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Gefitinib (INN) (IPA: ) is a drug used in the treatment of certain types of cancer. Acting in a similar manner to erlotinib (marketed as Tarceva), gefitinib selectively targets the mutant proteins in malignant cells. It is marketed by AstraZeneca under the trade name Iressa.
Mechanism of action
Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase domain. The target protein (EGFR) is also sometimes referred to as Her1 or ErbB-1 depending on the literature source.
EGFR is overexpressed in the cells of certain types of human carcinomas - for example in lung and breast cancers. This leads to inappropriate activation of the apoptotic Ras signal transduction cascade, eventually leading to uncontrolled cell proliferation. Research on gefitinib-sensitive non-small cell lung cancers has shown that a mutation in the EGFR tyrosine kinase domain is responsible for activating anti-apoptotic pathways.Pao W, Miller V, Zakowski M, Doherty J, Politi K, Sarkaria I, 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;101:13306-11. PMID 15329413 (Full text)Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science 2004;305:1163-7. PMID 15284455 These mutations tend to confer increased sensitivity to tyrosine kinase inhibitors such as gefitinib and erlotinib. Of the types of non-small cell lung cancer histologies, adenocarcinoma is the type that most often harbors these mutations. These mutations are more commonly seen in Asians, women, and non-smokers (who also tend to more often have adenocarcinoma).
More on [ Gefitinib ]
J Clin Oncol: Randomized Phase III Trial of Platinum-Doublet Chemotherapy Followed by Gefitinib Compare... www.amedeo.com/c.php?i=20038730
AmedeoSelection (Amedeo Selection) Wed, 06 Jan 2010 11:00:02 -0000
J Clin Oncol: Randomized Phase III Trial of Platinum-Doublet Chemotherapy Followed by Gefitinib Compare... www.amedeo.com/c.php?i=20038730
Heme/Onc: Randomized phase III trial of platinum-doublet chemotherapy followed by gefitinib compared with continued pla http://url4.eu/1412B
MDLinx (Sandeep Pulim MD) Wed, 06 Jan 2010 10:05:30 -0000
Heme/Onc: Randomized phase III trial of platinum-doublet chemotherapy followed by gefitinib compared with continued pla http://url4.eu/1412B
Heme/Onc: Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer http://url4.eu/14128
MDLinx (Sandeep Pulim MD) Wed, 06 Jan 2010 10:05:29 -0000
Heme/Onc: Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer http://url4.eu/14128
RT @LCSCnews: Gefitinib improved survival vs. cisplatin/docetaxel http://lungevity.org/l_community/viewtopic.php?t=43014
brownbeansprout (Katie Brown) Mon, 04 Jan 2010 19:59:58 -0000
RT @LCSCnews: Gefitinib improved survival vs. cisplatin/docetaxel http://lungevity.org/l_community/viewtopic.php?t=43014
Gefitinib improved survival vs. cisplatin/docetaxel http://lungevity.org/l_community/viewtopic.php?t=43014
LCSCnews (LCSC News) Mon, 04 Jan 2010 19:49:48 -0000
Gefitinib improved survival vs. cisplatin/docetaxel http://lungevity.org/l_community/viewtopic.php?t=43014
Gefitinib outdoes chemo in mNSCLC patients when it comes to progression free survival. http://snurl.com/typ4v
Callooh (Callooh) Mon, 04 Jan 2010 15:18:58 -0000
Gefitinib outdoes chemo in mNSCLC patients when it comes to progression free survival. http://snurl.com/typ4v
Iressa - Lung cancer information for health care professionals and patients regarding advanced non-small cell lung cancer treatment.
Meta Description: [ IRESSA for advanced non-small cell lung cancer treatment with an EGFR-TK (epidermal growth factor receptor-tyrosine kinase) inhibitor. Site provides relevant lung cancer information for oncology research to health care professionals and patients. ]
Iressa Consumer Information - FDA - Consumer FAQ in html format with a link to approved labeling in pdf format.
Meta Description: [ Patient Information Sheet for Iressa ]
