Boehringer Ingelheim secures NMPA approval for HERNEXEOS® in HER2-mutant NSCLC with 71% response rate in Beamion-LUNG 1

Boehringer Ingelheim secures NMPA approval for HERNEXEOS® in HER2-mutant NSCLC with 71% response rate in Beamion-LUNG 1

(IN BRIEF) Boehringer Ingelheim’s HERNEXEOS® (zongertinib tablets) has received accelerated approval in China for patients with advanced NSCLC carrying HER2 mutations who have progressed after prior therapy. The approval is supported by Beamion-LUNG 1 data, which showed a 71% objective response rate, 14.1 months median duration of response, and a 12.4-month median progression-free survival. The therapy recently gained Breakthrough Therapy Designation in China for first-line use and has demonstrated a manageable safety profile. Experts highlight that zongertinib is the first well-tolerated oral HER2-targeted treatment for NSCLC, offering a much-needed new option. Boehringer Ingelheim plans to expand its clinical program to other HER2-driven cancers, further positioning zongertinib as a potential new standard in oncology.

(PRESS RELEASE) INGELHEIM, 1-Sept-2025 — /EuropaWire/ — Boehringer Ingelheim has announced that HERNEXEOS® (zongertinib tablets) has been granted accelerated approval by China’s National Medical Products Administration (NMPA). The treatment is approved as monotherapy for adult patients with unresectable, locally advanced, or metastatic non-small cell lung cancer (NSCLC) whose tumors carry activating HER2 (ERBB2) mutations and who have already received at least one prior systemic therapy.

The decision by the NMPA is based on results from the Phase Ib Beamion-LUNG 1 trial, which demonstrated an objective response rate (ORR) of 71% among 75 patients. Notably, 7% achieved complete responses, with nearly all patients (96%) reaching disease control. The trial also reported a median duration of response of 14.1 months and median progression-free survival of 12.4 months, confirming the potential of zongertinib to deliver long-lasting benefit. These findings were presented at the AACR Annual Meeting 2025 and published in The New England Journal of Medicine.

HERNEXEOS® has shown a manageable safety profile, with a low discontinuation rate of 2.9%. Its approval follows the therapy’s designation as a Breakthrough Therapy and Priority Review in China, recognizing the unmet need for effective HER2-targeted treatments in NSCLC.

Professor Wu Yilong of Guangdong Provincial People’s Hospital and Chairman of the Chinese Thoracic Oncology Group (CTONG), welcomed the approval, stating: “The lack of a tolerable oral drug targeting HER2 mutations has been a major challenge for patients with NSCLC. Zongertinib sets a new benchmark, offering a highly effective targeted option for patients with very limited choices.”

The therapy has also received Breakthrough Therapy Designation in China for first-line use, reflecting its potential to transform outcomes for patients with advanced HER2-mutant NSCLC. As an irreversible tyrosine kinase inhibitor (TKI), zongertinib selectively inhibits HER2 while sparing wild-type EGFR, minimizing associated toxicities.

Shashank Deshpande, Chairman of the Board of Managing Directors at Boehringer Ingelheim, commented: “The NMPA’s decision highlights the urgent need for HER2-targeted therapies in NSCLC and strengthens our conviction in zongertinib’s potential. Building on the strong clinical evidence, we are now exploring its use in other HER2-driven cancers, including breast cancer and in tumor-agnostic indications.”

NSCLC accounts for around 85% of lung cancer cases, and HER2 mutations are found in 2–4% of cases, often linked with poor prognosis and brain metastases. With lung cancer the leading cause of cancer deaths in China, this approval represents an important milestone in addressing a critical unmet need.

Zongertinib has already received regulatory approvals in both the U.S. and China, and Orphan Drug Designation in Japan. The broader Beamion clinical program continues with Beamion-LUNG 2, a Phase III trial comparing zongertinib with standard of care in 416 patients with HER2-mutant NSCLC.

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

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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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