Gefitinib
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| Clinical data | |
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| Trade names | Iressa |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a607002 |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 59% (oral) |
| Protein binding | 90% |
| Metabolism | Hepatic (mainly CYP3A4) |
| Biological half-life | 6–49 hours |
| Excretion | Faecal |
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| ECHA InfoCard | 100.171.043 |
| Chemical and physical data | |
| Formula | C22H24ClFN4O3 |
| Molar mass | 446.902 g/mol |
| 3D model (Jmol) | |
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Gefitinib (ZD1839) (INN, /ɡɛˈfɪtᵻnɪb/, trade name Iressa) is a drug used for certain breast, lung and other cancers. Gefitinib is an EGFR inhibitor, like erlotinib, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. It is marketed by AstraZeneca and Teva.
Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase domain. Thus gefitinib is an EGFR inhibitor. The target protein (EGFR) is a member of a family of receptors (ErbB) which includes Her1(erb-B1), Her2(erb-B2), Her3(erb-B3) and Her4 (Erb-B4). 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 anti-apoptotic Ras signalling 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. 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).
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