Biochem/physiol Actions

Dacomitinib (PF-00299804) is an irreversible EGFR inhibitor and antineoplastic. It is a potent inhibitor of HER-1 (EGFR), -2 and -4 tyrosine kinase with IC50s of 6.0, 45.7 and 73.7 nM respectively for EGFR, ERBB2 and ERBB4. Dacomitinib 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.

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