Irreversible kinase inhibitor of the human EGFR family (EGFR/HER1, HER2, and HER4) and certain EGFR-activating mutations (exon 19 deletion or the exon 21 L858R substitution mutation)
Also inhibited the activity of DDR1, EPHA6, LCK, DDR2, and MNK1 in vitro at clinically relevant concentrations
Demonstrates dose-dependent inhibition of EGFR and HER2 autophosphorylation and tumor growth in mice bearing SC implanted human tumor xenografts driven by HER family targets including mutated EGFR; also, exhibits antitumor activity in orally dosed mice bearing intracranial human tumor xenografts driven by EGFR amplifications