Gefitinib
- Atc Codes:L01XE02
- CAS Codes:184475-35-2
- PHARMGKB ID:184475-35-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europa
Austria: Iressa; Bulgaria: Iressa; Czech Republic: Iressa; Denmark: Iressa; Estonia: Iressa; Finland: Iressa; Germany: Iressa; Greece: Iressa; Hungary: Iressa; Ireland: Iressa; Latvia: Iressa; Lithuania: Iressa; Malta: Iressa; Netherlands: Iressa; Portugal: Iressa; Romania: Iressa; Slovakia: Iressa; Slovenia: Iressa; Sweden: Iressa; UK: Iressa.
North America
USA: Iressa.
Latin America
Mexico: Iressa.
Asia
Japan: Iressa.
Drug combinations
Chemistry
Gefitinib: C~22~H~24~ClFN~4~O~3~. Mw: 446.90. 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-4-morpholin)propoxy]-. CAS-184475-35-2 (2002).
Pharmacologic Category
Other Antineoplastic Agents; Protein Kinase Inhibitors. Tyrosine Kinase Inhibitor. (ATC-Code: L01XE02).
Mechanism of action
Mechanism of antineoplastic action not fully understood. Gefitinib inhibits tyrosine kinases (TK) associated with transmembrane cell surface receptors found on both normal and cancer cells. One such receptor is epidermal growth factor receptor. TK activity appears to be vitally important to cell proliferation and survival.
Therapeutic use
Treatment of locally advanced or metastatic non-small cell lung cancer after failure of platinum-based and docetaxel therapies. Treatment limited to patients who are benefiting or have benefited from treatment with gefitinib.
Pregnancy and lactiation implications
Animal studies demonstrated fetal harm. There are no well-controlled studies in pregnant women.
Unlabeled use
Contraindications
Hypersensitivity to gefitinib or any component of the formulation. Pregnancy.
Warnings and precautions
Hazardous agent. Interruption of therapy may be required in poorly tolerated diarrhea. Eye pain might occur. Rare, sometimes fatal, pulmonary toxicity (e.g. alveolitis, interstitial pneumonia, pneumonitis) reported. Risk of increased mortality in patients with concurrent idiopathic pulmonary fibrosis whose condition worsens while receiving gefitinib. Adverse skin reactions reported (angioedema and urticaria). Hemorrhage (e.g. epistaxis, hematuria) and pancreatitis (rarely) reported. Use with caution in hepatic impairment (may cause hepatic injury and elevation of transaminases). Use with caution in severe renal impairment. Asymptomatic elevations of hepatic aminotransferase concentrations reported.