Zongertinib CAS# 2728667-27-2

Zongertinib (BI 1810631) is an irreversible, oral HER2-selective tyrosine kinase inhibitor that demonstrates potent preclinical efficacy in HER2-driven cancers. It effectively inhibits tumor growth in human non-small cell lung cancer (NSCLC) xenograft models, including those harboring HER2 tyrosine kinase domain (TKD) mutations. Notably, zongertinib spares wild-type EGFR, reducing associated toxicities. It also enhances the efficacy of antibody-drug conjugates and KRAS G12C inhibitors in combination therapies. These preclinical findings have translated into clinical activity, with zongertinib achieving a 71% objective response rate in patients with HER2-mutant NSCLC in the Beamion LUNG-1 trial