On May 21, Boehringer Ingelheim and Sino Biopharmaceutical jointly announced that zongertinib tablets have been approved by the National Medical Products Administration (NMPA) of China for first -line treatment of adult patients with unresectable locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring HER2 ( ERBB2 ) tyrosine kinase domain activating mutations. Zongertinib is an oral HER2 tyrosine kinase inhibitor. This approval follows the NMPA's Center for Drug Evaluation (CDE) granting the product Breakthrough Therapy designation for first-line indication and its NMPA approval for the treatment of previously treated patients in August 2025.
Zonaitinib tablets are an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 (ERBB2) while preserving wild-type EGFR , thereby helping to reduce related toxic reactions.
The incidence of HER2 mutations in non-small cell lung cancer is approximately 2%-4%. These mutations are more common in women, non-smokers, patients with lung adenocarcinoma, and younger individuals. These tumors are highly aggressive, have a high risk of brain metastasis, and result in extremely poor prognosis, and have long been considered one of the "refractory subtypes" among many known driver genes. In clinical practice, these patients face particularly prominent core challenges: a long-term lack of targeted oral drugs, limited efficacy and significant toxic side effects of traditional chemotherapy regimens, low response rates to immunotherapy, and difficulty in effectively controlling tumor growth. Furthermore, existing treatments often suffer from inconvenient administration, poor treatment adherence, and poor control of brain metastases, failing to effectively delay disease progression, leading to low quality of life and shortened survival. Their urgent clinical treatment needs have long remained unmet.
The conditional approval of zonetinib for first-line indication in China is based on the results of the Phase 1b Beamion-LUNG 1 cohort 2 clinical trial, which evaluated the efficacy and safety of zonetinib in treatment-naïve patients with HER2 ( ERBB2 ) activating mutations in advanced non-small cell lung cancer (NSCLC).
Data showed that in the treatment-naïve cohort 1 (N=74) patients, the confirmed objective response rate (ORR) was 76%, with 11% achieving complete response and 65% achieving partial response. The median duration of response (mDoR) was 15.2 months, and the median progression-free survival (mPFS) was 14.4 months. These data were reported at the European Conference on Lung Cancer 2026 (ELCC 2026) and were also published concurrently in the *New England Journal of Medicine*. Furthermore, the article also reported data from 30 patients with HER2- mutant advanced non-small cell lung cancer and active brain metastases, of whom 47% achieved an intracranial objective response (iORR) confirmed by the Neuro-oncology-Brain Metastasis Response Assessment (RANO-BM) criteria .

https://mp.weixin.qq.com/s/n6fvWLQQA7cGKMlc-q5uOQ