Gefitinib is an anilinoquinazoline compound with the chemical name 4-quinazolinamine, N-(3-chloro-4-flurophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]. Gefitinib inhibits receptor tyrosine kinases (TKs) including the epidermal growth factor recpetor (EGRF)-TK. Gefitinib also inhibits ATP-binding cassette transporter-mediated drug efflux, which in turn strongly increases the intracellular concentrations of co-administrated drug molecules that are transporter substrates.
After oral administration, gefitinib is widely distributed throughout the body. Gefitinib is metabolized in the liver by cytochrome P450s, primarily by CYP3A4, but CYP3A5 and CYP2D6 also play minor roles in gefitinib metabolism. In addition to its role as an ABC transporter inhibitor, gefitinib has also been implicated as an inhibitor of CYP2C19 and CYP2D6 activity. Therefore, gefitinib may inhibit the metabolism of co-administered drugs that are substrates of CYP2C19 and CYP2D6 and weakly inhibits the metabolism of substrates of CYP2C9, CYP3A4, and CYP1A2.
M. Whirl-Carrillo, E.M. McDonagh, J. M. Hebert, L. Gong, K. Sangkuhl, C.F. Thorn, R.B. Altman and T.E. Klein. "Pharmacogenomics Knowledge for Personalized Medicine" Clinical Pharmacology & Therapeutics (2012) 92(4): 414-417. Full text
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