Description
Dacomitinib is an ATP-competitive, irreversible pan-erbB receptor (EGFR) inhibitor that shows anticancer chemotherapeutic activity in models of squamous cell carcinoma, ovarian carcinoma, and non-small-cell lung cancer (NSCLC). Dacomitinib covalently modifies cytosine residues in the catalytic domain of this kinase, preventing phosphorylation of downstream targets such as Akt, and ERK, resulting in cell cycle arrest at the G0/G1 phase and induction of apoptosis. This compound also inhibits mutant EGF receptors in drug-resistant in vivo tumor models.