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Gefitinib

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Gefitinib is a type of drug which was used to treat non-small cell lung cancer that has spread to other parts of the body and has not already been treated with other anticancer therapy…

Product Description

Basic Characteristics

Product Name Gefitinib
CAS Number 184475-35-2
Molecular Formula C22H24ClFN4O3
Formula Weight 446.9
Synonyms Gefitinib(184475-35-2);

ZD1839;

Gefitinib Iressa;

N-(3-Chlor-4-fluorophenyl)-7-[methoxy-6-[(3-morpholin-4-yl)propoxyl]-quinazolin-4-yl]amine.

Appearance White powder
Storage and Handling Store at controlled room temperature 20°C-25°C.

 

Gefitinib Description

Gefitinib is a type of drug which was used to treat non-small cell lung cancer that has spread to other parts of the body and has not already been treated with other anticancer therapy. It is used in patients whose cancer has certain mutations (changes) in a gene called epidermal growth factor receptor (EGFR). It is also being studied in the treatment of other types of cancer. Gefitinib blocks certain proteins made by the mutated EGFR gene, which may help keep cancer cells from growing. It may also prevent the growth of new blood vessels that tumors need to grow. Gefitinib is a type of tyrosine kinase inhibitor and a type of antiangiogenesis agent. Also called Iressa and ZD1839.

 

Gefitinib Mechanism of Action

Targeted therapy is the result of about 100 years of research dedicated to understanding the differences between cancer cells and normal cells.  To date, cancer treatment has focused primarily on killing rapidly dividing cells because one feature of cancer cells is that they divide rapidly.  Unfortunately, some of our normal cells divide rapidly too, causing multiple side effects.

Targeted therapy is about identifying other features of cancer cells.  Scientists look for specific differences in the cancer cells and the normal cells.  This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects.  Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.

There are different types of targeted therapies, defined in three broad categories.  Some targeted therapies focus on the internal components and function of the cancer cell.  The targeted therapies use small molecules that can get into the cell and disrupt the function of the cells, causing them to die.  There are several types of targeted therapy that focus on the inner parts of the cells.   Other targeted therapies target receptors that are on the outside of the cell.   Therapies that target receptors are also known as monoclonal antibodies.  Antiangiogenesis inhibitors target the blood vessels that supply oxygen to the cells, ultimately causing the cells to starve.

Genefitinib is a targeted therapy that targets and binds to the epidermal growth factor receptors (EGFR) on the surface of the cell. EGFR is found on the surface of many normal and cancer cells.  By binding to these receptors genefitinib blocks an important pathway that promotes cell division. 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.

Research continues to identify which cancers may be best treated with targeted therapies and to identify additional targets for more types of cancer.

Note:  We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational, but is not a substitute for medical advice.

 

Gefitinib Application

Gefitinib is used to treat some people who have non-small cell lung cancer (NSCLC).

The drug only works for cases of NSCLC that have changes called EGFR mutations on the surface of their cells. EGFR mutations are most likely to occur in NSCLC in:

♦ women

♦ people who have never smoked

♦ people with adenocarcinoma (a specific type of NSCLC)

♦ people of Asian ancestry

There are tests to check the level of EGFR. These tests will help you and your doctors decide whether you are likely to benefit from treatment with gefitinib. These tests can be done at the same time as diagnosis or can be performed using samples of cancer cells from previous biopsies or surgery.

 

Gefitinib Side Effects & Warning

We haven’t listed all the side effects. It is very unlikely that you will have all of these side effects, but you might have some of them at the same time.

How often and how severe the side effects are can vary from person to person. They also depend on what other treatment you are having. For example, your side effects could be worse if you are also having other drugs or radiotherapy.

 

Common side effects

▪ Skin changes

▪ Diarrhoea

▪ Feeling or being sick

▪ Sore mouth and ulcers

▪ Loss of appetite

▪ Liver changes

▪ Lack of energy and strength

 

Occasional side effects

Each of these effects happens in more than 1 in 100 people (1%). You might have one or more of them. They include:

▪ An increased risk of bleeding such as a nose bleed or blood in the urine

▪ Dry, brittle or loose nails during treatment

▪ Inflammation of the bladder causing pain when passing urine and need to pass urine often

▪ Kidney problems that don’t usually cause any symptoms

▪ High temperature – fever

▪ Eye problems such as red, itchy, sore dry eyes or blurred vision

▪ Sore, red eyelids or ingrown eyelashes

▪ Thinning of your hair

▪ Lung problems

▪ Not enough water in your body (dehydration) caused by diarrhoea, being sick or loss of appetite

▪ An allergic reaction causing itching, rash or swelling tell your doctor if this happens

 

Rare side effects

Each of these effects happens in fewer than 1 in 100 people (1%). You might have one or more of them. They include:

▪ Inflammation of the pancreas

▪ A hole in the stomach or bowel

▪ Inflammation of the liver

▪ Eye problems

 

Reference

[1] Sordella R, Bell DW, Haber DA, Settleman J: Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. 2004 Aug 20;305(5687):1163-7. Epub 2004 Jul 29.

[2] Moasser MM, Basso A, Averbuch SD, Rosen N: The tyrosine kinase inhibitor ZD1839 (“Iressa”) inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8.

[3] Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.

[4] Nicholson RI, Hutcheson IR, Harper ME, Knowlden JM, Barrow D, McClelland RA, Jones HE, Wakeling AE, Gee JM: Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer. Endocr Relat Cancer. 2001 Sep;8(3):175-82.

[5] Suzumura T, Kimura T, Kudoh S, Umekawa K, Nagata M, Matsuura K, Tanaka H, Mitsuoka S, Yoshimura N, Kira Y, Nakai T, Hirata K: Reduced CYP2D6 function is associated with gefitinib-induced rash in patients with non-small cell lung cancer. BMC Cancer. 2012 Dec 4;12:568. doi: 10.1186/1471-2407-12-568.

[6] Shi Z, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS: The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance. Oncol Rep. 2009 Feb;21(2):483-9.

[7] An Y, Ongkeko WM: ABCG2: the key to chemoresistance in cancer stem cells? Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1529-42. doi: 10.1517/17425250903228834.

[8] Rossi S, editor. Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook; 2004.