On May 21, Sino Biopharmaceutical (1177.HK) and Boehringer Ingelheim jointly announced that Hernexeos^® (generic name in Chinese: zongertinib tablets, generic name in English: zongertinib), which they are co-promoting in mainland China, has been approved by the China National Medical Products Administration (NMPA). It is approved as a monotherapy for the first-line treatment of adult patients with unresectable locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring HER2 (ERBB2) tyrosine kinase domain activating mutations. This approval is another major milestone following the first-line indication of Hernexeos^® receiving Breakthrough Therapy Designation from the Center for Drug Evaluation (CDE) of the NMPA, and its approval by the NMPA in August 2025 for the treatment of previously treated patients. 

 

As the world's first approved oral HER2 tyrosine kinase inhibitor, the approval of Hernexeos^®'s first-line indication marks a new era of precision targeted first-line therapy for HER2-mutant advanced NSCLC in China. It ends the long-standing lack of efficient and precise targeted drugs for the first-line treatment of this patient population, while its oral administration method also offers greater convenience for patients.

 
The conditional approval of Hernexeos^®'s first-line indication in China is based on the results of the Phase 1b Beamion-LUNG 1 Cohort 2 clinical trial ^[1]. This trial evaluated the efficacy and safety of zongertinib in treatment-naive patients with advanced non-small cell lung cancer (NSCLC) harboring HER2 (ERBB2) activating mutations. Data showed that among the treatment-naive patients in Cohort 1 who received treatment (N=74), the confirmed objective response rate (ORR) was 76%, with 11% of patients achieving a complete response and 65% achieving a partial response. The median duration of response (mDoR) was 15.2 months, and the median progression-free survival (mPFS) was 14.4 months. These data were reported at the European Lung Cancer Congress 2026 (ELCC 2026), and the study results have also been simultaneously published in the New England Journal of Medicine. Furthermore, the article reported data on 30 patients with HER2-mutant advanced non-small cell lung cancer and active brain metastases, 47% of whom achieved a confirmed intracranial objective response (iORR) based on the Response Assessment in Neuro-Oncology-Brain Metastases (RANO-BM) criteria. 

 

The incidence of HER2 mutations in non-small cell lung cancer is approximately 2%-4% ^[2]. These mutations are more common in women, non-smokers, patients with lung adenocarcinoma, and younger populations. They are associated with high tumor invasiveness, a high risk of brain metastasis, and extremely poor patient prognosis ^[3,4]. For a long time, they have been considered one of the "refractory subtypes" among known driver genes ^[5]. In clinical diagnosis and treatment, the core pain points for these patients are particularly prominent: a long-term lack of targeted oral drugs, limited efficacy of traditional chemotherapy regimens ^[6] with significant toxic side effects, low response rates to immunotherapy, making it difficult to achieve effective tumor control. At the same time, existing treatment methods often have issues such as inconvenient administration and poor treatment adherence. They are also ineffective in controlling brain metastases and cannot effectively delay disease progression, leading to poor quality of life and shortened survival for patients. Their urgent clinical treatment needs have long been unmet. 

 

Professor Wu Yilong

Chairman of the Chinese Thoracic Oncology Group (CTONG)

Professor from Guangdong Provincial People's Hospital

 

"From the perspective of clinical practice, the multiple diagnostic and therapeutic pain points previously faced by patients with HER2-mutant advanced NSCLC not only subjected patients to dual physical and psychological stress but also became a key bottleneck restricting the development of precision therapy for lung cancer. The successful approval of zongertinib's first-line indication provides crucial support for breaking this dilemma. It completely breaks the treatment dilemma for these patients in the initial treatment phase, allowing them to escape the limitations of traditional treatment plans and obtain more targeted, convenient, and safer precision therapy options early in their treatment. This not only helps patients effectively extend their survival but also significantly reduces the physical discomfort and psychological burden of treatment, allowing them to maintain a good quality of life during the process. It truly achieves the leap from "having a drug to treat" to "having a good drug accessible", precisely responding to the core demands of clinical patients for high-quality treatment and long-term survival."

 

Chen Wenhan

General Manager of Human Pharma, Boehringer Ingelheim Greater China

 

"From the very beginning of its R&D, Hernexeos^® has focused on the most pressing clinical gap in the field of HER2-mutant non-small cell lung cancer, with the core orientation of filling the treatment void and meeting patient needs. As the world's first oral HER2-Tyrosine Kinase Inhibitor (TKI) drug, the successful approval of this first-line indication effectively addresses the clinical pain point of a long-term lack of first-line oral targeted drugs in the field of HER2-mutant non-small cell lung cancer, providing patients with a more convenient and targeted treatment option. Boehringer Ingelheim will always uphold the core philosophy of ‘patient-centricity.’ In the future, we will continue to focus on the high unmet clinical needs in the oncology field, work with all parties in the industry to accelerate the accessibility of innovative drugs, and promote the faster and wider benefit of cutting-edge medical achievements for Chinese patients."

 

Eric Tse

Chief Executive Officer of Sino Biopharma, Chairman of Chia Tai Tianqing

 

"The smooth approval of Hernexeos^®'s first-line indication is an important milestone in our strategic cooperation with Boehringer Ingelheim. It breaks the long-standing bottleneck of a lack of precision targeted drugs for these patients and also marks the official entry of HER2-mutant advanced non-small cell lung cancer in China into a new era of precision targeted first-line therapy. Sino Biopharmaceutical will continue to leverage its profound accumulation and exclusive resources in the anti-tumor field to fully enhance the accessibility of innovative good medicines and support the high-quality upgrading of domestic lung cancer diagnosis and treatment standards."

 

About HER2 (ERBB2)-Mutant Non-Small Cell Lung Cancer (NSCLC)

 

Lung cancer is one of the deadliest types of malignant tumor worldwide ^[7], with non-small cell lung cancer (NSCLC) being the most common type. HER2 (ERBB2) mutations account for about 2–4% of non-small cell lung cancers and are typically associated with a poor prognosis and a higher incidence of brain metastasis ^[8]. Abnormal changes in HER2 (ERBB2) (including mutations, amplification, and overexpression) can trigger abnormal cell proliferation, inhibit cell apoptosis, and promote tumor growth and spread ^[9,10]. Traditional chemotherapy and immunotherapy are not very effective in the HER2-mutant population ^[7]. Antibody-drug conjugates (ADCs) have shown some efficacy in this field, but they require intravenous administration and carry risks of potential adverse events such as myelosuppression and interstitial lung disease ^[6,10]. Therefore, patients with HER2-mutant advanced NSCLC still face significant unmet therapeutic needs and are in urgent need of an efficient, safe, and orally convenient precision targeted therapy drug. 

 

About Hernexeos^® (zongertinib tablets)

 

Hernexeos^® (zongertinib tablets) is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 (ERBB2) while sparing wild-type EGFR, which helps to reduce related toxic reactions,. Genetic testing can identify patients with advanced non-small cell lung cancer with HER2 (ERBB2) mutations to determine their suitability for treatment with Hernexeos^{® [8,11]}. 

 

About the Beamion Clinical Trials

 

BEAMION LUNG-1 (NCT04886804) is an open-label, Phase I dose-escalation clinical trial of zongertinib monotherapy for patients with unresectable or metastatic solid tumors harboring HER2 mutations, which includes dose confirmation and expansion. The trial is divided into two parts: the first part enrolls adult patients with various types of advanced cancer who have failed previous treatments and have HER2 gene aberrations (including mutations, amplification, overexpression, and fusion). The second part enrolls patients with HER2-mutant non-small cell lung cancer. BEAMION LUNG-2 is a Phase III, open-label, randomized, active-controlled study intended to enroll 270 patients with unresectable or metastatic non-squamous NSCLC harboring HER2 tyrosine kinase domain mutations, aiming to evaluate the efficacy of zongertinib compared to standard of care. 

 

About the Strategic Cooperation between Boehringer Ingelheim and Sino Biopharmaceutical

 

Boehringer Ingelheim and Sino Biopharmaceutical have established a strategic partnership dedicated to bringing innovative oncology therapies to the mainland China market. This collaboration will leverage the complementary strengths of both parties to provide more and better treatment options for cancer patients in China. The two parties will collaborate on multiple innovative oncology products from Boehringer Ingelheim that are in late-stage clinical development. Zongertinib is one of the strategic collaboration products between Boehringer Ingelheim and Sino Biopharmaceutical in mainland China. 

 

References:

[1] The New England Journal of Medicine, "Zongertinib for First-Line Treatment of HER2-Mutant Advanced Non-Small Cell Lung Cancer" Key results from the Beamion LUNG-1 Phase 1b clinical trial

[2] Guan Guohui, Jia Bo, Li Sheng, et al. Research Progress in Diagnosis and Treatment of HER2-Positive Non-Small Cell Lung Cancer [J]. Cancer, 2025, 44(6):314-327. 

[3] Trillo Aliaga P, Spitaleri G, Attili I, et al.HER2 in Non-Small Cell Lung Cancer (NSCLC): Evolution of the Therapeutic Landscape and Emerging Drugs-A Long Way to the Top.Molecules.2025.30(12): 2645.

[4] Heymach JV, Opdam F, Barve M, et al.HER2-Selective Tyrosine Kinase Inhibitor, Zongertinib (BI 1810631), in Patients With Advanced/Metastatic Solid Tumors With HER2 Alterations: A Phase Ia Dose-Escalation Study.J Clin Oncol.2025.43(11): 1337-1347.

[5] Heymach JV, Ruiter G, Ahn MJ, et al.Zongertinib in Previously Treated HER2-Mutant Non-Small-Cell Lung Cancer.N Engl J Med. 2025.392(23): 2321-2333.

[6] Zhang Liang, Yang Changliang, Li Peidong, Cheng Ying. Research Progress on HER-2 Mutant Advanced Non-Small Cell Lung Cancer. Cancer Research on Prevention and Treatment. 52(02): 87-92.

[7] Zeng J, Ma W, Young RB, Li T. Targeting HER2 genomic alterations in non-small cell lung cancer.J Natl Cancer Cent.2021;1(2):58-73.

[8] Baraibar I, et al.Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC.Crit Rev Oncol Hematol.2020;148:102906.

[9] Li BT, Smit EF, Goto Y, et al.Trastuzumab Deruxtecan in HER2-Mutant Non-Small-Cell Lung Cancer.N Engl J Med. 2022.386(3): 241-251.

[10] HERNEXEOS Prescribing Information.

[11] Wilding B, Woelflingseder L, Baum A, et al.Zongertinib (BI 1810631), an Irreversible HER2 TKI, Spares EGFR Signaling and Improves Therapeutic Response in Preclinical Models and Patients with HER2-Driven Cancers.Cancer Discov.2025;15(1):119-138.

 

Declaration:

1. This press release is intended to facilitate the communication and exchange of medical information and is for reference by healthcare professionals only. It is not for advertising purposes. 

2. The company does not recommend any drugs and/or indications. 

3. The information contained in this press release is for reference only and cannot replace professional medical guidance in any way, nor should it be considered as a diagnosis or treatment recommendation. If you wish to understand specific disease diagnosis and treatment information, please follow the advice or guidance of a physician or other healthcare professional.