Top 7 Drugs For Treating Lung Cancer-Approved by FDA

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Top 7 Drugs For Treating Lung Cancer-Approved by FDA

Top 7 Drugs For Treating Lung Cancer-Approved by FDA...................................................................... 1 What Is Lung Cancer?...................................................................................................................2 WhatAre The Types Of Lung Cancer?...........................................................................................3 WhatAre The Symptoms WhenYou Have Lung Cancer?..............................................................3 How Can I Know Whether I Have Lung Cancer?........................................................................... 5 What Is Stages Of My Lung Cancer?.............................................................................................6 (1) Stages of Non-Small Cell Lung Cancer............................................................................. 6 (2) Stages Of Small Cell Lung Cancer....................................................................................7 Why Do I Have Lung Cancer? ...................................................................................................... 7 HowTo Treat Your Lung Cancer? ............................................................................................... 10 ❶AZD-3759(CAS:1626387-80-1)...................................................................................... 11 ❷ Gefitinib(CAS:184475-35-2)............................................................................................ 11 ❸ AZD-9291(CAS:1421373-65-0)...................................................................................... 12 ❹ Dacomitinib(CAS:1110813-31-4)..................................................................................... 12 ❺ Ceritinib(CAS:1032900-25-6).......................................................................................... 13 ❻Afatinib(CAS:439081-18-2)............................................................................................. 13 ❼ Erlotinib(CAS:183321-74-6)............................................................................................ 14 Reference........................................................................................................................... 14

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What Is Lung Cancer?

Cancer can start any place in the body. Cancer that starts in the lung is called lung cancer. It starts when cells in the lung grow out of control and crowd out normal cells. This makes it hard for the body to work the way it should.

Cancer cells can spread to other parts of the body. Cancer cells in the lung can sometimes travel to the brain and grow there. When cancer cells do this, it’s called metastasis. To doctors, the cancer cells in the new place look just like the ones from the lung.

Cancer is always named for the place where it starts. So when lung cancer spreads to the brain (or any other place), it’s still called lung cancer. It’s not called brain cancer unless it starts from cells in the brain.

Noted: The lungs are 2 sponge-like organs found in the chest. The right lung has 3 parts called lobes. The left lung has 2 lobes. The lungs bring air in and out of the body. They take in oxygen and get rid of carbon dioxide, a waste product.

The windpipe, or trachea, brings air down into the lungs. It splits into 2 tubes called bronchi (one tube is called a bronchus).

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What Are The Types Of Lung Cancer?

Cancer that begins in the lungs is called primary lung cancer. Cancer that spreads to the lungs from another place in the body is known as secondary lung cancer. This page is about primary lung cancer.

There are two main forms of primary lung cancer. These are classified by the type of cells in which the cancer starts growing. They are: Non-small-cell lung cancer(NSCLC) — the most common form, accounting for more than 87% of cases. It can be one of three types: squamous cell carcinoma, adenocarcinoma or large-cell carcinoma.

Small-cell lung cancer(SCLC) — a less common form that usually spreads faster than non-small-cell lung cancer.

The type of lung cancer you have determines which treatments are recommended.

What Are The Symptoms When You Have Lung Cancer?

People with lung cancer may not have any symptoms until a later stage. If symptoms do appear, they can resemble those of a respiratory infection.

Some possible symptomsTrusted Source include: changes to a person’s voice, such as hoarseness frequent chest infections, such as bronchitis or pneumonia swelling in the lymph nodes in the middle of the chest a lingering cough that may start to get worse chest pain 3

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shortness of breath and wheezing In time, a person may also experience more severe symptoms, such as: severe chest pain bone pain and bone fractures headaches coughing up blood blood clots appetite loss and weight loss fatigue

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How Can I Know Whether I Have Lung Cancer?

The doctor asks you questions about your health and does a physical exam. If signs are pointing to lung cancer, more tests will be done.

Here are some of the tests you may need: Chest x-ray: This is often the first test done to look for spots on your lungs. If a change is seen, you’ll need more tests.

CT scan: This is also called a CAT scan. It’s a special kind of x-ray that takes detailed pictures of your insides. CT scans can also be used to help do a biopsy (see below).

PET scan: In this test, you are given a type of sugar that can be seen inside your body with a special camera. If there’s cancer, the sugar shows up as “hot spots” where the cancer is found. It can help when your doctor thinks the cancer has spread, but doesn’t know where.

Bronchoscopy: A thin, lighted, flexible tube is passed through your mouth into the bronchi. The doctor can look through the tube to find tumors. The tube also can be used to do a biopsy.

Blood tests: Blood tests are not used to find lung cancer, but they are done to tell the doctor more about your health.

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What Is Stages Of My Lung Cancer?

If you have non-small cell lung cancer, the doctor will want to find out how far it has spread. This is called staging. You may have heard other people say that their cancer was “stage 2” or “stage 3.” Your doctor will want to find out the stage of your cancer to help decide what type of treatment is best for you.

The stage describes the spread of the cancer through the lung. It also tells if the cancer has spread to nearby organs or to organs farther away.

Your stage can be stage 1, 2, 3, or 4. The lower the number, the less the cancer has spread. A higher number, such as stage 4, means a more serious cancer that has spread outside your lungs. Be sure to ask the doctor about your cancer’s stage and what it means.

(1) Stages of Non-Small Cell Lung Cancer Healthcare professionals typically use tumor size and spread to describe the stages of non-small cell lung cancer, as follows: ♦ Occult, or hidden: The cancer does not show up on imaging scans, but cancerous cells might appear in the phlegm or mucus. ♦ Stage 0: There are abnormal cells only in the top layers of cells lining the airways. ♦ Stage 1: A tumor is present in the lung, but it is 4 centimeters (cm) or under and has not spread to other parts of the body. ♦ Stage 2: The tumor is 7 cm or under and might have spread to nearby tissues and lymph nodes. ♦ Stage 3: The cancer has spread to lymph nodes and reached other parts of the lung and surrounding area. ♦ Stage 4: The cancer has spread to distant body parts, such as the bones or brain.

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(2) Stages Of Small Cell Lung Cancer Small cell lung cancer has its own categories. The stages are known as limited and extensive, and they refer to whether the cancer has spread within or outside the lungs.

In the limited stage, the cancer affects only one side of the chest, though it might already be present in some surrounding lymph nodes. Around one-third of people with this type find out that they have cancer when it is in the limited stage. Healthcare professionals can treat it with radiation therapy as a single area.

In the extensive stage, the cancer has spread beyond the one side of the chest. It may affect the other lung or other parts of the body. Around two-thirds of people with small cell lung cancer find out that they have it when it is already in the extensive stage.

Why Do I Have Lung Cancer?

Cancer develops after genetic damage to DNA and epigenetic changes. Those changes affect the cell’s normal functions, including cell proliferation, programmed cell death (apoptosis), and DNA repair.

As more damage accumulates, the risk for cancer increases.

These reasons lead to the lung cancer manily: ▲ Smoking Not all smokers get lung cancer, and not everyone who has lung cancer is a smoker. But there’s no doubt that smoking is the biggest risk factor, causing 9 out of 10Trusted Source lung cancers. In addition to cigarettes, cigar and pipe smoking are also linked to lung cancer. The more you smoke and the longer you smoke, the bigger your chance of developing lung cancer.

You don’t have to be a smoker to be affected. Breathing in other people’s smoke increases the risk of lung cancer. According to the Centers for Disease Control and Prevention CDC)Trusted Source, secondhand smoke is responsible for about 7,300 lung cancer deaths each year in the United States.

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Tobacco products contain more than 7,000 chemicals, and at least 70 are known to cause cancer.

When you inhale tobacco smoke, this mixture of chemicals is delivered directly to your lungs, where it immediately starts causing damage.

The lungs can usually repair damage at first, but the continued effect on lung tissue becomes harder to manage. That’s when damaged cells can mutate and grow out of control. The chemicals you inhale also enter your bloodstream and are carried throughout your body, increasing the risk of other types of cancer. Former smokers are still at risk of developing lung cancer, but quitting can lower that risk considerably. Within 10 years of quitting, the risk of dying from lung cancer drops by half. ▲ Radon gas Radon is a colorless and odorless gas generated by the breakdown of radioactive radium, which in turn is the decay product of uranium, found in the Earth’s crust. The radiation decay products ionize genetic material, causing mutations that sometimes become cancerous.

Radon is the second most-common cause of lung cancer in the US,causing about 21,000 deaths each year.The risk increases 8–16% for every 100 Bq/m³ increase in the radon concentration.Radon gas levels vary by locality and the composition of the underlying soil and rocks. About one in 15 homes in the US have radon levels above the recommended guideline of 4 picocuries per liter (pCi/l) (148 Bq/m³). ▲ Asbestos Asbestos can cause a variety of lung diseases such as lung cancer.

Tobacco smoking and asbestos both have synergistic effects on the development of lung cancer.In smokers who work with asbestos, the risk of lung cancer is increased 45-fold compared to the general population.Asbestos can also cause cancer of the pleura, called mesothelioma – which actually is different from lung cancer. ▲ Air pollution

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Outdoor air pollutants, especially chemicals released from the burning of fossil fuels, increase the risk of lung cancer.Fine particulates (PM2.5) and sulfate aerosols, which may be released in traffic exhaust fumes, are associated with a slightly-increased risk.For nitrogen dioxide, an incremental increase of 10 parts per billion increases the risk of lung cancer by 14%.Outdoor air pollution is estimated to cause 1–2% of lung cancers.

Tentative evidence supports an increased risk of lung cancer from indoor air pollution in relation to the burning of wood, charcoal, dung, or crop residue for cooking and heating.Women who are exposed to indoor coal smoke have roughly twice the risk, and many of the by-products of burning biomass are known or suspected carcinogens.This risk affects about 2.4 billion people worldwide,and it is believed to result in 1.5% of lung cancer deaths. ▲ Genetics About 8% of lung cancer is caused by inherited factors.In relatives of people that are diagnosed with lung cancer, the risk is doubled, likely due to a combination of genes.Polymorphisms on chromosomes 5, 6, and 15 are known to affect the risk of lung cancer.Single-nucleotide polymorphisms (SNPs) of the genes encoding the nicotinic acetylcholine receptor (nAChR) – CHRNA5, CHRNA3, and CHRNB4 – are of those associated with an increased risk of lung cancer, as well as RGS17 – a gene regulating G-protein signaling. ▲ Other reasons Numerous other substances, occupations, and environmental exposures have been linked to lung cancer. The International Agency for Research on Cancer (IARC) states that there is some “sufficient evidence” to show that the following are carcinogenic in the lungs: Some metals (aluminium production, cadmium and cadmium compounds, chromium(VI) compounds, beryllium and beryllium compounds, iron and steel founding, nickel compounds, arsenic and inorganic arsenic compounds, and underground hematite mining) Some products of combustion (incomplete combustion, coal (indoor emissions from household coal burning), coal gasification, coal-tar pitch, coke production, soot, and diesel engine exhaust) 9

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Ionizing radiation (X-ray and gamma).

Some toxic gases (methyl ether (technical grade), and bis-(chloromethyl) ether, sulfur mustard, MOPP (vincristine-prednisone-nitrogen mustard-procarbazine mixture) and fumes from painting) Rubber production and crystalline silica dust.

There is a small increase in the risk of lung cancer in people affected by systemic sclerosis.

How To Treat Your Lung Cancer?

There are many ways to treat lung cancer. Surgery and radiation are used to treat only the cancer. They do not affect the rest of the body.

Chemo drugs, targeted therapy, and immunotherapy go through the whole body. They can reach cancer cells almost anywhere in the body.

The treatment for lung cancer can include surgery, radiation, chemotherapy, targeted therapy, and immunotherapy. The treatment plan that’s best for you will depend on: The stage of the cancer The chance that a type of treatment will help Your age Other health problems you have Your feelings about the treatment and the side effects that may come with it.

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Many patients with lung cancer choose drug therapy in the early stage, because it is the most direct and simple way to control the spread of cancer cells. The following drugs are commonly used to treat lung cancer(SCLC and NSCLC):

❶ AZD-3759(CAS:1626387-80-1) AZD-3759 is a potent epidermal growth factor receptor(EGFR) inhibitor, with potential antineoplastic activity. AZD-3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR.This prevents EGFR-mediated signaling, and may lead to both induction of cell dealth and inhibition of tumor growth in EGFR-overexpressing cells.

❷ Gefitinib(CAS:184475-35-2) Gefitinib is a tyrosine kinase inhibitor used as first-line therapy to treat non-small cell lung carcinoma (NSCLC) that meets certain genetic mutation criteria.

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Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that binds to the adenosine triphosphate (ATP)-binding site of the enzyme. EGFR is often shown to be overexpressed in certain human carcinoma cells, such as lung and breast cancer cells. Overexpression leads to enhanced activation of the anti-apoptotic Ras signal transduction cascades, subsequently resulting in increased survival of cancer cells and uncontrolled cell proliferation. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. By inhibiting EGFR tyrosine kinase, the downstream signaling cascades are also inhibited, resulting in inhibited malignant cell proliferation.

❸ AZD-9291(CAS:1421373-65-0) AZD-9291 is also called Osimertinib which is a tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma.

AZD-9291 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that binds to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) that predominate in non-small cell lung cancer (NSCLC) tumours following treatment with first-line EGFR-TKIs. As a third-generation tyrosine kinase inhibitor, AZD-9291 is specific for the gate-keeper T790M mutation which increases ATP binding activity to EGFR and results in poor prognosis for late-stage disease. Furthermore, AZD-9291 has been shown to spare wild-type EGFR during therapy, thereby reducing non-specific binding and limiting toxicity.

❹ Dacomitinib(CAS:1110813-31-4) Dacomitinib is a medication used to treat non small cell lung cancer with EGFR exon 19 deletion of exon 21 L858R substitution.

Dacomitinib, designed as (2E)-N-16-4-(piperidin-1-yl) but-2-enamide, is an oral highly selective quinazalone part of the second-generation tyrosine kinase inhibitors which are characterized by the irreversible binding at the ATP domain of the epidermal growth factor receptor family kinase domains. Dacomitinib is a medication for the treatment 12

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of non-small-cell lung carcinoma (NSCLC). It is a selective and irreversible inhibitor of EGFR.

❺ Ceritinib(CAS:1032900-25-6) Ceritinib is also called LDK378 that is an antineoplastic kinase inhibitor used to treat anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) in patients with inadequate clinical response or intolerance to crizotinib.

Ceritinib is used for the treatment of adults with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) following failure (secondary to resistance or intolerance) of prior crizotinib therapy. About 4% of patients with NSCLC have a chromosomal rearrangement that generates a fusion gene between EML4 (echinoderm microtubule-associated protein-like 4) and ALK (anaplastic lymphoma kinase), which results in constitutive kinase activity that contributes to carcinogenesis and seems to drive the malignant phenotype. Ceritinib exerts its therapeutic effect by inhibiting autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells. Following treatment with crizotinib (a first-generation ALK inhibitor), most tumours develop drug resistance due to mutations in key “gatekeeper” residues of the enzyme. This occurrence led to development of novel second-generation ALK inhibitors such as ceritinib to overcome crizotinib resistance. The FDA approved ceritinib in April 2014 due to a surprisingly high response rate (56%) towards crizotinib-resistant tumours and has designated it with orphan drug status.

❻ Afatinib(CAS:439081-18-2) Afatinib is an antineoplastic agent used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with non-resistant EGFR mutations or resistance to platinum-based chemotherapy.

Afatinib is a 4-anilinoquinazoline tyrosine kinase inhibitor in the form of a dimaleate salt available as Boehringer Ingelheim’s brand name 13

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Gilotrif. For oral use, afatinib tablets are a first-line (initial) treatment for patients with metastatic non-small cell lung cancer (NSCLC) with common epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test 4. Gilotrif (afatinib) is the first FDA-approved oncology product from Boehringer Ingelheim.

❼ Erlotinib(CAS:183321-74-6) Erlotinib is an EGFR tyrosine kinase inhibitor used to treat certain small cell lung cancers or advanced metastatic pancreatic cancers. It belongs to a class of drugs known as tyrosine kinase inhibitors. It works by blocking the function of a protein called the epidermal growth factor receptor (EGFR). The EGFR is found on the surface of many cancer cells as well as normal cells. It serves as an “antenna,” receiving signals from other cells and the environment that tell the cell to grow and divide. The EGFR plays an important role in growth and development prenatally and during childhood and helps to maintain normal replacement of old and damaged cells in adults. However, many cancer cells have unusually large amounts of the EGFR on their surface, or their EGFR has been altered by mutation of the DNA that carries the genetic code for the protein. The result is that the signals coming from the EGFR are much too strong, leading to excessive cell growth and division, a hallmark of cancer.

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Reference [1] Underner M, Urban T, Perriot J, de Chazeron I, Meurice JC (June 2014). “[Cannabis smoking and lung cancer]”. Revue des Maladies Respiratoires. 31 (6): 488–98. doi:10.1016/j.rmr.2013.12.002. PMID 25012035.

[2] Schmid K, Kuwert T, Drexler H (March 2010). “Radon in indoor spaces: an underestimated risk factor for lung cancer in 14

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environmental medicine”. Deutsches Ärzteblatt International. 107 (11): 181–6.

[3] Davies RJ, Lee YC (2010). “18.19.3”. Oxford Textbook Medicine (5th ed.). OUP Oxford. ISBN 978-0-19-920485-4.

[4] Cooper WA, Lam DC, O’Toole SA, Minna JD (October 2013).

“Molecular biology of lung cancer”. Journal of Thoracic Disease. 5 Suppl 5 (Suppl. 5): S479–90. doi:10.3978/j.issn.2072-1439.2013.08.03. PMC 3804875. PMID 24163741.

[5] Kumar V, Abbas AK, Aster JC (2013). “Chapter 5”. Robbins Basic Pathology (9th ed.). Elsevier Saunders. p. 212. ISBN 978-1-4377-1781-5.

[6] Subramanian J, Govindan R (February 2007). “Lung cancer in never smokers: a review”. Journal of Clinical Oncology. 25 (5): 561–70.

[7] Ferri FF (2014). Ferri’s Clinical Advisor 2015 E-Book: 5 Books in 1.

Elsevier Health Sciences. p. 708. ISBN 978-0-323-08430-7.

[8] Carr LL, Jett JR (2015). “Chapter 114: Treatment of non-small-cell lung cancer: chemotherapy”. In Grippi MA, Elias JA, Fishman JA, Kotloff RM, Pack AI, Senior RM (eds.). Fishman’s Pulmonary Diseases and Disorders (5th ed.). McGraw-Hill. p. 1752. ISBN 978-0-07-179672-9.

[9] Murray N, Turrisi AT (March 2006). “A review of first-line treatment for small-cell lung cancer”. Journal of Thoracic Oncology. 1 (3): 270–8. doi:10.1016/s1556-0864(15)31579-3. PMID 17409868.

[10] Ikushima H (February 2010). “Radiation therapy: state of the art and the future”. The Journal of Medical Investigation. 57 (1–2): 1–11. doi:10.2152/jmi.57.1. PMID 20299738.

[11] Arriagada R, Goldstraw P, Le Chevalier T (2002). Oxford Textbook of Oncology (2nd ed.). Oxford University Press. p. 2094.

ISBN 978-0-19-262926-5.

[12] Goldstein SD, Yang SC (October 2011). “Role of surgery in small cell lung cancer”. Surgical Oncology Clinics of North America. 20 (4): 769–77.

[13] Lung cancer survival statistics.Cancer Research UK. 15 May 2015. Archived from the original on 7 October 2014.

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[14] Prince-Paul M (April 2009). “When hospice is the best option: an opportunity to redefine goals”. Oncology. 23 (4 Suppl Nurse Ed): 13–7.

PMID 19856592.

[15] Stewart BW, Wild CP (2014). World cancer report 2014. Lyon: IARC Press. pp. 350–352. ISBN 978-92-832-0429-9.

[16] National Cancer Institute; SEER stat fact sheets: Lung and Bronchus. Surveillance Epidemiology and End Results. 2010 [1] Archived 6 July 2014 at the Wayback Machine.

[17] Heavey S, O’Byrne KJ, Gately K (April 2014). “Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC”. Cancer Treatment Reviews. 40 (3): 445–56.

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