207_Combined course Presentations

Iressa - Gefitinib

The first selective inhibitor that targets the mutant proteins in malignant cells Used to treat lung cancer Only ~10% of non-small cell lung cancer patients response to Iressa Toxicities include acne, diarrhea, nausea, vomiting and skin reactions chemical class: quinazoline orally bioavailable (compliance) selective inhibitor of EGFR tyrosine kinase - EGFR IC50 = 0.023-0.079 µM - erbB2 IC50 = 1.2-3.7 µM

competitive inhibitor of ATP-binding inhibits ligand-induced cell growth - IC50 = 0.08 µM