Boehringer Ingelheim  announced that China’s National Medical Products Administration (NMPA) has approved HERNEXEOS® (zongertinib tablets) as monotherapy for the treatment of adult patients with unresectable, locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring activating HER2 (ERBB2) mutations who have received at least one prior systemic therapy. This accelerated approval follows Breakthrough Therapy Designation and Priority Review, underscoring the significant clinical benefit of this novel treatment.

The approval is supported by data from the Phase Ib Beamion-LUNG 1 trial, which demonstrated an objective response rate (ORR) of 71% (N=75), including 7% complete responses, with 96% of patients achieving disease control. The median duration of response (mDoR) was 14.1 months and median progression-free survival (PFS) was 12.4 months. These results, previously presented at the AACR Annual Meeting 2025 and published in The New England Journal of Medicine, mark the first time an oral HER2-targeted therapy has shown this level of efficacy in HER2-mutant NSCLC.

“The absence of a well-tolerated oral drug targeting HER2 has been a long-standing challenge in the treatment of NSCLC. The approval of zongertinib will change this landscape, setting a new treatment benchmark for HER2-mutant advanced lung cancer,” said Professor Wu Yilong, Guangdong Provincial People’s Hospital, Chairman of the Chinese Thoracic Oncology Group (CTONG). “This innovative therapy provides a highly effective, targeted oral option for a patient population with extremely limited choices and poor prognosis.”

Zongertinib demonstrated a manageable safety profile with a discontinuation rate of only 2.9%. The therapy has also received Breakthrough Therapy Designation by the CDE for first-line treatment of adult patients with unresectable or metastatic NSCLC with HER2 tyrosine kinase domain mutations, paving the way for broader use earlier in the treatment pathway.

“It is encouraging to see the NMPA’s recognition of zongertinib’s potential. Breakthrough Therapy Designation for first-line use reflects the urgent need for innovation in HER2-mutant NSCLC,” said Shashank Deshpande, Chairman of the Board of Managing Directors, Boehringer Ingelheim. “With robust clinical data and regulatory momentum, we are confident zongertinib can redefine the treatment standard for HER2-driven cancers, and we are expanding its evaluation to breast cancer and tumor-agnostic settings.”

Lung cancer remains the leading cause of cancer death in China, with non-small cell lung cancer accounting for approximately 85% of cases. HER2 mutations are present in an estimated 2–4% of NSCLC patients, associated with poor prognosis and a higher incidence of brain metastases. The approval of HERNEXEOS® marks a major advancement in delivering targeted, effective therapies to this underserved population.