Erlotinib (OSI744, Tarceva)

Description: Erlotinib (formerly OSI744, trade name: Tarceva) is a quinazoline-based EGFR (epidermal growth factor receptor) inhibitor with potential antineoplastic activity. It inhibits EGFR with IC50 of 2 nM in cell-free assays, and is >1000-fold more sensitive for EGFR over human c-Src or v-Abl. Erlotinib is an FDA-approved medicine for the treatment of non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer. It acts by competing with adenosine triphosphate and reversibly binding to the intracellular catalytic domain of EGFR tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation.