Boehringer Ingelheim (BI)'s zongertinib has received approval from China's National Medical Products Administration (NMPA) as the world's first oral HER2 tyrosine kinase inhibitor (TKI) for previously treated HER2-mutant non-small cell lung cancer (NSCLC). The covalent binder targets wild-type and mutant HER2 receptors including exon 20 mutants, demonstrating 71% objective response rate (ORR) and 96% disease control rate (DCR) in the Phase Ia/Ib Beamion LUNG-1 trial (n=75). Median progression-free survival (PFS) reached 12.4 months with 14.1-month duration of response (DOR) in this population representing 2% to 4% of Chinese NSCLC patients.

The approval follows BI's April 2024 strategic partnership with Sino Biopharmaceutical to co-develop and commercialise oncology assets in China. Zongertinib's novel mechanism addresses poor prognosis in HER2-mutant NSCLC where median overall survival (OS) historically ranges from 1.6 to 1.9 years from Stage IV diagnosis. The drug showed favourable tolerability with only 2.9% treatment discontinuation rates in clinical trials.

According to PharmCube's NextBiopharm® database, zongertinib has entered development in eight other indications. Click here to request a free trial for NextBiopharm®.