Boehringer Ingelheim (BI)'s oral HER2 tyrosine kinase inhibitor (TKI), Hernexeos (zongertinib), has received US regulatory approval for the first-line treatment of adults with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) harbouring HER2 (ERBB2) tyrosine kinase domain-activating mutations. The drug, initially approved in August 2025 for previously treated patients, is now the first and only oral HER2 TKI approved for this indication in the front-line setting. Hernexeos is designed to selectively inhibit HER2 while sparing wild-type EGFR to minimise off-target toxicity.

The approval is based on data from the Phase I Beamion LUNG-1 study, which showed a confirmed objective response rate (ORR) of 76% and a median duration of response (mDOR) of at least 6 months in 64% of treatment-naive patients. BI is currently conducting the confirmatory Phase III Beamion LUNG-2 trial to further evaluate Hernexeos as a first-line therapy for this patient population.

PharmCube's NextBiopharm® database shows that the drug is under active development in seven oncology indications. Click here to request a free trial for NextBiopharm®.