uMB f ounders week 2021
David J. Ramsay Entrepreneur of the Year Virtual Presentation Tuesday, Oct. 26, 2021 | 4:30 p.m.
Vincent Njar, PhD School of Medicine Drug Discovery and Development from Academia: The Quest for Novel and Efficacious Small-Molecule Anti-Cancer Drugs Drug Discovery: Ingenuity and Serendipity, or Is It the Other Way Around?
Drug Discovery and Development from Academia: The Quest for Novel and Efficacious Small-Molecule Anti-Cancer Drugs Drug Discovery: Ingenuity and Serendipity, or Is It the Other Way Around?
In Dr. Njar’s effort to discover potent and specific inhibitors of CYP17, the key enzyme that catalyzes the biosynthesis of androgens from progestins, VN/124-1 (now called Galeterone) was identified as a selective development candidate that modulates multiple targets in the androgen receptor signaling pathway. Galeterone and its analogs were later shown to inhibit Mnk1/2-eIF4E signaling via induction of ubiquitin-proteasome degradation of Mnk1/2 proteins. The Galeterone technology was licensed to Tokai Pharmaceuticals, Inc., which advanced it to Phase 3 clinical trials in men with castration-resistant prostate cancer. LTN Pharmaceuticals, Inc. is continuing its clinical development. In addition to another clinical trial in pancreatic cancer, the next-generation Galeterone analogs, which are an order of magnitude more potent than Galeterone, are in development. Dr. Njar’s second technology concerns the invention and development of potent inhibitors of CYP26, the major enzyme responsible for the metabolism of all-trans retinoic acid. These inhibitors also are called retinoic acid metabolism blocking agents (RAMBAs). RAMBAs also were shown to possess multiple desirable anticancer activities, including modulation of Mnk1/2-eIF4E and androgen receptor signaling pathways. To develop the RAMBAs technology, UMB’s New Ventures Initiative and Dr. Njar co-founded Isoprene Pharmaceuticals, Inc., which recently was awarded a two-year, $2 million Small Business Innovation Research grant by the National Cancer Institute for the advanced/clinical development of the lead compound VNLG-152R for the treatment of triple negative breast cancer.
Vincent Njar, PhD Professor, Department of Pharmacology School of Medicine Dr. Njar is a leading medicinal chemist and oncopharmacologist who has made significant discoveries in the development of novel therapeutics for breast, prostate, and pancreatic cancer. He is head of the medicinal chemistry section in the Center for Biomolecular Therapeutics at the Institute for Bioscience and Biotechnology Research at the University of Maryland School of Medicine (UMSOM). He is an inaugural Distinguished University Professor, the highest appointment bestowed on a faculty member at UMB. Dr. Njar’s significant contributions to science include the design, discovery, and clinical translation of the CYP17 inhibitor Galeterone for the treatment of cancer. Because of its clinical efficacy, Galeterone and subsequent variants continue to be developed as novel therapeutics. Dr. Njar’s most recent National Institutes of Health R01 grant focuses on the development of next-generation Galeterone analogs for prostate cancer. Dr. Njar founded two startup companies — Terpene Pharmaceuticals, LLC and Isoprene Pharmaceuticals, Inc. (IPI), a cancer therapeutic company — and has served as president and board member of both. IPI recently was awarded a two-year, $2 million grant from the National Cancer Institute for a translational project to develop a novel therapeutic for triple negative breast cancer. Dr. Njar has secured 34 issued patents, more than 30 pending patents, and numerous active intellectual property and licensing activities at UMB. He is the lead inventor of these technologies. He obtained his PhD in organic chemistry from University College London in the United Kingdom. Except for a brief stint at Thomas Jefferson University in Philadelphia, he has worked at UMSOM for almost 20 years.
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