Hernexeos (zongertinib tablets) approved in China as first oral targeted therapy for previously treated patients with HER2-mutant advanced NSCLC – Boehringer
Boehringer Ingelheim’s Hernexeos (zongertinib tablets) has been approved as monotherapy by China’s National Medical Products Administration (NMPA) for the treatment of adult patients with unresectable, locally advanced or metastatic non-small cell lung cancer (NSCLC) whose tumors have activating HER2 (ERBB2) mutations and who have received at least one line of prior systemic therapy. The accelerated approval followed a Breakthrough Therapy Designation and Priority Review status, reflecting the high recognition of its clinical benefit.
“The absence of a well-tolerated oral drug targeting HER2, has been a long-standing challenge in the treatment of non-small cell lung cancer. The approval of zongertinib will change this landscape, setting a new treatment benchmark for HER2-mutant advanced non-small cell lung cancer,” said Professor Wu Yilong from Guangdong Provincial People’s Hospital, Chairman of the Chinese Thoracic Oncology Group (CTONG). “This innovative drug provides a highly effective, targeted, oral treatment option for this patient population, which has an extremely poor prognosis and very limited treatment choices.”
The conditional approval has been granted based on data from the Phase Ib Beamion-LUNG 1 trial, which demonstrated an objective response rate (ORR) of 71% (N=75). Data showed 7% of patients had a complete response (CR), with almost all patients (96%) achieving disease control. The median duration of response (mDoR) was 14.1 months, and the median progression-free survival (PFS) was 12.4 months. These results were previously presented at the American Association for Cancer Research (AACR) Annual Meeting 2025 and simultaneously published in The New England Journal of Medicine.
Hernexeos demonstrated a manageable safety profile with a low discontinuation rate of 2.9%.ernexeos.
The therapy was recently granted Breakthrough Therapy Designation by China’s Center for Drug Evaluation (CDE) for the first-line treatment of adult patients with unresectable or metastatic NSCLC harboring activating mutations in the HER2 tyrosine kinase domain (TKD). Zongertinib is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby limiting associated toxicities.
“It is encouraging to see the NMPA’s continued recognition of zongertinib’s potential. Breakthrough Therapy Designation for first-line use of zongertinib in China illustrates the urgent need in this patient population. It is a critical next step to making this therapy available to more patients in need,” said Shashank Deshpande, Chairman of the Board of Managing Directors at Boehringer Ingelheim. “Given the robust clinical evidence, regulatory approvals and breakthrough designation, we are confident that zongertinib has the potential to redefine the standard for treating HER2-driven cancers. Therefore, we have initiated clinical studies to evaluate this therapy in other cancers, including breast cancer and the tumor-agnostic setting.”
About the Beamion clinical trial program
Beamion LUNG-1 (NCT04886804): An open-label, Phase I dose escalation trial, with dose confirmation and expansion, of zongertinib as monotherapy in people with unresectable or metastatic solid tumors with HER2 alterations. The study has 2 parts. The first part is open to adults with different types of advanced cancer with HER2 alterations that include mutations, amplifications, over-expression and fusions for whom previous treatment was not successful. The second part is open to people with HER2-mutant non-small cell lung cancer.
Beamion LUNG-2 is a phase III, open label, randomized, active-controlled study that will enroll 416 patients with unresectable, or metastatic non-squamous NSCLC harboring HER2 tyrosine kinase domain mutations to evaluate zongertinib compared with standard of care.
Citation: Zongertinib in Previously Treated HER2-Mutant Non–Small-Cell Lung Cancer. Authors: John V. Heymach, M.D., Ph.D., Gerrina Ruiter, M.D., Ph.D., Myung-Ju Ahn, M.D., Nicolas Girard, M.D., Ph.D. et al. Published April 28, 2025 N Engl J Med 2025; 392:2321-2333 DOI: 10.1056/NEJMoa2503704 VOL. 392 NO. 23
