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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