Boehringer’s HERNEXEOS® approved in China as first oral targeted therapy for previously treated patients with HER2-mutant advanced NSCLC
This press release is not intended for UK and US media.
- HERNEXEOS® (zongertinib tablets) has been approved based on an objective response rate of 71% (N=75), as demonstrated in the Beamion-LUNG 1 clinical trial1
- Zongertinib recently received Breakthrough Therapy Designation for the first-line treatment of advanced HER2-mutant NSCLC by the Center for Drug Evaluation (CDE)
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.1 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.2
HERNEXEOS® demonstrated a manageable safety profile with a low discontinuation rate of 2.9%.
Breakthrough Designation for first-line use
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.”
Targeting lung cancer through HER2 mutation-directed treatment
Lung cancer is the leading cause of cancer death in China and the incidence and mortality rates of lung cancer have significantly increased in recent years.3 NSCLC is the most common type of lung cancer, accounting for approximately 85% of all cases.4 HER2 mutations occur in approximately 2–4% of NSCLC cases and are associated with a poor prognosis and higher incidence of brain metastases.5,6,7 Alterations in the HER2 (ERBB2) gene, including mutations, amplification and overexpression, trigger uncontrolled cell proliferation, inhibiting cell death, and promoting tumor growth and spread.5,7
About non-small cell lung cancer (NSCLC)
Lung cancer claims more lives than any other cancer type and the incidence is set to increase to over 3 million cases worldwide by 2040.7,8 NSCLC is the most common type of lung cancer.4 Due to a lack of symptoms and misdiagnoses,9 most patients with NSCLC present at stage III or IV, where the disease has metastasized locally or to other organs.10 The estimated 5-year survival rate historically has been less than 10% for metastatic disease.11,12,13 People living with advanced NSCLC can experience a detrimental physical, psychological, and emotional impact on their daily lives.14,15,16
About zongertinib
Zongertinib has been approved by the U.S. FDA (as HERNEXEOS®) and China’s NMPA (as HERNEXEOS®). It is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby limiting associated toxicities. This orally administered, targeted therapy has also been granted Orphan Drug Designation in Japan.
Zongertinib received 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).
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.
About Boehringer Ingelheim in oncology
We have a clear aspiration – to transform the lives of people with cancer by delivering meaningful advances, with the ultimate goal of curing a range of cancers. Boehringer Ingelheim’s generational commitment to driving scientific innovation is reflected by the company’s robust pipeline of cancer cell-directed and immuno-oncology investigational therapies, as well as the smart combination of these approaches. Boehringer’s ambition in oncology is to take a diligent and broad approach, creating a collaborative research network to tap into a diversity of minds, which is vital in addressing some of the most challenging, but potentially most impactful, areas of cancer research. Simply put, for Boehringer Ingelheim, cancer care is personal, today and for generations.
About Boehringer Ingelheim
Boehringer Ingelheim is a biopharmaceutical company active in both human and animal health. As one of the industry’s top investors in research and development, the company focuses on developing innovative therapies that can improve and extend lives in areas of high unmet medical need. Independent since its foundation in 1885, Boehringer takes a long-term perspective, embedding sustainability along the entire value chain. Our approximately 54,500 employees serve over 130 markets to build a healthier and more sustainable tomorrow.
References
1HERNEXEOS Prescribing Information
2Heymach, J. et al. Zongertinib in previously treated HER2-mutant non-small cell lung cancer. N Engl J Med. 2025;01-13.
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6Li, B.T. et al. Trastuzumab Deruxtecan in HER2-Mutant Non–Small-Cell Lung Cancer. N Engl J Med. 2022;386:241–51
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8International Agency for Research on Cancer – World Health Organization. Rates of trachea, bronchus and lung cancer. Available at: https://gco.iarc.fr/tomorrow/en (Accessed: January 2025).
9American Cancer Society. Lung Cancer Early Detection, Diagnosis, and Staging. Available at: https://www.cancer.org/cancer/lung-cancer/detection-diagnosis-staging/signs-symptoms.html (Accessed: January 2025).
10Casal-Mouriño, A. et al. Epidemiology of stage III lung cancer: frequency, diagnostic characteristics, and survival. Transl Lung Cancer Res. 2021;10(1):506-518.
11National Cancer Institute Surveillance, Epidemiology, and End Results (SEER). 5-Year Survival Rates. https://www.seer.cancer.gov/csr/1975_2016/results_merged/topic_survival.pdf (Accessed July 2025).
12Belaroussi, Y. et al. Survival outcomes of patients with metastatic non-small cell lung cancer receiving chemotherapy or immunotherapy as first-line in a real-life setting. Sci Rep. 2023.13, 9584.
13Simeone, J. C. et al. Treatment patterns and overall survival in metastatic non-small-cell lung cancer in a real-world US setting. Fut. Oncol. Lond. Engl. 2019. 15(30), 3491–3502.
14Valentine, T. R. et al. Illness Perceptions and Psychological and Physical Symptoms in Newly Diagnosed Lung Cancer. Health Psychol. 2022 Jun; 41(6): 379–388.
15Andersen, B. L. et al. Newly diagnosed patients with advanced non-small cell lung cancer: A clinical description of those with moderate to severe depressive symptoms. Lung Cancer. 2020 Jul;145:195-204.
16Presley, C. J. et al. Functional Disability Among Older Versus Younger Adults With Advanced Non–Small-Cell Lung Cancer. JCO Oncol Pract. 2021 May 3;17(6):e848–e858.
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