PF-06459988

Description:
PF-06459988 is a potent and selective ATP-competitive inhibitor of the epidermal growth factor receptor (EGFR). It is an orally bioavailable small molecule that potently and selectively inhibits EGFR with a binding affinity more than 10,000 times greater than other known kinases. PF-06459988 has shown efficacy in inhibiting the growth of human cancer cells in vitro and in vivo. In addition, it has been shown to inhibit the proliferation of human keratinocytes. PF-06459988 binds to the ATP site on EGFR with higher affinity than ATP, and then undergoes covalent modification of the catalytic domain to form a stable complex. This covalent modification prevents phosphorylation at tyrosine residues by inhibiting protein kinase activity.PF-06459988 has been shown to be well tolerated in Phase 1 clinical studies for patients with advanced solid tumors.