BI-1622 is a highly selective, orally active HER2(ERBB2) inhibitor (IC50: 7 nM). BI-1622 is >25-fold selective for EGFR. In a mouse model of transplanted tumors transfected with H2170 and PC9 cells, BI-1622 exhibited high in vivo antitumor effects with good drug metabolism and pharmacokinetic properties.