Dacomitinib

Dacomitinib, also known as PF-00299804, is a second-generation irreversible pan-erbB (HER) receptor tyrosine kinase inhibitor.  It is believed to irreversibly inhibit erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members.  The HER family of tyrosine kinases included receptors HER-1 (EGFR), HER-2,3 and 4.  The HER signaling pathway plays a role in the normal regulation of cell growth and proliferation, differentiation, and apoptosis.  Activation of HER receptors drives signal transduction pathways; dysregulated signaling through the HER receptors may lead to malignant transformation and growth.