BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, exhibiting an IC50 of 7 nM. It demonstrates more than 25-fold selectivity over EGFR. BI-1622 has shown high antitumor efficacy in vivo within xenograft mouse tumor models using engineered H2170 and PC9 cells, coupled with a favorable agent metabolism and pharmacokinetics profile.
- Orally active.
- Potent and highly selective HER2 (ERBB2) inhibitor (IC50 of 7 nM).
- Exhibits >25-fold selectivity over EGFR.
- High antitumor efficacy in vivo in xenograft mouse tumor models.
- Favorable agent metabolism and pharmacokinetics profile.
- Inhibits proliferation of HER2-dependent cell lines.
- Good permeability and no PgP-mediated efflux liability.