Zongertinib

Not intended for UK and US media Therapy approved based on Phase Ib Beamion LUNG-1 trial data, demonstrating robust efficacy (75.7% objective response rate) in treatment-naïve patients1Expedited approval as an initial treatment in China follows U.S. accelerated approval for HERNEXEOS® (zongertinib tablets) in February, reflecting high recognition of urgency and unmet clinical need2This marks a new step in advancing targeted options for HER2 (ERBB2)-mutant NSCLC in China, where lung cancer is the leading cause of cancer death and the incidence and mortality rates have significantly increased in recent years3 Ingelheim, Germany – Boehringer Ingelheim’s HERNEXEOS® (zongertinib tablets) has been conditionally approved as monotherapy by China’s National Medical Products Administration (NMPA) as an initial treatment for adult patients with unresectable, locally advanced or metastatic non-small cell lung cancer (NSCLC) whose tumors have activating HER2 (ERBB2) tyrosine kinase domain (TKD) mutations.1 The approval is based on data demonstrating a 75.7% objective response rate, with full approval contingent on confirmation of clinical benefit in an ongoing trial. It represents another major milestone following the Breakthrough Therapy Designation (BTD) from the Center for Drug Evaluation (CDE) of China’s NMPA for first-line treatment.4 The therapy is also approved for patients in China who have received prior treatment.5 "In the past, patients with HER2‑mutant advanced non-small cell lung cancer faced significant diagnostic and treatment challenges in clinical practice. These challenges not only placed considerable physical and psychological burdens on patients but also limited the delivery of precise lung cancer treatment,” said Professor Yi-Long Wu from Guangdong Provincial People's Hospital, Chairman of the Chinese Thoracic Oncology Group (CTONG). “This advancement directly addresses patients’ core clinical needs for quality care." The approval is based on data from a cohort of treatment-naïve patients (N=74) in the Phase Ib Beamion LUNG-1 trial, which demonstrated an objective response rate (ORR) of 75.7%, including 10.8% achieving complete response (CR) and 64.9% achieving partial response (PR). The median duration of response (mDoR) was 15.2 months. Treatment-related adverse events (AEs) were predominantly low-grade. In a pooled safety population, which included 177 patients with HER2 (ERBB2)-mutant NSCLC in Beamion LUNG-1, AEs led to dose reductions in 9% of patients and dose discontinuations in 6% of patients. Data for treatment-naive patients were presented at the European Lung Cancer Congress 2026 (ELCC 2026) and published in The New England Journal of Medicine.6 “The first-line approval of HERNEXEOS in China marks an important step forward in our ambition to redefine the treatment of HER2-driven cancers,” said Shashank Deshpande, Chairman of the Board of Managing Directors at Boehringer Ingelheim. “Building on strong global momentum, including approvals in the U.S., and supported by compelling clinical evidence, we are advancing this therapy across various stages of disease and tumor types. This milestone reflects not only the progress we have made, but the broader opportunity ahead – to deliver unprecedented impact for people living with cancer, now and for generations to come.” About HER2 (ERBB2)-mutant non-small cell lung cancer (NSCLC) Lung cancer claims more lives than any other cancer type7 and the incidence is set to increase to over 3 million cases worldwide by 2040.8 NSCLC is the most common type of lung cancer.7 The condition is often diagnosed at a late stage9, and fewer than 3 in 10 patients are alive five years after diagnosis.9,10 People living with advanced NSCLC can experience a detrimental physical, psychological, and emotional impact on their daily lives.8,11,12 Up to 4% of lung cancers are driven by HER2 (ERBB2) mutations (or gene alterations).7 Mutations in HER2 can lead to overexpression and overactivation, which can in turn result in uncontrolled cell production, inhibition of cell death and promotion of tumor growth and spread.13 About HERNEXEOS® (zongertinib tablets) HERNEXEOS (zongertinib tablets) is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby minimizing associated toxicities. HERNEXEOS is approved in the U.S., China, Hong Kong and Japan as the first orally administered targeted therapy for adult patients with HER2 (ERBB2)-mutant advanced non-small cell lung cancer. Zongertinib is not approved in other markets. The treatment is being evaluated in ongoing trials across a range of earlier stages and advanced solid tumors with HER2 alterations. Beamion LUNG-2 is an ongoing Phase III controlled study evaluating zongertinib as an initial treatment for patients with advanced NSCLC that has HER2 tyrosine kinase domain mutations (NCT06151574). Beamion LUNG-3 is a Phase III clinical trial investigating zongertinib as an adjuvant monotherapy in patients with early-stage, resectable NSCLC (Stage II-IIIB) with HER2 (ERBB2)-mutations (NCT07195695). About Boehringer Ingelheim in oncology We have a clear aspiration – to transform the lives of people facing cancer by delivering unprecedented impact, with the ultimate goal to redefine standards of care. Boehringer Ingelheim’s long-term commitment to scientific innovation is reflected by the company’s robust pipeline of cancer cell-directed and immuno-oncology investigational therapies, as well as in smart combinations of these approaches. In everything we do, we focus on people — not just data — working alongside them to develop solutions that truly meet their needs and help move cancer into the background of their lives. This drives our research approach, drawing on diverse minds and a long-term perspective to address the needs of people facing cancer today and for generations to come. Read more at https://www.boehringer-ingelheim.com/human-health/cancer. About Boehringer IngelheimBoehringer 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 54,300 employees serve over 130 markets to build a healthier and more sustainable tomorrow. Learn more at www.boehringer-ingelheim.com. References HERNEXEOS Prescribing Information.U.S. Food and Drug Administration. FDA grants accelerated approval to zongertinib for unresectable or metastatic non-squamous non-small cell lung cancer. Available at: https://www.fda.gov/drugs/resources-information-approved-drugs/fda-grants-accelerated-approval-zongertinib-unresectable-or-metastatic-non-squamous-non-small-cell (Accessed: May 2026).Cao, M., Chen, W. Epidemiology of lung cancer in China. Thorac Cancer. 2019 Jan;10(1):3-7.Li J, Zhang H, Li X, et al. POSC187 Epidemiology of Lung Cancer in China: A Targeted Literature Review. Value in Health, 2022 Jan; 25(1);S137.Boehringer Ingelheim. Boehringer’s HERNEXEOS approved in China as first oral targeted therapy for previously treated patients with HER2-mutant advanced NSCLC. Available at: https://www.boehringer-ingelheim.com/human-health/cancer/lung-cancer/hernexeos-approved-china-targeted-therapy-nsclc (Accessed: May 2026).Heymach JV, Yamamoto N, Girard N, et al. First-Line Zongertinib in Advanced HER2-Mutant Non–Small-Cell Lung Cancer. N Engl J Med. 2026(394):1675-1684.Zeng J, Ma W, Young RB, Li T. Targeting HER2 genomic alterations in non-small cell lung cancer. J Natl Cancer Cent. 2021 May 3;1(2):58-73.Valentine, T. R. et al. Illness Perceptions and Psychological and Physical Symptoms in Newly Diagnosed Lung Cancer. Health Psychol. 2022 Jun; 41(6): 379–388.National 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: February 2026).Casal-Mouriño, A. et al. Epidemiology of stage III lung cancer: frequency, diagnostic characteristics, and survival. Transl Lung Cancer Res. 2021;10(1):506-518.Andersen, 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.Presley, 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.Galogre M, et al. A review of HER2 overexpression and somatic mutations in cancers, Critical Reviews in Oncology/Hematology, Volume 186, 2023, 103997.

Boehringer Ingelheim has received conditional approval from China’s National Medical Products Administration (NMPA) for zongertinib (Hernexeos) as a first-line monotherapy in adults with unresectable, locally advanced or metastatic HER2-mutant NSCLC, marking the first targeted oral therapy cleared for this population at initial diagnosis in China. The decision, based on a 75.7% objective response rate in treatment-naïve patients from the Phase Ib Beamion LUNG-1 trial, follows the drug’s US FDA accelerated approval in February 2026 and extends zongertinib’s regulatory footprint to the US, China, Hong Kong, and Japan. Beamion LUNG-1 is an open-label Phase Ib dose-escalation and expansion study evaluating zongertinib across HER2-aberrant solid tumors. The China NMPA approval drew on data from a cohort of 74 treatment-naïve patients with HER2 (ERBB2) tyrosine kinase domain activating mutations, in which zongertinib produced an ORR of 75.7%, comprising a 10.8% complete response rate and a 64.9% partial response rate. The median duration of response was 15.2 months. These data were presented at the European Lung Cancer Congress 2026 and published in the New England Journal of Medicine. In a pooled safety population of 177 patients with HER2-mutant NSCLC enrolled in Beamion LUNG-1, treatment-related adverse events were predominantly low-grade; dose reductions occurred in 9% of patients and dose discontinuations in 6%. The conditional approval requires confirmation of clinical benefit from an ongoing trial before full approval is granted. Competitive context Zongertinib is an irreversible TKI that selectively inhibits HER2 while sparing wild-type EGFR, a design intended to reduce the diarrhea and rash associated with pan-HER inhibitors. The primary approved alternative in HER2-mutant NSCLC is AstraZeneca and Daiichi Sankyo’s Enhertu (trastuzumab deruxtecan), an intravenous antibody-drug conjugate approved by the FDA in 2022 for previously treated patients; cross-trial comparisons are limited, but zongertinib’s 75.7% first-line ORR compares favorably in absolute terms to the roughly 37–38% ORR reported for trastuzumab deruxtecan in the second-line DESTINY-Lung02 setting, with the caveat that patient populations and trial designs differ materially. Bayer’s Hyrnuo (sevabertinib), a reversible oral HER2 TKI, received FDA accelerated approval in November 2025 for previously treated patients, adding a second oral option in the post-platinum setting. The confirmatory Phase III Beamion LUNG-2 trial, evaluating zongertinib as initial treatment in HER2 TKD-mutant advanced NSCLC, is ongoing and will provide the randomized data needed to support full approval in both China and the US. This article was generated with AI assistance and reviewed and edited by the AllSci editorial team Explore more at AllSci News: https://allsci.com/news/ Your email address will not be published. Required fields are marked * Comment * Name * Email * Website Privacy Terms About Us Copyright © 2026. AllSci Corp. All rights reserved.