Gefitinib (formally labeled as ZD1839)is a selective epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor that blocks the growth of GEO colon, ZR-75-1, MCF-10A Ha-ras breast and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM. By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer (NSCLC) with approval. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit. Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.
Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor.
ZD1839 (Iressa), a novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, potently inhibits the growth of EGFR-positive cancer cell lines with or without erbB2 overexpression.
ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase.
Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial.