TAK-285 is a potent, dual inhibitor of HER2 and EGFR (HER1) with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM. TAK-285 (50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice.
