients are initially diagnosed. u

References 1. Avet-Loiseau H, Attal M, Moreau P, et al. Genetic abnormalities and survival in multiple myeloma: the experience of the Intergroupe Franco-

phone du Myélome. Blood. 2007;109:3489-3495. 2. Jaksic W, Trudel S, Chang H, et al. Clinical outcomes in t(4;14) multiple myeloma: a chemotherapy-sensitive disease characterized by rapid relapse and alkylating agent resistance. J Clin Oncol. 2005;23:7069-7073. 3. Moreau P, Attal M, Garban F, et al. Heterogeneity of t(4;14) in multiple myeloma. Long-term follow-up of 100 cases treated with tandem transplantation in IFM99 trials. Leukemia. 2007;21:2020-2024. 4. Avet-Loiseau H, Leleu X, Roussel M, et al. Bortezomib plus dexamethasone induction improves outcome of patients with t(4;14) myeloma but not outcome of patients with del(17p). J Clin Oncol. 2010;28:4630-4634. 5. Cavo M, Tacchetti P, Patriarca F, et al. Bortezomib with thalidomide plus dexamethasone compared with thalidomide plus dexamethasone as induction therapy before, and consolidation therapy after, double autologous stem-cell transplantation in newly diagnosed multiple myeloma: a randomised phase 3 study. Lancet. 2010;376:2075-2085.

INTERVIEW WITH THE INNOVATORS An exclusive PMO series Personalized Medicine in Oncology™ is pleased to offer insightful interviews with leaders in oncology about their approach to personalized medicine. To watch our interviews, visit www.PersonalizedMedOnc.com/videolibrary

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The Cancer Immunotherapy Trials Network: A National Strategy for the Development and Implementation of Immunotherapy for the Treatment of Cancer Holbrook E. Kohrt, MD, PhD Stanford Cancer Institute, Stanford, California Howard L. Kaufman, MD Rush University Cancer Center, Chicago, Illinois Mary L. Disis, MD University of Washington, Seattle, Washington

Key Points • The clinical development of immunotherapy has lagged behind the theoretical and preclinical models, but the potential for durable therapeutic responses has been recognized for many years • The lack of widespread clinical expertise with immunotherapy presents a challenge for fully realizing the therapeutic opportunities of emerging immunotherapeutic strategies • The Cancer Immunotherapy Trials Network was established to address these concerns and promote the rapid development of new immunotherapy agents and combination therapy using an integrated national network

T

umor immunotherapy is a modality of cancer therapy that utilizes the immune system to recognize and eradicate cancer.1-5 The potential for tumor immunotherapy has been recognized for over a century after William Coley’s initial observation, “at the end of two weeks [since vaccination with erysipelas] the tumor in the neck had disappeared.”1 The work of Burnet and Thomas in the 1950s further established that the immune system was capable of immune surveillance and provided the foundation for understanding the nature of tumor rejection antigens. In the 1980s such rejection antigens were indeed identified in cancer cells,

most notably in melanoma. These discoveries paved the way for vaccine development and provided a basic foundation for understanding how the immune system can be used for therapeutic purposes in cancer. The clinical development of immunotherapy has lagged behind the theoretical and preclinical models, but the potential for durable therapeutic responses has been recognized for many years. The first major success was the use of allogeneic hematopoietic cell transplantation for leukemia, which was first performed in 1956.6 The use of nonspecific agents followed, including approval of Bacillus Calmette-Guérin for superficial blad-

Dr Kohrt is an Assistant Professor of Oncology at the Stanford Cancer Institute. His research focuses on models of tumor immunology, including vaccine therapy for patients undergoing bone marrow transplantation. Dr Kaufman is Director of the Rush University Cancer Center, Associate Dean of the Rush Medical College, and Professor of Surgery and Immunology & Microbiology at the Rush University Medical Center. His primary research interests are in melanoma and tumor immunotherapy. Dr Disis is Associate Member at the Fred Hutchinson Cancer Research Center, Professor in the Division of Medical Oncology, and Associate Dean of Translational Science at the University of Washington School of Medicine. She is involved in researching vaccines and immunotherapy for cancer.

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der cancer, the cytokine interferon-alpha for treatment Network (CITN) was established to address these conof hairy cell leukemia and adjuvant therapy of stage III cerns and promote the rapid development of new immelanoma, and interleukin-2 for treatment of metastatic munotherapy agents and combination therapy using an renal cell carcinoma and melanoma. integrated national network. Monoclonal antibodies targeting surSipuleucel-T and face molecules on tumor cells mediate antitumor activity, at least in part, Ipilimumab as Paradigms through immune mechanisms, and sevSipuleucel-T and ipilimumab higheral approved agents are current stanlight several important features of dard of care, most notably rituximab, modern tumor immunotherapy. Sipuwhich targets CD20 and is approved leucel-T is an antigen-specific vaccine for the treatment of patients with nonwith limited side effects, both attracHodgkin lymphoma,7 and trastuzumab, tive pharmacologic features, but it is which targets HER2/neu and is apassociated with limited clinical effiproved for the treatment of HER2cacy. In contrast, ipilimumab is not Howard L. Kaufman, MD expressing metastatic breast cancer.1 antigen specific and has significant The development of antigen-spetoxicity requiring close clinical monicific immunotherapy remained a more elusive goal, and toring, but it may be associated with significant clinical caution was warranted based on significant toxicity rebenefit. The characteristics of these agents will be briefly 2,8-12 ported with an anti-CD28 monoclonal antibody. discussed. Sipuleucel-T is composed of autologous peripheral Despite these challenges, the field has been re-energized with the approval of sipuleucel-T, an antigen-specific blood mononuclear cells, including dendritic cells, an vaccine for prostate cancer in 2010, and ipilimumab, immune-stimulating cytokine (granulocyte-macrophage an anticytotoxic T-lymphocyte antigen 4 (CTLA-4) colony-stimulating factor, GM-CSF), and prostatic acid monoclonal antibody for metastatic melanoma in phosphatase (PAP), a prostate-associated tumor anti2011.4,5 These agents, while first in class, have ushered in a new era of tumor immunotherapy and have highAgents from the interleukin family, such lighted the potential of such treatment in patients with IL-15 and IL-7, have high potential to advanced cancer. The unique toxicity profiles of these agents, the need for more appropriate clinical end points benefit cancer patients but are not based on the mechanism of action of immunotherapy broadly available for testing. agents, and the lack of widespread clinical expertise with immunotherapy presents a challenge for fully realgen.4 The cells are extracted from patients through izing the therapeutic opportunities of emerging imleukapheresis and require ex vivo loading of the PAP munotherapeutic strategies. Most importantly, the major and GM-CSF, transport back to the clinic, and IV infubarrier to the development of effective immunotherapy sion into patients. In the pivotal randomized phase 3 is the lack of broad availability of already invented imtrial, vaccination improved median survival by 4.1 munotherapy agents with known and profound ability months in patients with asymptomatic or mildly sympto augment immune responses. Agents from the intertomatic metastatic castration-resistant prostate cancer.4 leukin (IL) family, such as IL-15 and IL-7, have high poThis was the first vaccine to be approved in the United tential to benefit cancer patients but are not broadly States for the treatment of established cancer utilizing available for testing. The Cancer Immunotherapy Trials

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an antigen-specific target. Vaccination is generally well tolerated, but challenges with autologous cell collection and viability, ex vivo manipulation and regulatory requirements, and the lack of a clear correlation between survival and induction of PAP-specific T-cell immunity suggest that further studies are needed to optimize this form of immunotherapy. Because clinical development of sipuleucel-T for FDA approval began in 1997, the formulation and regimen of sipuleucel-T have remained unchanged for almost 15 years. Given the advances made in immunology and immunotherapy in the past decade and a half, it is axiomatic that regimens based on current immunologic science would provide higher and longerlasting immune responses (ie, greater areas under the curve) and, in the case of sipuleucel-T, enhanced patient benefit. The question remains, “Which strategies are most likely to be effective and the most ripe for testing?” Agents such as IL-15, IL-7, anti–CTLA-4, and anti– PD-1 (programmed death 1) are among the priority agents being tested by the CITN and others that are likely to increase the efficacy of sipuleucel-T.

Ipilimumab is a humanized anti–CTLA-4 monoclonal antibody and has demonstrated therapeutic benefit in patients with metastatic melanoma. CTLA-4 is an inhibitory checkpoint receptor expressed on the surface of T cells, where it serves to inhibit T-cell activation and helps regulate the balance between immune activation and tolerance.13-15 T-cell function is regulated by a series of signals typically provided by antigen-presenting cells.16,17 In preclinical studies, the addition of an antagonist CTLA-4 monoclonal antibody with a specific vaccine was shown to induce antigen-specific T-cell activation and mediate rejection of B16 melanoma in mice.18 Ipilimumab is a humanized anti–CTLA-4 monoclonal antibody and has demonstrated therapeutic benefit in patients with metastatic melanoma.19-21 In a dose-finding trial, objective re-

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sponses were seen in 11.1% of patients at the 10-mg/kg dose and in 4.2% at the 3-mg/kg dose, with no responses at the lower dose.19 The early studies of ipilimumab also identified a unique toxicity profile characterized by autoimmune events, including dermatitis, colitis, hepatitis, endocrinopathies, and neuritis.22-24 Mortality related to bowel perforation was reported in less than 2% of patients in early studies before the development of autoimmune toxicity was recognized. The autoimmune side effects are manageable with early use of low-dose steroids and, rarely, more intensive immunosuppressive treatment.24 The pivotal phase 3 clinical trial was a prospective, randomized, double-blind study of 676 HLA-A2 patients with previously treated metastatic melanoma.25 Patients treated with ipilimumab demonstrated an overall survival benefit of 10 months compared with 6.4 months in the vaccine-alone arm.25 A subsequent trial in treatment-naive metastatic melanoma patients demonstrated that overall survival was significantly prolonged to 11.2 months in the ipilimumab-treated patients compared with 9.1 months in dacarbazine-treated patients. A survival effect persisted at 3 years, with 20.8% alive in the ipilimumab/dacarbazine-treated arm compared with 12.2% in the dacarbazine-alone arm (hazard ratio for death, 0.72; P<.001).26 An interesting finding in both phase 3 ipilimumab studies was the lack of improvement in progression-free survival, suggesting that the immune response is slow to develop and can result in a delayed therapeutic response. Indeed, studies have shown that responses may be delayed for several months, and this has led to a new set of clinical immune response guidelines for clinical monitoring of patients on immunotherapy studies.27,28 These guidelines require further validation, and this may be possible through the CITN. PD-1 is another T-cell coinhibitory receptor that binds to the PD-1 and PD-2 ligands (PD-L1, PD-L2) on antigen-presenting cells and suppresses T-cell activation. PD-1 is highly expressed on both activated and exhausted T cells following exposure to chronic antigen, while PD-L1 is expressed directly on cancer cells in a

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number of different tumors, including melanoma, renal cell, colorectal, ovarian, and non–small cell lung cancer (NSCLC).29-39 A humanized antibody to PD-1 has been evaluated in patients with previously treated solid tumors, with objective responses reported in patients with colorectal cancer, melanoma, and NSCLC.40,41 More recently, a phase 1 clinical trial using an anti–PD-L1 monoclonal antibody in a dose-escalation design ranging from 0.3 mg/kg to 10 mg/kg was conducted in patients with metastatic cancer, with objective clinical responses observed in 9 of 52 evaluable melanoma, 2 of 17 renal cell carcinoma, 5 of 49 NSCLC, and 1 of 17 ovarian cancer patients.42 These clinical data are encouraging, and there are numerous other agents that have shown preclinical potential or early-stage clinical evidence of therapeutic effectiveness. For example, novel cytokines in development include IL-15, IL-18, IL-21, and new immune checkpoint-targeted monoclonal antibodies against OX40, 4-1BB, GITR, and CD27 are in development. Further, there is evidence that blockade of CTLA-4 and PD-1 can act synergistically against the murine B16 melanoma, providing evidence that combination immunotherapy should be pursued in the clinic.43 Because of the availability of these new agents, coupled with the cost of drug development and the need for more appropriate clinical trial designs that can better capture the impact of immunotherapy drugs, a model for prioritization of agents and trial design is needed to ensure that the full impact of tumor immunotherapy can be realized for patients with cancer.

work performed through the network is expediting regulatory approval of cancer immunotherapy. CITN members help design novel early-phase trials developing strategies and biomarkers that inform phase 3 pivotal trials. The CITN will implement and complete complex multicomponent trials that facilitate subsequent development pathways, particularly of agents in combination. The CITN will also provide high-quality immune response and biomarker data that elucidate mechanism of response and inform design of subsequent trials.

The goal of the CITN is to facilitate broad availability of multiple immunotherapy agents with defined biologic function for cancer therapy. The CITN is a collaborative research project established by and operating under a grant from the National Cancer Institute (NCI) and awarded to the Central Operating and Statistical Center (COSC) at the Fred Hutchinson Cancer Research Center (FHCRC). The COSC provides overall leadership, organizational infrastructure, and statistical and protocol coordination support. A competitive grant process was used by the NCI to select 28 participating sites across the United States and Canada. Input from NCI and industry partners is also utilized to foster the identification of promising agents and integration to promote combination strategies.

Organizational Structure of the CITN Mission of the CITN The goal of the CITN is to facilitate broad availability of multiple immunotherapy agents with defined biologic function for cancer therapy. The CITN is selecting, designing, and conducting early-phase trials with highly promising immunotherapy agents and provides a platform for high-quality immune monitoring and biomarker studies essential to inform subsequent development pathways leading to the commercialization of these agents for treating patients with cancer. The

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The organization model of the CITN is an interactive, inclusive organization whose members and collaborators strive toward common goals. The overall organizational structure and governance of the CITN is outlined in the Figure. The CITN, collaborating with the NCI, industry, and various disease-oriented and nonprofit foundations, uses the collective experience and wisdom in the field to prioritize and develop optimal trials in a synergistic fashion that will be more informative than those performed by scientists and companies

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working in isolation. The NCI, FHCRC, and member institutions each contributes resources to the CITN. Within the NCI, the Biological Resources Branch, Biometrics Research Branch, and Cancer Therapy Evaluation Program (CTEP) provide support to CITN trials. CTEP plays an important role in study regulatory and data management through the Cancer Trials Support Unit, site monitoring and auditing through the Clinical Trials Monitoring Branch, and application for investigational new drugs through the Regulatory Affairs Branch. Three core facilities are provided by FHCRC, specifically in collaboration with the HIV Vaccine Trials Network (regulatory and trial operations support), the Statistical Center for HIV/AIDS Research & Prevention (supporting statistical design and analysis), and a

Each member site provides guidance in trial design, patient enrollment, safety reporting, protocol compliance, as well as biospecimen collection and laboratory analysis. joint collaboration with FHCRC and the University of Washington (scientific leadership and laboratory management). Each member site provides guidance in trial design, patient enrollment, safety reporting, protocol compliance, as well as biospecimen collection and laboratory analysis. To foster new cancer immunotherapy clinical trials, the CITN works closely with corporate/pharmaceutical entities to identify and select agents for investigation and to obtain access to these therapeutics. Given the complexity of trial implementation, the CITN partners with foundations and nonprofit organizations with expertise in a specific disease or therapeutic area. Leadership of the CITN comprises the Executive Committee including the COSC principal investigator (PI), 3 PIs from member sites, an administrative director, laboratory director, and NCI program officer (Figure). At the level of an identified drug and selected

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protocol, the CITN organizes Concept Working Groups, which have the responsibility of determining the study design and final clinical trial protocol. The Working Group includes a chair and cochairs from member sites, consultants familiar with the disease area or the therapeutic, a statistician, patient advocate, protocol development manager, immune monitoring core representative, CTEP/NCI member, and an industry representative, depending on the agent and industry interest in contributing.

Processes of the CITN The list of priority agents to be investigated by the CITN resulted from 3 prior NCI workshops and feedback from over 80 leaders providing clinical and scientific expertise. The first workshop, Immunotherapy Agent Workshop, ranked the top 20 agents from 126 suggestions with known substantial immunologic activity that have not been adequately tested in cancer patients.44 Shortly thereafter, the Cancer Antigen Prioritization Project ranked 75 target cancer antigens according to predetermined and predefined characteristics to focus on the 6 most promising.45 Finally, given the potential for combining agents, an Immune Response Modifier Pathway Working Group developed criteria to structure the combination of immunopotentiating agents with vaccines in clinical trials.46 The final list of top agents to bring to patients in clinical trials is shown in Table 1 and includes T-cell growth factors (IL-7 and IL-15), dendritic cell activators (anti-CD40), inhibitors of Tcell checkpoint blockade (anti–PD-1), dendritic cell growth factors (Flt3L), vaccine adjuvants (IL-12), and T-cell stimulators (4-1BB). Clinical trials entering the CITN are selected by a peer review process. Trials can be submitted from both academia and industry. A Letter of Intent is reviewed by the CITN Executive Committee and either rejected or forwarded to the CITN Steering Committee for further review. The Steering Committee is composed of a subgroup of CITN site investigators. Members of the Steering Committee serve for 3-year terms. The com-

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Figure. Organizational Structure of the Cancer Immunotherapy Trials Network FHCRC/UW Scientific leadership Lab management SCHARP Statistical design and analysis

HVTN Core, Fiscal, Trial Operations Regulatory

Fred Hutchinson Cancer Research Center

Foundations or Nonprofit Entities

Concept and Trial Collaboration Biometrics Research Branch Review data

Member Sites

Cancer Immunotherapy Trials Network

National Cancer Institute

RAB INDs CTSU Trial/regulatory support, EDC/ data mgmt

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Patient Enrollment Safety reporting Protocol compliance

Corporate Entities Define strategies for agent approval, access to agents Biological Resources Branch

Cancer Therapy Evaluation Program (CTEP)

mittee will approve or disapprove the proposal and assign the concept a priority. High-priority concepts move forward in the system, while approved but lower-priority concepts may be held while an alternate funding strategy is developed. Once a concept is deemed high priority, a lead investigator is identified and a Working Group is formed. This Working Group fully develops the protocol. Simultaneously, the Correlative Sciences Committee works with the protocol group to develop the laboratory analysis to support the study. Once completed, the protocol moves forward for institutional and CTEP approval.

Biospecimen collection Lab analysis contract

Trial Designs Committee Leadership

CTMB Site audits/ monitoring

FHCRC: Fred Hutchinson Cancer Research Center UW: University of Washington HVTN: HIV Vaccine Trials Network SCHARP: Statistical Center for HIV/AIDS Research & Prevention CTSU: Cancer Trials Support Unit CTMB: Clinical Trials Monitoring Branch RAB: Regulatory Affairs Branch IND: Investigational new drugs

During the review process, the CITN Executive Committee determines the source of and obtains the proposed immunotherapy agent(s), discusses with member sites and determines the financial expense of the trial, and reviews the trial implementation/start-up steps needed at participating institutions. Given the limited per patient budget of the CITN, depending on the expense of the particular trial, secondary sources of funding are obtained. Prior to finalization and CTEP approval, pharmaceutical/industrial agreements are reached in order to guarantee drug supply. A key component of the CITN is a central immuno-

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Table 1. CITN Trials in Development as of August 2012 Agent (rank)*

Function

Trial(s)

IL-15 (#1)

T-cell and natural killer cell growth factor

Trial with NCI E coli rhIL-15 in solid tumors to develop a subcutaneous regimen with a safety profile appropriate for combining with vaccines, standard antibody therapy, and other agents; protocol submitted to CTEP (PIs: Miller [U Minnesota] and Kohrt [Stanford U]) Trial with Altor mammalian-derived IL-15/IL-15αSu/Fc Fusion Complex, an IL-15 agent with theoretically improved pharmacokinetics; to be cofunded by approved Melanoma Research Alliance grant to Dr Margolin (PI: Margolin [U Washington])

IL-7 (#5)

T-cell growth factor

Trial of sipuleucel-T (Provenge; Dendreon) + IL-7 (Cytheris) modulate first FDA-approved cancer vaccine; LOI submitted to CTEP; grant submitted to Prostate Cancer Foundation for cofunding (PIs: Fong [UC San Francisco] and Ferrari [New York U]) Trial of MAGE-A3 + AS15 ASCI (GSK) + IL-7 (Cytheris); commitment for agents and partial funding by GSK and Cytheris (PI: Gajewski [U Chicago])

Anti-CD40 (#4)

Dendritic cell activator

Trial of neoadjuvant CP-870,893 (Pfizer) in resectable pancreas cancer; initiated and led by Dr Vonderheide at U Penn as single institution with commitment for expansion to other CITN sites; cofunded by U Penn and CITN; protocol approved by Institutional Review Board and FDA

Flt3 Ligand (#11)

Dendritic cell growth factor

Trial of Flt3 ligand to expand DC followed by poly ICLC (#15*) and Resiquimod (#18*) to activate DC and NY-ESO-1-DEC-205 fusion protein vaccine to target DC; Celldex committed to provide agents; in collaboration with CVC/CRI investigators (PIs: Wolchok [MSKCC], Odunsi [Roswell Park CC], Bhardwaj [New York U]; all three are CITN and CVC/CRI investigators)

IDO Inhibitors (#7)

IDO inhibition

Trials in development with Incyte (INCB24360) and/or NewLink Genetics (1-MT), most likely in ovarian cancer and melanoma (Evaluating concepts by Odunsi [Roswell Park CC], Slingluff [U Virginia])

Anti–PD-1 (#2)

Anti-checkpoint

Active discussions with Merck for trials in lymphoma, ovarian, and head & neck cancers (Evaluating concepts by Kohrt, Levy [Stanford U], Coukos, Adams [U Penn], Pai [Johns Hopkins U])

Anti–IL-10 (#10)

Inhibitor of suppression

Active discussions with Merck for trials in ovarian and breast cancer (Evaluating concepts by Coukos [U Penn] and Salazar [U Washington])

*Numbers represent ranking from the NCI Immunotherapy Agent Workshop; https://dcb.nci.nih.gov/Reports/Pages/ immunotherapyagentworkshop.aspx. CITN indicates Cancer Immunotherapy Trials Network; CTEP, Cancer Therapy Evaluation Program; CVC/CRI, Cancer Vaccine Collaborative/Cancer Research Institute; DC, dendritic cell; IDO, indoleamine 2,3-dioxygenase; GSK, GlaxoSmithKline; IL-7, interleukin-7; IL-10, interleukin-10; IL-15, interleukin-15; LOI, Letter of Intent; MSKCC, Memorial Sloan-Kettering Cancer Center; NCI, National Cancer Institute; PD-1, programmed death 1; PI, principal investigator; rhIL-15, recombinant human IL-15.

logic monitoring laboratory and a CITN member laboratory network. The central laboratory assures adequate shipping and processing of samples from the studies and manages the assays that will be performed by the central

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laboratory or other laboratories in the network. Within the network lies significant expertise in basic immunologic monitoring, flow cytometry, analysis of the tumor microenvironment, assessment of circulating tumor

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Table 2. Participating CITN Study Sites in the United States and Canada State/Province

Study Site

Principal Investigator

Site Contact

California

Stanford University UC San Diego UC San Francisco Yale University Moffitt Cancer Center University of Miami Emory University Rush University University of Chicago National Cancer Institute Dana-Farber Cancer Institute University of Minnesota Dartmouth University Memorial Sloan-Kettering Cancer Center New York University Roswell Park Duke University Case Western Reserve Ohio State University Providence Medical Center

Ronald Levy, MD Thomas Kipps, MD, PhD Lawrence Fong, MD Mario Sznol, MD Scott Antonia, MD, PhD Joseph Rosenblatt, MD Edmund Waller, MD, PhD Howard Kaufman, MD Thomas Gajewski, MD, PhD Jeff Schlom, PhD F. Stephen Hodi, MD Jeffrey Miller, MD Marc Ernstoff, MD Jedd Wolchok, MD, PhD

(650) 498-7061 (858) 657-7000 (877) 827-3222 (203) 785-5702 (888) 663-3488 (866) 574-5124 (888) 946-7447 (312) 942-0600 (855) 702-8222 (301) 496-4164 (866) 408-3324 (888) 226-2376 (800) 639-6918 (800) 525-2225

Nina Bhardwaj, MD, PhD Kunle Odunsi, MD, PhD H. Kim Lyerly, MD Pierre Triozzi, MD William Carson, MD Walter Urba, MD, PhD

(212) 263-6485 (877) 275-7724 (888) 275-3853 (800) 641-2422 (800) 293-5123 (800) 833-8899 x56014 (855) 216-0098

Connecticut Florida Georgia Illinois Maryland Massachusetts Minnesota New Hampshire New York

North Carolina Ohio Oregon Pennsylvania

University of Pennsylvania University of Pittsburgh

Texas

Baylor University MD Anderson Cancer Center University of Virginia University of Washington University of Wisconsin University of Toronto

Virginia Washington Wisconsin Ontario

cells, and other specialized assays. The laboratory analyses are prioritized into primary and secondary assays. Primary assays are those that are performed during the course of the study, and secondary assays are those that may be performed once the study has been completed. Prioritization of the analysis maximizes the collection of useful information in the most efficient manner possible.

Member Sites of the CITN The CITN selected member sites through a competitive National Institutes of Health grant process and se-

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Carl June, MD Robert Ferris, MD, PhD Hassane Zarour, MD Karolina Palucka, MD, PhD Laurence Cooper, MD, PhD Craig Slingluff, MD John Thompson, MD Paul Sondel, MD, PhD Pamela Ohashi, PhD

(877) 470-7241 (214) 820-7451 (877) 632-6789 (434) 924-5022 (855) 557-0555 (800) 622-8922 (416) 946-2000

lection criteria, including basic tumor immunotherapy experience at the site, willingness to participate in proposed clinical trials, availability of clinical trial infrastructure, and ability to participate in establishing validation standards or collect biospecimen data for inclusion in immune monitoring and biomarker correlative studies. Member sites were asked to select a PI for coordinating the activities at each site and to participate in the executive committee. The member sites are located throughout the continental United States and Canada, assuring patient access for pivotal clinical trials. The member sites and PI contact information is listed

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in Table 2. Further information and updates are available on the CITN Web site at www.CITNinfo.org.

How to Refer to the CITN Clinical trials initiated through the CITN will be listed on www.clinicaltrials.gov, at member institutions’ trial registries, and at www.CITNinfo.org. Study contacts, including study PI or trial coordinator will be listed for each participating institution in a CITN organized clinical trial. Patients are encouraged to speak with their primary oncologist to discuss their interest in clinical trials, including CITN and non-CITN developed trials. Risks and benefits of a clinical trial and alternative treatment options should be discussed when considering a patient’s next therapy. Referring physicians should contact a local PI or co-PI based on the specific trial of interest. Contact information, similarly, can be obtained at the sites listed above. Pharmaceutical and industry representatives with interest in collaboration should contact Martin A. “Mac” Cheever, MD, the principal investigator of the CITN based at the FHCRC.

munotherapy agents. The NCI has established the CITN as a means to prioritize immunotherapy agents and combinations, gain access to high-priority agents, develop clinical trial designs that are appropriate for detecting therapeutic effectiveness, validating and incorporating correlative immune monitoring and biomarker assays into clinical trials, and implementing a national network for patient participation in pivotal tumor immunotherapy trials. The CITN provides a uniquely organized effort to conduct early-phase trials, with a focus on trials likely to achieve the quickest route to proof of concept, demonstration of patient benefit, and provide a pathway to regulatory approval. By accelerating ongoing interactions between CITN investigators, industry, foundations, and nonprofit entities, the CITN strives to have many immunotherapy agents with defined biologic function broadly available for rapid clinical trial evaluation. The CITN will play a significant role in firmly establishing the effectiveness of tumor immunotherapy and defining the clinical application of immunotherapy as a standard treatment for patients with cancer. u

Acknowledgments

Patients are encouraged to speak with their primary oncologist to discuss their interest in clinical trials, including CITN and non-CITN developed trials.

The authors would like to acknowledge Dr “Mac” Cheever for useful discussions and guidance in the manuscript preparation, and Judith Kaiser for providing investigator contact information.

References Conclusion Cancer immunotherapy has come of age, and the promise of improved survival by targeting the immune response against cancer has been demonstrated with several agents, including sipuleucel-T and ipilimumab. However, this marks only the beginning of an era of immunotherapy that faces significant challenges in selection of agents, design of clinical trials, ensuring availability of novel therapies, and developing processes for working through the complex regulatory, intellectual property, and financial challenges for combining im-

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1. Krieg AM. Therapeutic potential of Toll-like receptor 9 activation. Nat Rev Drug Discov. 2006;5:471-484. 2. Mellman I, Coukos G, Dranoff G. Cancer immunotherapy comes of age. Nature. 2011;480:480-489. 3. Topalian SL, Weiner GJ, Pardoll DM. Cancer immunotherapy comes of age. J Clin Oncol. 2011;29:4828-4836. 4. Kantoff PW, Higano CS, Shore ND, et al. Sipuleucel-T immunotherapy for castration-resistant prostate cancer. N Engl J Med. 2010;363:411-422. 5. Hodi FS, O’Day SJ, McDermott DF, et al. Improved survival with ipilimumab in patients with metastatic melanoma. N Engl J Med. 2010;363:711-723. 6. Thomas ED, Lochte HL Jr, Lu WC, et al. Intravenous infusion of bone marrow in patients receiving radiation and chemotherapy. N Engl J Med. 1957;257:491-496. 7. Maloney DG. Immunotherapy for non-Hodgkin’s lymphoma: monoclonal antibodies and vaccines. J Clin Oncol. 2005;23:6421-6428. 8. Houot R, Levy R. Idiotype vaccination for lymphoma: moving towards optimisation. Leuk Lymphoma. 2009;50:1-2. 9. Houot R, Levy R. Vaccines for lymphomas: idiotype vaccines and beyond. Blood Rev. 2009;23:137-142.

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10. Peled N, Oton AB, Hirsch FR, et al. MAGE A3 antigen-specific cancer immunotherapeutic. Immunotherapy. 2009;1:19-25. 11. Korman AJ, Peggs KS, Allison JP. Checkpoint blockade in cancer immunotherapy. Adv Immunol. 2006;90:297-339. 12. Stebbings R, Findlay L, Edwards C, et al. “Cytokine storm” in the phase I trial of monoclonal antibody TGN1412: better understanding the causes to improve preclinical testing of immunotherapeutics. J Immunol. 2007;179:3325-3331. 13. Waterhouse P, Penninger JM, Timms E, et al. Lymphoproliferative disorders with early lethality in mice deficient in Ctla-4. Science. 1995;270:985-988. 14. Tivol EA, Borriello F, Schweitzer AN, et al. Loss of CTLA-4 leads to massive lymphoproliferation and fatal multiorgan tissue destruction, revealing a critical negative regulatory role of CTLA-4. Immunity. 1995;3:541-547. 15. Chambers CA, Sullivan TJ, Allison JP. Lymphoproliferation in CTLA4-deficient mice is mediated by costimulation-dependent activation of CD4+ T cells. Immunity. 1997;7:885-895. 16. Greenwald RJ, Freeman GJ, Sharpe AH. The B7 family revisited. Annu Rev Immunol. 2005;23:515-548. 17. Salama AK, Hodi FS. Cytotoxic T-lymphocyte-associated antigen-4. Clin Cancer Res. 2011;17:4622-4628. 18. van Elsas A, Hurwitz AA, Allison JP. Combination immunotherapy of B16 melanoma using anti-cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) and granulocyte/macrophage colony-stimulating factor (GMCSF)-producing vaccines induces rejection of subcutaneous and metastatic tumors accompanied by autoimmune depigmentation. J Exp Med. 1999;190:355-366. 19. Wolchok JD, Neyns B, Linette G, et al. Ipilimumab monotherapy in patients with pretreated advanced melanoma: a randomised, double-blind, multicentre, phase 2, dose-ranging study. Lancet Oncol. 2010;11:155-164. 20. O’Day SJ, Maio M, Chiarion-Seleni V, et al. Efficacy and safety of ipilimumab monotherapy in patients with pretreated advanced melanoma: a multicenter single-arm phase II study. Ann Oncol. 2010;21:1712-1717. 21. Weber J, Thompson JA, Hamid O, et al. A randomized, double-blind, placebo-controlled, phase II study comparing the tolerability and efficacy of ipilimumab administered with or without prophylactic budesonide in patients with unresectable stage III or IV melanoma. Clin Cancer Res. 2009;15:5591-5598. 22. Robinson MR, Chan CC, Yang JC, et al. Cytotoxic T lymphocyteassociated antigen 4 blockade in patients with metastatic melanoma: a new cause of uveitis. J Immunother. 2004;27:478-479. 23. Blansfield JA, Beck KE, Tran K, et al. Cytotoxic T-lymphocyte-associated antigen-4 blockage can induce autoimmune hypophysitis in patients with metastatic melanoma and renal cancer. J Immunother. 2005;28:593-598. 24. Phan GQ, Yang JC, Sherry RM, et al. Cancer regression and autoimmunity induced by cytotoxic T lymphocyte-associated antigen 4 blockade in patients with metastatic melanoma. Proc Natl Acad Sci U S A. 2003; 100:8372-8377. 25. Hodi FS, O’Day SJ, McDermott DF, et al. Improved survival with ipilimumab in patients with metastatic melanoma. N Engl J Med. 2010;363: 711-723. 26. Robert C, Thomas L, Bondarenko I, et al. Ipilimumab plus dacarbazine for previously untreated metastatic melanoma. N Engl J Med. 2011;364: 2517-2526. 27. Wolchok JD, Hoos A, O’Day S, et al. Guidelines for the evaluation of immune therapy activity in solid tumors: immune-related response criteria. Clin Cancer Res. 2009;15:7412-7420.

28. Hoos A, Eggermont AM, Janetzki S, et al. Improved endpoints for cancer immunotherapy trials. J Natl Cancer Inst. 2010;102:1388-1397. 29. Freeman GJ, Long AJ, Iwai Y, et al. Engagement of the PD-1 immunoinhibitory receptor by a novel B7 family member leads to negative regulation of lymphocyte activation. J Exp Med. 2000;192:1027-1034. 30. Barber DL, Wherry EJ, Masopust D, et al. Restoring function in exhausted CD8 T cells during chronic viral infection. Nature. 2006;439:682-687. 31. Hirano F, Kaneko K, Tamura H, et al. Blockade of B7-H1 and PD-1 by monoclonal antibodies potentiates cancer therapeutic immunity. Cancer Res. 2005;65:1089-1096. 32. Sheppard KA, Fitz LJ, Lee JM, et al. PD-1 inhibits T-cell receptor induced phosphorylation of the ZAP70/CD3zeta signalosome and downstream signaling to PKCtheta. FEBS Lett. 2004;574:37-41. 33. Okazaki T, Maeda A, Nishimura H, et al. PD-1 immunoreceptor inhibits B cell receptor-mediated signaling by recruiting src homology 2-domain-containing tyrosine phosphatase 2 to phosphotyrosine. Proc Natl Acad Sci U S A. 2001;98:13866-13871. 34. Yamazaki T, Akiba H, Iwai H, et al. Expression of programmed death 1 ligands by murine T cells and APC. J Immunol. 2002;169:5538-5545. 35. Iwai Y, Ishida M, Tanaka Y, et al. Involvement of PD-L1 on tumor cells in the escape from host immune system and tumor immunotherapy by PD-L1 blockade. Proc Natl Acad Sci U S A. 2002;99:12293-12297. 36. Hino R, Kabashima K, Kato Y, et al. Tumor cell expression of programmed cell death-1 ligand 1 is a prognostic factor for malignant melanoma. Cancer. 2010;116:1757-1766. 37. He YF, Zhang GM, Wang XH, et al. Blocking programmed death-1 ligand-PD-1 interactions by local gene therapy results in enhancement of antitumor effect of secondary lymphoid tissue chemokine. J Immunol. 2004;173:4919-4928. 38. Strome SE, Dong H, Tamura H, et al. B7-H1 blockade augments adoptive T-cell immunotherapy for squamous cell carcinoma. Cancer Res. 2003;63:6501-6505. 39. Okazaki T, Honjo T. PD-1 and PD-1 ligands: from discovery to clinical application. Int Immunol. 2007;19:813-824. 40. Brahmer JR, Drake CG, Wollner I, et al. Phase I study of single-agent anti-programmed death-1 (MDX-1106) in refractory solid tumors: safety, clinical activity, pharmacodynamics, and immunologic correlates. J Clin Oncol. 2010;28:3167-3175. 41. Topalian SL, Hodi FS, Brahmer JR, et al. Safety, activity, and immune correlates of anti-PD-1 antibody in cancer. N Engl J Med. 2012;366:24432454. 42. Brahmer JR, Tykodi SS, Chow LQ, et al. Safety and activity of antiPD-L1 antibody in patients with advanced cancer. N Engl J Med. 2012; 366:2455-2465. 43. Curran MA, Montalvo W, Yagita H, et al. PD-1 and CTLA-4 combination blockade expands infiltrating T cells and reduces regulatory T and myeloid cells within B16 melanoma tumors. Proc Natl Acad Sci U S A. 2010;107:4275-4280. 44. National Cancer Institute Immunotherapy Agent Workshop. https://dcb.nci.nih.gov/Reports/Pages/immunotherapyagentworkshop.aspx. Accessed September 20, 2012. 45. Cheever MA, Allison JP, Ferris AS, et al. The prioritization of cancer antigens: a National Cancer Institute pilot project for the acceleration of translational research. Clin Cancer Res. 2009;15:5323-5337. 46. Cheever MA, Matrisian LM. Report of the Immune Response Modifier Pathway Prioritization Working Group (IRMP WG), November 2009. http://deainfo.nci.nih.gov/advisory/ctac/workgroup/ctacsupmat.htm. Accessed September 20, 2012.

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The Last Word

A Personal Introduction and Invitation to Join My Journey Through the World of Personalized Medicine

W

elcome to our new column, The Last Word. realms of the healthcare process and fire your imaginaAt the outset, let me comment on the tion by opening up new vistas of this still nascent irony of the title, for this is not a forum that process of care whose implications and downstream efpresumes to have the “last word” on any aspects of perfects are so plentiful. This model of care is facilitated by sonalized medicine. The column will new technologies, but its mission is serve as the concluding editorial in timeless: the ancient pursuit to bring each issue of Personalized Medicine in health to those who have lost it and Oncology, where I am given the chance stand to lose their lives without stopto explore the extraordinary opportuping the process of destruction that nities personalized medicine offers cancer is posing to them. patients. Along the way, The Last Word will Permit me to acquaint you with me stop to explore the very matter of as you join my journey through the change, how disruptive innovation ininner workings of our healthcare sysherently repels all but a small group tem. I am a veteran of nearly 40 years known to pharmaceutical marketers as in the healthcare industry, which innovators, who take their place on a Robert E. Henry began with pre-med studies motivated classic bell-shaped curve for new prodby an enduring desire to heal. Howuct adoption. It will examine how clinever, a nagging desire to understand human nature led ical oncologists operating within the population-based me to graduate with a major in the humanities. But model of care must overcome their comfort level with healthcare beckoned again, and leaving graduate studies it and find how to live with the uncertainties of a new in history to join a pharmaceutical company, I soon paradigm that eradicates old fixed boundaries that deforged a career in medical education programs and pubfined expectations. It will explore healthcare delivery as lishing that fuses humanities with medical and managed a matter of overall resource allocation. care best practices. Convinced that medical care is So sit back and get ready to enjoy the ride. I can even at heart a cultural pursuit and not merely scientific, I promise to share a most apt quote from a very old Joan will discuss the balance between healthcare discovery Baez folk song. These are all part of The Last Word – it’s and value. the last word in enjoyment of the learning process that The Last Word will position healthcare as the crown goes with an initiative as splendid as the personalized of a civilized culture, with personalized medicine fulfillmedicine model for oncologic care. u ing medicine’s cultural pursuit to serve individual paYour host, tient’s needs, not grouping patients together in a depersonalized population-based manner. I hope that you will find The Last Word every bit as fascinating as my own exploration of uncharted waters Robert E. Henry of healthcare has been. I will take you into the inner

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AVASTIN® (bevacizumab) Solution for intravenous infusion Initial U.S. Approval: 2004 WARNING: GASTROINTESTINAL PERFORATIONS, SURGERY AND WOUND HEALING COMPLICATIONS, and HEMORRHAGE Gastrointestinal Perforations The incidence of gastrointestinal perforation, some fatal, in Avastin-treated patients ranges from 0.3 to 2.4%. Discontinue Avastin in patients with gastrointestinal perforation. [See Dosage and Administration (2.4), Warnings and Precautions (5.1).] #

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Surgery and Wound Healing Complications The incidence of wound healing and surgical complications, including serious and fatal complications, is increased in Avastin-treated patients. Discontinue Avastin in patients with wound dehiscence. The appropriate interval between termination of Avastin and subsequent elective surgery required to reduce the risks of impaired wound healing/wound dehiscence has not been determined. Discontinue at least 28 days prior to elective surgery. Do not initiate Avastin for at least 28 days after surgery and until the surgical wound is fully healed. [See Dosage and Administration (2.4), Warnings and Precautions (5.2), Adverse Reactions (6.1).] Hemorrhage Severe or fatal hemorrhage, including hemoptysis, gastrointestinal bleeding, central nervous systems (CNS) hemorrhage, epistaxis, and vaginal bleeding occurred up to five-fold more frequently in patients receiving Avastin. Do not administer Avastin to patients with serious hemorrhage or recent hemoptysis. [See Dosage and Administration (2.4), Warnings and Precautions (5.3), Adverse Reactions (6.1).] 1 INDICATIONS AND USAGE 1.1 Metastatic Colorectal Cancer (mCRC) Avastin is indicated for the first- or second-line treatment of patients with metastatic carcinoma of the colon or rectum in combination with intravenous 5-fluorouracil– based chemotherapy.

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1.2 Non-Squamous Non–Small Cell Lung Cancer (NSCLC) Avastin is indicated for the first-line treatment of unresectable, locally advanced, recurrent or metastatic non–squamous non–small cell lung cancer in combination with carboplatin and paclitaxel. 1.3 Glioblastoma Avastin is indicated for the treatment of glioblastoma with progressive disease in adult patients following prior therapy as a single agent. The effectiveness of Avastin in glioblastoma is based on an improvement in objective response rate. There are no data demonstrating an improvement in disease-related symptoms or increased survival with Avastin. [See Clinical Studies (14.3).] 1.4 Metastatic Renal Cell Carcinoma (mRCC) Avastin is indicated for the treatment of metastatic renal cell carcinoma in combination with interferon alfa. 4 CONTRAINDICATIONS None. 5 WARNINGS AND PRECAUTIONS 5.1 Gastrointestinal Perforations Serious and sometimes fatal gastrointestinal perforation occurs at a higher incidence in Avastin treated patients compared to controls. The incidence of gastrointestinal perforation ranged from 0.3 to 2.4% across clinical studies. [See Adverse Reactions (6.1).] The typical presentation may include abdominal pain, nausea, emesis, constipation, and fever. Perforation can be complicated by intra-abdominal abscess and fistula formation. The majority of cases occurred within the first 50 days of initiation of Avastin. Discontinue Avastin in patients with gastrointestinal perforation. [See Boxed Warning, Dosage and Administration (2.4).]

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5.2 Surgery and Wound Healing Complications Avastin impairs wound healing in animal models. [See Nonclinical Toxicology (13.2).] In clinical trials, administration of Avastin was not allowed until at least 28 days after surgery. In a controlled clinical trial, the incidence of wound healing complications, including serious and fatal complications, in patients with mCRC who underwent surgery during the course of Avastin treatment was 15% and in patients who did not receive Avastin, was 4%. [See Adverse Reactions (6.1).] Avastin should not be initiated for at least 28 days following surgery and until the surgical wound is fully healed. Discontinue Avastin in patients with wound healing complications requiring medical intervention. The appropriate interval between the last dose of Avastin and elective surgery is unknown; however, the half-life of Avastin is estimated to be 20 days. Suspend Avastin for at least 28 days prior to elective surgery. Do not administer Avastin until the wound is fully healed. [See Boxed Warning, Dosage and Administration (2.4).] 5.3 Hemorrhage Avastin can result in two distinct patterns of bleeding: minor hemorrhage, most commonly Grade 1 epistaxis; and serious, and in some cases fatal, hemorrhagic events. Severe or fatal hemorrhage, including hemoptysis, gastrointestinal bleeding, hematemesis, CNS hemorrhage, epistaxis, and vaginal bleeding occurred up to five-fold more frequently in patients receiving Avastin compared to patients receiving only chemotherapy. Across indications, the incidence of Grade ≥ 3 hemorrhagic events among patients receiving Avastin ranged from 1.2 to 4.6%. [See Adverse Reactions (6.1).] Serious or fatal pulmonary hemorrhage occurred in four of 13 (31%) patients with squamous cell histology and two of 53 (4%) patients with non-squamous non-small cell lung cancer receiving Avastin and chemotherapy compared to none of the 32 (0%) patients receiving chemotherapy alone. In clinical studies in non–small cell lung cancer where patients with CNS metastases who completed radiation and surgery more than 4 weeks prior to the start of Avastin

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AVASTIN® (bevacizumab)

AVASTIN® (bevacizumab)

AVASTIN® (bevacizumab)

were evaluated with serial CNS imaging, symptomatic Grade 2 CNS hemorrhage was documented in one of 83 Avastin-treated patients (rate 1.2%, 95% CI 0.06%–5.93%). Intracranial hemorrhage occurred in 8 of 163 patients with previously treated glioblastoma; two patients had Grade 3–4 hemorrhage. Do not administer Avastin to patients with recent history of hemoptysis of ≥ 1/2 teaspoon of red blood. Discontinue Avastin in patients with hemorrhage. [See Boxed Warning, Dosage and Administration (2.4).]

Dosage and Administration (2.4), Warnings and Precautions (5.2).] L Hemorrhage [See Boxed Warning, Dosage and Administration (2.4), Warnings and Precautions (5.3).] L Non-Gastrointestinal Fistula Formation [See Dosage and Administration (2.4), Warnings and Precautions (5.4).] L Arterial Thromboembolic Events [See Dosage and Administration (2.4), Warnings and Precautions (5.5).] L Hypertensive Crisis [See Dosage and Administration (2.4), Warnings and Precautions (5.6).] L Reversible Posterior Leukoencephalopathy Syndrome [See Dosage and Administration (2.4), Warnings and Precautions (5.7).] L Proteinuria [See Dosage and Administration (2.4), Warnings and Precautions (5.8).] L Ovarian Failure [See Warnings and Precautions (5.10), Use in Specific Populations (8.6).] The most common adverse reactions observed in Avastin patients at a rate > 10% and at least twice the control arm rate, are epistaxis, headache, hypertension, rhinitis, proteinuria, taste alteration, dry skin, rectal hemorrhage, lacrimation disorder, back pain and exfoliative dermatitis. Across all studies, Avastin was discontinued in 8.4 to 21% of patients because of adverse reactions.

receiving PC alone (17.2%). Febrile neutropenia was also increased (5.4% for PC plus Avastin vs. 1.8% for PC alone). There were 19 (4.5%) infections with Grade 3 or 4 neutropenia in the PC plus Avastin arm of which 3 were fatal compared to 9 (2%) neutropenic infections in patients receiving PC alone, of which none were fatal. During the first 6 cycles of treatment, the incidence of serious infections including pneumonia, febrile neutropenia, catheter infections and wound infections was increased in the PC plus Avastin arm [58 patients (13.6%)] compared to the PC alone arm [29 patients (6.6%)]. In Study 5, one fatal event of neutropenic infection occurred in a patient with previously treated glioblastoma receiving Avastin alone. The incidence of any grade of infection in patients receiving Avastin alone was 55% and the incidence of Grade 3-5 infection was 10%.

6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data below reflect exposure to Avastin in 4198 patients with CRC, non-squamous NSCLC, glioblastoma, or mRCC trials including controlled (Studies 1, 2, 4, and 7) or uncontrolled, single arm (Study 5) treated at the recommended dose and schedule for a median of 8 to 23 doses of Avastin. [See Clinical Studies (14).] The population was aged 18-88 years (median 60 years), 43.6% male and 83.8% white. The population included 1783 first- and second-line mCRC patients who received a median of 10 doses of Avastin, 480 first-line metastatic NSCLC patients who received a median of 8 doses of Avastin, 163 glioblastoma patients who received a median of 9 doses of Avastin, and 337 mRCC patients who received a median of 16 doses of Avastin. These data also reflect exposure to Avastin in 363 patients with metastatic breast cancer (MBC) who received a median of 9.5 doses of Avastin, 669 female adjuvant CRC patients who received a median of 23 doses of Avastin and exposure to Avastin in 403 previously untreated patients with diffuse large B-cell lymphoma (DLBCL) who received a median of 8 doses of Avastin. Avastin is not approved for use in MBC, adjuvant CRC, or DLBCL.

Congestive Heart Failure (CHF) The incidence of Grade ≥ 3 left ventricular dysfunction was 1.0% in patients receiving Avastin compared to 0.6% in the control arm across indications. In patients with metastatic breast cancer (MBC), an indication for which Avastin is not approved, the incidence of Grade 3–4 CHF was increased in patients in the Avastin plus paclitaxel arm (2.2%) as compared to the control arm (0.3%). Among patients receiving prior anthracyclines for MBC, the rate of CHF was 3.8% for patients receiving Avastin as compared to 0.6% for patients receiving paclitaxel alone. The safety of continuation or resumption of Avastin in patients with cardiac dysfunction has not been studied. In previously untreated patients with diffuse large B-cell lymphoma (DLBCL), an indication for which Avastin is not approved, the incidence of CHF and decline in left-ventricular ejection fraction (LVEF) were signficantly increased in the Avastin plus R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone) arm (n=403) compared to the placebo plus R-CHOP arm (n=379); both regimens were given for 6 to 8 cycles. At the completion of R-CHOP therapy, the incidence of CHF was 10.9% in the Avastin plus R-CHOP arm compared to 5.0% in the R-CHOP alone arm [relative risk (95% CI) of 2.2 (1.3, 3.7)]. The incidence of a LVEF event, defined as a decline from baseline of 20% or more in LVEF or a decline from baseline of 10% or more to a LVEF value of less than 50%, was also increased in the Avastin plus R-CHOP arm (10.4%) compared to the R-CHOP alone arm (5.0%). Time to onset of left-ventricular dysfunction or CHF was 1-6 months after initiation of therapy in at least 85% of the patients and was resolved in 62% of the patients experiencing CHF in the Avastin arm compared to 82% in the control arm.

5.4 Non-Gastrointestinal Fistula Formation Serious and sometimes fatal non-gastrointestinal fistula formation involving tracheo-esophageal, bronchopleural, biliary, vaginal, renal and bladder sites occurs at a higher incidence in Avastin-treated patients compared to controls. The incidence of non-gastrointestinal perforation was ≤ 0.3% in clinical studies. Most events occurred within the first 6 months of Avastin therapy. Discontinue Avastin in patients with fistula formation involving an internal organ. [See Dosage and Administration (2.4).] 5.5 Arterial Thromboembolic Events Serious, sometimes fatal, arterial thromboembolic events (ATE) including cerebral infarction, transient ischemic attacks, myocardial infarction, angina, and a variety of other ATE occurred at a higher incidence in patients receiving Avastin compared to those in the control arm. Across indications, the incidence of Grade ≥ 3 ATE in the Avastin containing arms was 2.6% compared to 0.8% in the control arms. Among patients receiving Avastin in combination with chemotherapy, the risk of developing ATE during therapy was increased in patients with a history of arterial thromboembolism, or age greater than 65 years. [See Use in Specific Populations (8.5).] The safety of resumption of Avastin therapy after resolution of an ATE has not been studied. Discontinue Avastin in patients who experience a severe ATE. [See Dosage and Administration (2.4).] 5.6 Hypertension The incidence of severe hypertension is increased in patients receiving Avastin as compared to controls. Across clinical studies the incidence of Grade 3 or 4 hypertension ranged from 5-18%. Monitor blood pressure every two to three weeks during treatment with Avastin. Treat with appropriate anti-hypertensive therapy and monitor blood pressure regularly. Continue to monitor blood pressure at regular intervals in patients with Avastin-induced or -exacerbated hypertension after discontinuation of Avastin. Temporarily suspend Avastin in patients with severe hypertension that is not controlled with medical management. Discontinue Avastin in patients with hypertensive crisis or hypertensive encephalopathy. [See Dosage and Administration (2.4).] 5.7 Reversible Posterior Leukoencephalopathy Syndrome (RPLS) RPLS has been reported with an incidence of < 0.1% in clinical studies. The onset of symptoms occurred from 16 hours to 1 year after initiation of Avastin. RPLS is a neurological disorder which can present with headache, seizure, lethargy, confusion, blindness and other visual and neurologic disturbances. Mild to severe hypertension may be present. Magnetic resonance imaging (MRI) is necessary to confirm the diagnosis of RPLS. Discontinue Avastin in patients developing RPLS. Symptoms usually resolve or improve within days, although some patients have experienced ongoing neurologic sequelae. The safety of reinitiating Avastin therapy in patients previously experiencing RPLS is not known. [See Dosage and Administration (2.4).] 5.8 Proteinuria The incidence and severity of proteinuria is increased in patients receiving Avastin as compared to controls. Nephrotic syndrome occurred in < 1% of patients receiving Avastin in clinical trials, in some instances with fatal outcome. [See Adverse Reactions (6.1).] In a published case series, kidney biopsy of six patients with proteinuria showed findings consistent with thrombotic microangiopathy. Monitor proteinuria by dipstick urine analysis for the development or worsening of proteinuria with serial urinalyses during Avastin therapy. Patients with a 2 + or greater urine dipstick reading should undergo further assessment with a 24-hour urine collection. Suspend Avastin administration for ≥ 2 grams of proteinuria/24 hours and resume when proteinuria is < 2 gm/24 hours. Discontinue Avastin in patients with nephrotic syndrome. Data from a postmarketing safety study showed poor correlation between UPCR (Urine Protein/Creatinine Ratio) and 24 hour urine protein (Pearson Correlation 0.39 (95% CI 0.17, 0.57). [See Use in Specific Populations (8.5).] The safety of continued Avastin treatment in patients with moderate to severe proteinuria has not been evaluated. [See Dosage and Administration (2.4).] 5.9 Infusion Reactions Infusion reactions reported in the clinical trials and post-marketing experience include hypertension, hypertensive crises associated with neurologic signs and symptoms, wheezing, oxygen desaturation, Grade 3 hypersensitivity, chest pain, headaches, rigors, and diaphoresis. In clinical studies, infusion reactions with the first dose of Avastin were uncommon (< 3%) and severe reactions occurred in 0.2% of patients. Stop infusion if a severe infusion reaction occurs and administer appropriate medical therapy. [See Dosage and Administration (2.4).] 5.10 Ovarian Failure The incidence of ovarian failure was higher (34% vs. 2%) in premenopausal women receiving Avastin in combination with mFOLFOX chemotherapy as compared to those receiving mFOLFOX chemotherapy alone for adjuvant treatment for colorectal cancer, a use for which Avastin is not approved. Inform females of reproductive potential of the risk of ovarian failure prior to starting treatment with Avastin. [See Adverse Reactions (6.1), Use in Specific Populations (8.6).] 6 ADVERSE REACTIONS The following serious adverse reactions are discussed in greater detail in other sections of the label: L Gastrointestinal Perforations [See Boxed Warning, Dosage and Administration (2.4), Warnings and Precautions (5.1).] L Surgery and Wound Healing Complications [See Boxed Warning,

Surgery and Wound Healing Complications The incidence of post-operative wound healing and/or bleeding complications was increased in patients with mCRC receiving Avastin as compared to patients receiving only chemotherapy. Among patients requiring surgery on or within 60 days of receiving study treatment, wound healing and/or bleeding complications occurred in 15% (6/39) of patients receiving bolus-IFL plus Avastin as compared to 4% (1/25) of patients who received bolus-IFL alone. In Study 5, events of post-operative wound healing complications (craniotomy site wound dehiscence and cerebrospinal fluid leak) occurred in patients with previously treated glioblastoma: 3/84 patients in the Avastin alone arm and 1/79 patients in the Avastin plus irinotecan arm. [See Boxed Warning, Dosage and Administration (2.4), Warnings and Precautions (5.2).] Hemorrhage The incidence of epistaxis was higher (35% vs. 10%) in patients with mCRC receiving bolus-IFL plus Avastin compared with patients receiving bolus-IFL plus placebo. All but one of these events were Grade 1 in severity and resolved without medical intervention. Grade 1 or 2 hemorrhagic events were more frequent in patients receiving bolus-IFL plus Avastin when compared to those receiving bolus-IFL plus placebo and included gastrointestinal hemorrhage (24% vs. 6%), minor gum bleeding (2% vs. 0), and vaginal hemorrhage (4% vs. 2%). [See Boxed Warning, Dosage and Administration (2.4), Warnings and Precautions (5.3).] Venous Thromboembolic Events The overall incidence of Grade 3–4 venous thromboembolic events in Study 1 was 15.1% in patients receiving bolus-IFL plus Avastin and 13.6% in patients receiving bolus-IFL plus placebo. In Study 1, more patients in the Avastin containing arm experienced deep venous thrombosis (34 vs. 19 patients ) and intra-abdominal venous thrombosis (10 vs. 5 patients). The risk of developing a second thromboembolic event while on Avastin and oral anticoagulants was evaluated in two randomized studies. In Study 1, 53 patients (14%) on the bolus-IFL plus Avastin arm and 30 patients (8%) on the bolus-IFL plus placebo arm received full dose warfarin following a venous thromboembolic event (VTE). Among these patients, an additional thromboembolic event occurred in 21% (11/53) of patients receiving bolus-IFL plus Avastin and 3% (1/30) of patients receiving bolus-IFL alone. In a second, randomized, 4-arm study in 1401 patients with mCRC, prospectively evaluating the incidence of VTE (all grades), the overall incidence of first VTE was higher in the Avastin containing arms (13.5%) than the chemotherapy alone arms (9.6%). Among the 116 patients treated with anticoagulants following an initial VTE event (73 in the Avastin plus chemotherapy arms and 43 in the chemotherapy alone arms), the overall incidence of subsequent VTEs was also higher among the Avastin treated patients (31.5% vs. 25.6%). In this subgroup of patients treated with anticoagulants, the overall incidence of bleeding, the majority of which were Grade 1, was higher in the Avastin treated arms than the chemotherapy arms (27.4% vs. 20.9%). [See Dosage and Administration (2.4).] Neutropenia and Infection The incidences of neutropenia and febrile neutropenia are increased in patients receiving Avastin plus chemotherapy compared to chemotherapy alone. In Study 1, the incidence of Grade 3 or 4 neutropenia was increased in mCRC patients receiving IFL plus Avastin (21%) compared to patients receiving IFL alone (14%). In Study 4, the incidence of Grade 4 neutropenia was increased in NSCLC patients receiving paclitaxel/carboplatin (PC) plus Avastin (26.2%) compared with patients

Proteinuria Grade 3-4 proteinuria ranged from 0.7 to 7.4% in Studies 1, 2, 4 and 7. The overall incidence of proteinuria (all grades) was only adequately assessed in Study 7, in which the incidence was 20%. Median onset of proteinuria was 5.6 months (range 15 days to 37 months) after initiation of Avastin. Median time to resolution was 6.1 months (95% CI 2.8 months, 11.3 months). Proteinuria did not resolve in 40% of patients after median follow up of 11.2 months and required permanent discontinuation of Avastin in 30% of the patients who developed proteinuria (Study 7). [See Warnings and Precautions (5.8).]

Ovarian Failure The incidence of new cases of ovarian failure (defined as amenorrhoea lasting 3 or more months, FSH level ≥ 30 mIU/mL and a negative serum β-HCG pregnancy test) was prospectively evaluated in a subset of 179 women receiving mFOLFOX chemotherapy alone (n = 84) or with Avastin (n = 95). New cases of ovarian failure were identified in 34% (32/95) of women receiving Avastin in combination with chemotherapy compared with 2% (2/84) of women receiving chemotherapy alone [relative risk of 14 (95% CI 4, 53)]. After discontinuation of Avastin treatment, recovery of ovarian function at all time points during the post-treatment period was demonstrated in 22% (7/32) of the Avastin-treated women. Recovery of ovarian function is defined as resumption of menses, a positive serum β-HCG pregnancy test, or a FSH level < 30 mIU/mL during the post-treatment period. Long term effects of Avastin exposure on fertility are unknown. [See Warnings and Precautions (5.10), Use in Specific Populations (8.6).] Metastatic Colorectal Cancer (mCRC) The data in Table 1 and Table 2 were obtained in Study 1, a randomized, double-blind, controlled trial comparing chemotherapy plus Avastin with chemotherapy plus placebo. Avastin was administered at 5 mg/kg every 2 weeks. All Grade 3–4 adverse events and selected Grade 1–2 adverse events (hypertension, proteinuria, thromboembolic events) were collected in the entire study population. Severe and life-threatening (Grade 3–4) adverse events, which occurred at a higher incidence ( ≥ 2%) in patients receiving bolus-IFL plus Avastin as compared to bolus-IFL plus placebo, are presented in Table 1. Table 1 NCI-CTC Grade 3−4 Adverse Events in Study 1 (Occurring at Higher Incidence [ ≥ 2 %] Avastin vs. Control))

NCI-CTC Grade 3-4 Events Body as a Whole Asthenia Abdominal Pain Pain Cardiovascular Hypertension Deep Vein Thrombosis Intra-Abdominal Thrombosis Syncope Digestive Diarrhea Constipation Hemic/Lymphatic Leukopenia Neutropeniaa a

Arm 1 IFL+ + Placebo (n = 396) 74%

Arm 2 IFL+ + Avastin (n = 392) 87%

7% 5% 5%

10% 8% 8%

2% 5% 1% 1%

12% 9% 3% 3%

25% 2%

34% 4%

31% 14%

37% 21%

Central laboratories were collected on Days 1 and 21 of each cycle. Neutrophil counts are available in 303 patients in Arm 1 and 276 in Arm 2.

Grade 1–4 adverse events which occurred at a higher incidence ( ≥ 5%) in patients receiving bolus-IFL plus Avastin as compared to the bolus-IFL plus placebo arm are presented in Table 2. Grade 1–4 adverse events were collected


AVASTIN® (bevacizumab)

AVASTIN® (bevacizumab)

for the first approximately 100 patients in each of the three treatment arms who were enrolled until enrollment in Arm 3 (5-FU/LV + Avastin) was discontinued. Table 2 NCI-CTC Grade 1-4 Adverse Events in Study 1 (Occurring at Higher Incidence [≥ 5%] in IFL + Avastin vs. IFL)

Table 3 NCI-CTC Grades 1−5 Adverse Events in Study 7 (Occurring at Higher Incidence [≥ 5%] in IFN-α + Avastin vs. IFN-α + Placebo) System Organ Class/ IFN-α + Placebo (n = 304) Preferred terma Gastrointestinal disorders Diarrhea 16% General disorders and administration site conditions Fatigue 27% Investigations Weight decreased 15% Metabolism and nutrition disorders Anorexia 31% Musculoskeletal and connective tissue disorders Myalgia 14% Back pain 6% Nervous system disorders Headache 16% Renal and urinary disorders Proteinuria 3% Respiratory, thoracic and mediastinal disorders Epistaxis 4% Dysphonia 0% Vascular disorders Hypertension 9%

Arm 1 Arm 2 Arm 3 IFL + Placebo IFL + Avastin 5-FU/LV + Avastin (n = 98) (n = 102) (n = 109) Body as a Whole Pain Abdominal Pain Headache Cardiovascular Hypertension Hypotension Deep Vein Thrombosis Digestive Vomiting Anorexia Constipation Stomatitis Dyspepsia GI Hemorrhage Weight Loss Dry Mouth Colitis Hemic/Lymphatic Thrombocytopenia Nervous Dizziness Respiratory Upper Respiratory Infection Epistaxis Dyspnea Voice Alteration Skin/Appendages Alopecia Skin Ulcer Special Senses Taste Disorder Urogenital Proteinuria

55% 55% 19%

61% 61% 26%

62% 50% 26%

14% 7% 3%

23% 15% 9%

34% 7% 6%

47% 30% 29% 18% 15% 6% 10% 2% 1%

52% 43% 40% 32% 24% 24% 15% 7% 6%

47% 35% 29% 30% 17% 19% 16% 4% 1%

0%

5%

5%

20%

26%

19%

39% 10% 15% 2%

47% 35% 26% 9%

40% 32% 25% 6%

26% 1%

32% 6%

6% 6%

9%

14%

21%

24%

36%

36%

Avastin in Combination with FOLFOX4 in Second-line mCRC Only Grade 3-5 non-hematologic and Grade 4–5 hematologic adverse events related to treatment were collected in Study 2. The most frequent adverse events (selected Grade 3–5 non-hematologic and Grade 4–5 hematologic adverse events) occurring at a higher incidence (≥2%) in 287 patients receiving FOLFOX4 plus Avastin compared to 285 patients receiving FOLFOX4 alone were fatigue (19% vs. 13%), diarrhea (18% vs. 13%), sensory neuropathy (17% vs. 9%), nausea (12% vs. 5%), vomiting (11% vs. 4%), dehydration (10% vs. 5%), hypertension (9% vs. 2%), abdominal pain (8% vs. 5%), hemorrhage (5% vs. 1%), other neurological (5% vs. 3%), ileus (4% vs. 1%) and headache (3% vs. 0%). These data are likely to under-estimate the true adverse event rates due to the reporting mechanisms used in Study 2. Unresectable Non-Squamous Non-Small Cell Lung Cancer (NSCLC) Only Grade 3-5 non-hematologic and Grade 4-5 hematologic adverse events were collected in Study 4. Grade 3–5 non-hematologic and Grade 4–5 hematologic adverse events (occurring at a higher incidence (≥2%) in 427 patients receiving PC plus Avastin compared with 441 patients receiving PC alone were neutropenia (27% vs. 17%), fatigue (16% vs. 13%), hypertension (8% vs. 0.7%), infection without neutropenia (7% vs. 3%), venous thrombus/embolism (5% vs. 3%), febrile neutropenia (5% vs. 2%), pneumonitis/ pulmonary infiltrates (5% vs. 3%), infection with Grade 3 or 4 neutropenia (4% vs. 2%), hyponatremia (4% vs. 1%), headache (3% vs. 1%) and proteinuria (3% vs. 0%). Glioblastoma All adverse events were collected in 163 patients enrolled in Study 5 who either received Avastin alone or Avastin plus irinotecan. All patients received prior radiotherapy and temozolomide. Avastin was administered at 10 mg/kg every 2 weeks alone or in combination with irinotecan. Avastin was discontinued due to adverse events in 4.8% of patients treated with Avastin alone. In patients receiving Avastin alone (N = 84), the most frequently reported adverse events of any grade were infection (55%), fatigue (45%), headache (37%), hypertension (30%), epistaxis (19%) and diarrhea (21%). Of these, the incidence of Grade ≥ 3 adverse events was infection (10%), fatigue (4%), headache (4%), hypertension (8%) and diarrhea (1%). Two deaths on study were possibly related to Avastin: one retroperitoneal hemorrhage and one neutropenic infection. In patients receiving Avastin alone or Avastin plus irinotecan (N = 163), the incidence of Avastin-related adverse events (Grade 1–4) were bleeding/ hemorrhage (40%), epistaxis (26%), CNS hemorrhage (5%), hypertension (32%), venous thromboembolic event (8%), arterial thromboembolic event (6%), wound-healing complications (6%), proteinuria (4%), gastrointestinal perforation (2%), and RPLS (1%). The incidence of Grade 3–5 events in these 163 patients were bleeding/hemorrhage (2%), CNS hemorrhage (1%), hypertension (5%), venous thromboembolic event (7%), arterial thromboembolic event (3%), wound-healing complications (3%), proteinuria (1%), and gastrointestinal perforation (2%). Metastatic Renal Cell Carcinoma (mRCC) All grade adverse events were collected in Study 7. Grade 3–5 adverse events occurring at a higher incidence ( ≥ 2%) in 337 patients receiving interferon alfa (IFN-α) plus Avastin compared to 304 patients receiving IFN-α plus placebo arm were fatigue (13% vs. 8%), asthenia (10% vs. 7%), proteinuria (7% vs. 0%), hypertension (6% vs. 1%; including hypertension and hypertensive crisis), and hemorrhage (3% vs. 0.3%; including epistaxis, small intestinal hemorrhage, aneurysm ruptured, gastric ulcer hemorrhage, gingival bleeding, haemoptysis, hemorrhage intracranial, large intestinal hemorrhage, respiratory tract hemorrhage, and traumatic hematoma). Grade 1–5 adverse events occurring at a higher incidence ( ≥ 5%) in patients receiving IFN-α plus Avastin compared to the IFN-α plus placebo arm are presented in Table 3.

AVASTIN® (bevacizumab)

IFN-α + Avastin (n = 337) 21% 33% 20% 36% 19% 12% 24% 20% 27% 5% 28%

a

Adverse events were encoded using MedDRA, Version 10.1.

The following adverse events were reported at a 5-fold greater incidence in the IFN-α plus Avastin arm compared to IFN-α alone and not represented in Table 3: gingival bleeding (13 patients vs. 1 patient); rhinitis (9 vs.0 ); blurred vision (8 vs. 0); gingivitis (8 vs. 1); gastroesophageal reflux disease (8 vs.1 ); tinnitus (7 vs. 1); tooth abscess (7 vs.0); mouth ulceration (6 vs. 0); acne (5 vs. 0); deafness (5 vs. 0); gastritis (5 vs. 0); gingival pain (5 vs. 0) and pulmonary embolism (5 vs. 1). 6.2 Immunogenicity As with all therapeutic proteins, there is a potential for immunogenicity. The incidence of antibody development in patients receiving Avastin has not been adequately determined because the assay sensitivity was inadequate to reliably detect lower titers. Enzyme-linked immunosorbent assays (ELISAs) were performed on sera from approximately 500 patients treated with Avastin, primarily in combination with chemotherapy. High titer human anti-Avastin antibodies were not detected. Immunogenicity data are highly dependent on the sensitivity and specificity of the assay. Additionally, the observed incidence of antibody positivity in an assay may be influenced by several factors, including sample handling, timing of sample collection, concomitant medications, and underlying disease. For these reasons, comparison of the incidence of antibodies to Avastin with the incidence of antibodies to other products may be misleading. 6.3 Postmarketing Experience The following adverse reactions have been identified during post-approval use of Avastin. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Body as a Whole: Polyserositis Cardiovascular: Pulmonary hypertension, RPLS, Mesenteric venous occlusion Eye disorders (from unapproved intravitreal use for treatment of various ocular disorders): Permanent loss of vision; Endophthalmitis (infectious and sterile); Intraocular inflammation; Retinal detachment; Increased intraocular pressure; Hemorrhage including conjunctival, vitreous hemorrhage or retinal hemorrhage; Vitreous floaters; Ocular hyperemia; Ocular pain or discomfort Gastrointestinal: Gastrointestinal ulcer, Intestinal necrosis, Anastomotic ulceration Hemic and lymphatic: Pancytopenia Hepatobiliary disorders: Gallbladder perforation Musculoskeletal: Osteonecrosis of the jaw Renal: Renal thrombotic microangiopathy (manifested as severe proteinuria) Respiratory: Nasal septum perforation, dysphonia Systemic Events (from unapproved intravitreal use for treatment of various ocular disorders): Arterial thromboembolic events, Hypertension, Gastrointestinal perforation, Hemorrhage

Because of the observed teratogenic effects of bevacizumab in animals and of other inhibitors of angiogenesis in humans, bevacizumab should be used during pregnancy only if the potential benefit to the pregnant woman justifies the potential risk to the fetus. 8.3 Nursing Mothers It is not known whether Avastin is secreted in human milk. Human IgG is excreted in human milk, but published data suggest that breast milk antibodies do not enter the neonatal and infant circulation in substantial amounts. Because many drugs are secreted in human milk and because of the potential for serious adverse reactions in nursing infants from bevacizumab, a decision should be made whether to discontinue nursing or discontinue drug, taking into account the half-life of the bevacizumab (approximately 20 days [range 11–50 days]) and the importance of the drug to the mother. [See Clinical Pharmacology (12.3).] 8.4 Pediatric Use The safety, effectiveness and pharmacokinetic profile of Avastin in pediatric patients have not been established. Antitumor activity was not observed among eight children with relapsed glioblastoma treated with bevacizumab and irinotecan. There is insufficient information to determine the safety and efficacy of Avastin in children with glioblastoma. Juvenile cynomolgus monkeys with open growth plates exhibited physeal dysplasia following 4 to 26 weeks exposure at 0.4 to 20 times the recommended human dose (based on mg/kg and exposure). The incidence and severity of physeal dysplasia were dose-related and were partially reversible upon cessation of treatment. 8.5 Geriatric Use In Study 1, severe adverse events that occurred at a higher incidence ( ≥ 2%) in patients aged ≥65 years as compared to younger patients were asthenia, sepsis, deep thrombophlebitis, hypertension, hypotension, myocardial infarction, congestive heart failure, diarrhea, constipation, anorexia, leukopenia, anemia, dehydration, hypokalemia, and hyponatremia. The effect of Avastin on overall survival was similar in elderly patients as compared to younger patients. In Study 2, patients aged ≥65 years receiving Avastin plus FOLFOX4 had a greater relative risk as compared to younger patients for the following adverse events: nausea, emesis, ileus, and fatigue. In Study 4, patients aged ≥65 years receiving carboplatin, paclitaxel, and Avastin had a greater relative risk for proteinuria as compared to younger patients. [See Warnings and Precautions (5.8).] Of the 742 patients enrolled in Genentech-sponsored clinical studies in which all adverse events were captured, 212 (29%) were age 65 or older and 43 (6%) were age 75 or older. Adverse events of any severity that occurred at a higher incidence in the elderly as compared to younger patients, in addition to those described above, were dyspepsia, gastrointestinal hemorrhage, edema, epistaxis, increased cough, and voice alteration. In an exploratory, pooled analysis of 1745 patients treated in five randomized, controlled studies, there were 618 (35%) patients aged ≥65 years and 1127 patients <65 years of age. The overall incidence of arterial thromboembolic events was increased in all patients receiving Avastin with chemotherapy as compared to those receiving chemotherapy alone, regardless of age. However, the increase in arterial thromboembolic events incidence was greater in patients aged ≥65 years (8.5% vs. 2.9%) as compared to those <65 years (2.1% vs. 1.4%). [See Warnings and Precautions (5.5).] 8.6 Females of Reproductive Potential Avastin increases the risk of ovarian failure and may impair fertility. Inform females of reproductive potential of the risk of ovarian failure prior to starting treatment with Avastin. Long term effects of Avastin exposure on fertility are unknown. In a prospectively designed substudy of 179 premenopausal women randomized to receive chemotherapy with or without Avastin, the incidence of ovarian failure was higher in the Avastin arm (34%) compared to the control arm (2%). After discontinuation of Avastin and chemotherapy, recovery of ovarian function occurred in 22% (7/32) of these Avastin-treated patients. [See Warnings and Precautions (5.10), Adverse Reactions (6.1).] 10 OVERDOSAGE The highest dose tested in humans (20 mg/kg IV) was associated with headache in nine of 16 patients and with severe headache in three of 16 patients.

7 DRUG INTERACTIONS A drug interaction study was performed in which irinotecan was administered as part of the FOLFIRI regimen with or without Avastin. The results demonstrated no significant effect of bevacizumab on the pharmacokinetics of irinotecan or its active metabolite SN38. In a randomized study in 99 patients with NSCLC, based on limited data, there did not appear to be a difference in the mean exposure of either carboplatin or paclitaxel when each was administered alone or in combination with Avastin. However, 3 of the 8 patients receiving Avastin plus paclitaxel/carboplatin had substantially lower paclitaxel exposure after four cycles of treatment (at Day 63) than those at Day 0, while patients receiving paclitaxel/carboplatin without Avastin had a greater paclitaxel exposure at Day 63 than at Day 0. In Study 7, there was no difference in the mean exposure of interferon alfa administered in combination with Avastin when compared to interferon alfa alone. 8 USE IN SPECIFIC POPULATIONS 8.1 Pregnancy Pregnancy Category C There are no adequate or well controlled studies of bevacizumab in pregnant women. While it is not known if bevacizumab crosses the placenta, human IgG is known to cross the placenta Reproduction studies in rabbits treated with approximately 1 to 12 times the recommended human dose of bevacizumab demonstrated teratogenicity, including an increased incidence of specific gross and skeletal fetal alterations. Adverse fetal outcomes were observed at all doses tested. Other observed effects included decreases in maternal and fetal body weights and an increased number of fetal resorptions. [See Nonclinical Toxicology (13.3).]

Avastin® (bevacizumab) Manufactured by: Genentech, Inc. A Member of the Roche Group 1 DNA Way South San Francisco, CA 94080-4990

06/12 AVA0000759203 10127309 Initial U.S.Approval: February 2004 Code Revision Date: May 2012 Avastin® is a registered trademark of Genentech, Inc. © 2012 Genentech, Inc.


To confront a common threat across approved indications...

Think Avastin

Clinically meaningful activity in 4 distinct tumor types1

Because anti-angiogenesis matters Avastin is designed to directly inhibit the VEGF ligand to specifically inhibit angiogenesis1*

VEGF=vascular endothelial growth factor. *The mechanism of action of Avastin has been elucidated primarily in preclinical models. Its clinical significance is unknown.

Indications

Most common adverse events

Avastin is indicated for the treatment of metastatic renal cell carcinoma in combination with interferon alfa. Avastin is indicated for the treatment of glioblastoma as a single agent for adult patients with progressive disease following prior therapy. The effectiveness of Avastin in glioblastoma is based on an improvement in objective response rate. There are no data demonstrating an improvement in disease-related symptoms or increased survival with Avastin. Avastin is indicated for the first-line treatment of unresectable, locally advanced, recurrent or metastatic non–squamous non–small cell lung cancer in combination with carboplatin and paclitaxel. Avastin is indicated for the first- or second-line treatment of patients with metastatic carcinoma of the colon or rectum in combination with intravenous 5-fluorouracil– based chemotherapy.

Most common adverse reactions observed in Avastin patients at a rate >10% and at least twice the control arm rate were — Epistaxis — Proteinuria — Lacrimation disorder — Headache — Taste alteration — Back pain — Hypertension — Dry skin — Exfoliative dermatitis — Rhinitis — Rectal hemorrhage Across all studies, Avastin was discontinued in 8.4% to 21% of patients because of adverse reactions

Pregnancy warning Avastin may impair fertility Based on animal data, Avastin may cause fetal harm Advise patients of the potential risk to the fetus during and following Avastin and the need to continue adequate contraception for at least 6 months following the last dose of Avastin For nursing mothers, discontinue nursing or Avastin, taking into account the importance of Avastin to the mother In mRCC, the most common grade 3–5 adverse events in AVOREN, occurring at a ≥2% higher incidence in Avastin-treated patients vs controls, were fatigue (13% vs 8%), asthenia (10% vs 7%), proteinuria (7% vs 0%), hypertension (6% vs 1%), and hemorrhage (3% vs 0.3%) In GBM Study AVF3708g, in patients receiving Avastin alone, the most frequently reported adverse events were infection (55%), fatigue (45%), headache (37%), hypertension (30%), epistaxis (19%), and diarrhea (21%). Of these, the incidence of grade ≥3 adverse events was infection (10%), fatigue (4%), headache (4%), hypertension (8%), and diarrhea (1%). Two deaths were possibly related to Avastin: 1 retroperitoneal hemorrhage and 1 neutropenic infection In GBM patients receiving Avastin alone or Avastin plus irinotecan,† the incidences of Avastin-related adverse events (grade 1–4) were bleeding/hemorrhage (40%), epistaxis (26%), CNS hemorrhage (5%), hypertension (32%), venous thromboembolic events (8%), arterial thromboembolic events (6%), wound healing complications (6%), proteinuria (4%), GI perforation (2%), and RPLS (1%). The incidences of grade 3–5 events in these 163 patients were bleeding/hemorrhage (2%), CNS hemorrhage (1%), hypertension (5%), venous thromboembolic events (7%), arterial thromboembolic events (3%), wound healing complications (3%), proteinuria (1%), and GI perforation (2%). Intracranial hemorrhage occurred in 8 of 163 patients; 2 patients had grade 3–4 hemorrhage In NSCLC, grade 3–5 (nonhematologic) and grade 4–5 (hematologic) adverse events in Study E4599 occurring at a ≥2% higher incidence in Avastin-treated patients vs controls were neutropenia (27% vs 17%), fatigue (16% vs 13%), hypertension (8% vs 0.7%), infection without neutropenia (7% vs 3%), venous thrombus/embolism (5% vs 3%), febrile neutropenia (5% vs 2%), pneumonitis/pulmonary infiltrates (5% vs 3%), infection with grade 3 or 4 neutropenia (4% vs 2%), hyponatremia (4% vs 1%), headache (3% vs 1%), and proteinuria (3% vs 0%) In first-line MCRC, the most common grade 3–4 events in Study 2107, which occurred at a ≥2% higher incidence in the Avastin plus IFL vs IFL groups, were asthenia (10% vs 7%), abdominal pain (8% vs 5%), pain (8% vs 5%), hypertension (12% vs 2%), deep vein thrombosis (9% vs 5%), intra-abdominal thrombosis (3% vs 1%), syncope (3% vs 1%), diarrhea (34% vs 25%), constipation (4% vs 2%), leukopenia (37% vs 31%), and neutropenia (21% vs 14%) In second-line MCRC, the most common grade 3–5 (nonhematologic) and 4–5 (hematologic) events in Study E3200, which occurred at a higher incidence (≥2%) in the Avastin plus FOLFOX4 vs FOLFOX4 groups, were diarrhea (18% vs 13%), nausea (12% vs 5%), vomiting (11% vs 4%), dehydration (10% vs 5%), ileus (4% vs 1%), neuropathy–sensory (17% vs 9%), neurologic–other (5% vs 3%), fatigue (19% vs 13%), abdominal pain (8% vs 5%), headache (3% vs 0%), hypertension (9% vs 2%), and hemorrhage (5% vs 1%)

Boxed WARNINGS Gastrointestinal (GI) perforation — Serious and sometimes fatal GI perforation occurs at a higher incidence in Avastintreated patients compared to controls — The incidences of GI perforation ranged from 0.3% to 2.4% across clinical studies — Discontinue Avastin in patients with GI perforation Surgery and wound healing complications — The incidence of wound healing and surgical complications, including serious and fatal complications, is increased in Avastin-treated patients — Do not initiate Avastin for at least 28 days after surgery and until the surgical wound is fully healed. The appropriate interval between termination of Avastin and subsequent elective surgery required to reduce the risks of impaired wound healing/wound dehiscence has not been determined — Discontinue Avastin at least 28 days prior to elective surgery and in patients with wound healing complications requiring medical intervention Hemorrhage — Severe or fatal hemorrhage, including hemoptysis, GI bleeding, hematemesis, central nervous system hemorrhage, epistaxis, and vaginal bleeding, occurred up to 5-fold more frequently in patients receiving Avastin. Across indications, the incidence of grade ≥3 hemorrhagic events among patients receiving Avastin ranged from 1.2% to 4.6% — Do not administer Avastin to patients with serious hemorrhage or recent hemoptysis (≥1/2 tsp of red blood) — Discontinue Avastin in patients with serious hemorrhage (ie, requiring medical intervention)

Additional serious adverse events Additional serious and sometimes fatal adverse events with increased incidence in the Avastin-treated arm vs control included — Non-GI fistula formation (≤0.3%) — Arterial thromboembolic events (grade ≥3, 2.6%) — Proteinuria (nephrotic syndrome, <1%) Additional serious adverse events with increased incidence in the Avastin-treated arm vs control included — Hypertension (grade 3–4, 5%–18%) — Reversible posterior leukoencephalopathy syndrome (RPLS) (<0.1%) Infusion reactions with the first dose of Avastin were uncommon (<3%), and severe reactions occurred in 0.2% of patients Inform females of reproductive potential of the risk of ovarian failure prior to starting treatment with Avastin †

Avastin is not approved for use in combination with irinotecan.

Please see accompanying brief summary of Prescribing Information, including Boxed WARNINGS, for additional important safety information. Reference: 1. Avastin Prescribing Information. Genentech, Inc. December 2011.

©2012 Genentech USA, Inc.

All rights reserved.

AVA0000488301

Printed in USA.

(01/12)

www.avastin.com


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