On January 4th, the first batch of Zonaitinib tablets (Shenghetu®), jointly promoted by Boehringer Ingelheim and China Biopharmaceutical (1177.HK), arrived in China and will be put into clinical use in Guangzhou, Shanghai, and other regions as soon as possible. As the world's first and currently only oral targeted drug approved in China for the treatment of HER2-mutant advanced non-small cell lung cancer (NSCLC), Zonaitinib provides patients with a highly effective, safe, targeted, and oral new treatment option, officially ushering in a new era of highly selective oral targeted therapy for the treatment of HER2-mutant advanced NSCLC in China.
In August 2025, Zonaitinib received formal approval from the China National Medical Products Administration (NMPA) for the treatment of adult patients with unresectable locally advanced or metastatic non-small cell lung cancer (NSCLC) who have HER2 (ERBB2) activating mutations and have previously received at least one systemic therapy. Notably, Zonaitinib took only one year from submitting its marketing authorization application in January 2025 to benefiting patients, demonstrating the "China speed" of rapid implementation of innovative therapies.
The approval of zonetinib was based on the positive results of the Beamion-LUNG 1 study, which evaluated the efficacy and safety of zonetinib in patients with HER2 (ERBB2)-mutant advanced NSCLC. Data showed that in the cohort 1 of previously treated patients (N=75), the objective response rate (ORR) was 71% (95% CI: 60-80), of which 7% achieved complete remission, and the disease control rate (DCR) was 96%; the median duration of response (DoR) was 14.1 months, and the median progression-free survival (PFS) was 12.4 months [1] . In addition, the safety of zonetinib was manageable, with a treatment discontinuation rate of only 2.9% in the study [2] .
Further analysis of the clinical benefits of 39 Asian patients (including 18 Chinese patients) in cohort 1 revealed [3] that Asian and Chinese patients benefited more significantly. The ORR of zonetinib in previously treated HER2 TKD-mutant Asian patients increased to 77%, and the DCR reached 100%. Most patients could be observed at the first evaluation (median time to objective response was 1.4 months) and could achieve sustained response (median DoR 14.1 months). The ORR in the Chinese population reached 83%, the DCR was 100%, and the median PFS was 15.5 months, which bought valuable survival time for patients with advanced disease.
HER2 activating mutation NSCLC is a highly heterogeneous and aggressive disease, and there is still a huge unmet need for treatment in the first-line treatment field. There is currently no approved targeted therapy. At the 2025 European Society for Medical Oncology (ESMO) Annual Meeting, the Beamion LUNG-1 Phase Ib clinical trial data were presented for the first time to evaluate the efficacy of zonetinib in treatment-naïve patients with advanced HER2 (ERBB2) mutation NSCLC. The results showed that the response rate confirmed by blinded independent central imaging assessment was 77%, of which 8% of patients achieved complete remission and 96% of patients achieved disease control [4] .
Previously, zotinib had been granted Breakthrough Therapy Designation by the U.S. Food and Drug Administration (FDA) and the Center for Drug Evaluation (CDE) of the China National Medical Products Administration for the first-line treatment of adult patients with unresectable/metastatic NSCLC with HER2 TKD activating mutations.

https://mp.weixin.qq.com/s/c3ztpppbWPdKSiSzAzj07A