Gefitinib hydrochloride (ZD1839) is a potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.
Gefitinib inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM.
Gefitinib blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM.
Gefitinib significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.
Gefitinib has been used to treat advanced (or recurrent) non-small cell lung cancer.
