On February 26, the FDA granted zongertinib through a special approval pathway for the treatment of adult patients with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) who have HER2 (ERBB2) tyrosine kinase domain activating mutations . Zonatitinib, developed by Boehringer Ingelheim, is the world's first and currently only approved oral HER2 tyrosine kinase inhibitor (TKI). It selectively inhibits HER2 (ERBB2) while avoiding inhibition of wild-type EGFR, thereby minimizing related toxicities. In August 2025, Zonatitinib received approval from both the FDA and the NMPA for the treatment of adult patients with unresectable or metastatic non-squamous NSCLC who have HER2 (ERBB2) tyrosine kinase domain activating mutations and have previously received systemic therapy.With this approval, the target population for zotinib has been further expanded to include individuals who have not received systemic therapy.This approval is based on data from the Phase I Beamion LUNG-1 study. Results showed that the confirmed objective response rate (cORR) was 76% in 72 treatment-naïve patients with advanced NSCLC, with 11% achieving complete response (CR) and 65% achieving partial response (PR); 64% and 44% of patients, respectively, had a median duration of response (DoR) of ≥6 months and ≥12 months.Boehringer Ingelheim is conducting a confirmatory phase III clinical trial (Beamion LUNG-2) of zotinib as first-line treatment for advanced non-squamous NSCLC with HER2 (ERBB2) tyrosine kinase domain activating mutations.

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