RegulationPriority Review (United States), Breakthrough Therapy (United States), Fast Track (United States), Accelerated Approval (United States), Priority Review (China), Breakthrough Therapy (China), Conditional marketing approval (China), Orphan Drug (Japan)

Structure/Sequence

Molecular FormulaC29H29N9O2

InChIKeyYSGNGFPNTLERCR-UHFFFAOYSA-N

CAS Registry2728667-27-2

Clinical Trials associated with Zongertinib

NCT07195695

/ Not yet recruitingPhase 3

Beamion LUNG-3: A Randomized, Controlled, Multi-center Trial Evaluating Zongertinib as an Adjuvant Monotherapy Compared With Standard of Care in Patients With Early-stage, Resectable Non-small Cell Lung Cancer (Stage II-IIIB) Harboring Tyrosine Kinase Domain Activating HER2 Mutations

This study is open to adults 18 years and older who have early-stage non-small cell lung cancer (NSCLC). Their cancer must have a specific change in a gene called HER2. Genes provide the instructions for making proteins, and this change leads to a faulty HER2 protein. People can join if their lung cancer was removed by surgery, and they have already received certain other anti-cancer treatments. The purpose of this study is to find out if a study medicine called zongertinib helps people with this type of cancer live longer without their cancer coming back after surgery, when compared to standard treatment. Zongertinib is being developed to target the faulty HER2 protein, which can cause cancer cells to grow.
In this study, participants are assigned by chance to one of two treatment groups, with an equal chance of being in either group. One group takes the study medicine, zongertinib, by mouth once a day for up to 3 years. The other group receives a standard treatment, chosen by their doctor. This standard treatment may be an immunotherapy medicine given by infusion into a vein every 3 or 4 weeks for up to 1 year, or regular check-ups without active study medicine (observation).
Participants can be in this study for up to about 11 years. During this time, they visit the study site regularly for check-ups and study-related tests. The frequency of these visits varies depending on their treatment and how long they have been in the study. In addition to visits at the study site, participants in some treatment groups will also have phone calls with the study team every 3 weeks to check on their health between their scheduled visits.
Doctors check for any signs of cancer coming back using imaging scans (like CT or MRI scans); these scans are generally done every 3 months for the first 2 years, then every 6 months for the next 3 years, and then yearly. Participants also fill in questionnaires about their overall wellbeing, health and symptoms. Throughout the study, doctors also check participants' health and note any unwanted effects.

Start Date05 Dec 2025

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT06692322

/ CompletedPhase 1

Pharmacokinetics, Safety and Tolerability of Zongertinib Following Oral Administration in Male and Female Participants of Non-childbearing Potential With Different Degrees of Hepatic Impairment (Child-Pugh Classification A and B) Compared With Matched Male and Female Participants of Non-childbearing Potential With Normal Hepatic Function (an Open-label, Non-randomised, Single-dose, Parallel, Individual-matched Design Trial)

This study is open to adults between 18 and 80 years of age. People with a body mass index (BMI) between 18 and 42 kg/m^2 can take part. Women can only participate if they cannot get pregnant. This study includes people with mild liver problems, people with moderate liver problems, and people without liver problems as a matching control. The purpose of this study is to find out how mild and moderate liver problems affect how the body handles a medicine called zongertinib.
Participants take zongertinib once as tablets. Participants with liver problems are treated in a step-by-step approach with a few days in between for the doctors to review the data and make sure the participants can tolerate the treatment. Participants may continue their regular treatment for their liver problems during the study.
Participants are in the study for about 5 weeks. During this time, they visit the study site 4 times. This also includes an overnight stay for 6 nights. During study visits, the doctors regularly check participants' health and take note of any unwanted effects. To assess the study endpoints, the study staff regularly takes blood samples.

Start Date15 Jan 2025

Sponsor / Collaborator

Boehringer Ingelheim GmbH

CTR20242277

/ RecruitingPhase 1/2

Beamion BCGC-1：一项评价口服zongertinib（BI 1810631）单药或联合其他药物用于治疗晚期HER2+转移性乳腺癌（mBC）和转移性胃癌、食管胃结合部癌或食管腺癌（mGEAC）患者的Ib期剂量递增和II期剂量优化、随机、开放性、多中心临床研究

[Translation] Beamion BCGC-1: A Phase Ib, dose-escalation and Phase II, dose-optimization, randomized, open-label, multicenter study evaluating oral zongertinib (BI 1810631) alone or in combination with other agents in patients with advanced HER2+ metastatic breast cancer (mBC) and metastatic gastric, gastroesophageal junction, or esophageal adenocarcinoma (mGEAC)

本研究的目的是确定zongertinib与德曲妥珠单抗、恩美曲妥珠单抗或曲妥珠单抗（联合或不联合卡培他滨）联合治疗时对已扩散的不同类型HER2+癌症患者的最佳耐受剂量。另一个目的是检查zongertinib单药治疗或与其他治疗联合使用是否可以使肿瘤缩小。Zongertinib 能抑制HER2，而HER2 能促进癌细胞生长。

[Translation]

The goal of this study was to determine the best-tolerated dose of zongertinib in combination with trastuzumab dapoxetine, trastuzumab emtansine, or trastuzumab (with or without capecitabine) in patients with different types of HER2+ cancer that has spread. Another goal was to examine whether zongertinib, alone or in combination with other treatments, could shrink tumors. Zongertinib inhibits HER2, which drives cancer cell growth.

Start Date25 Oct 2024

Sponsor / Collaborator

Boehringer Ingelheim (China) Investment Co., Ltd.

[+5]

100 Clinical Results associated with Zongertinib

100 Translational Medicine associated with Zongertinib

100 Patents (Medical) associated with Zongertinib

Literatures (Medical) associated with Zongertinib

01 Nov 2025·CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

The development of Zongertinib for HER2-mutant NSCLC

Review

Author: Park, Cathleen J ; Brazel, Danielle ; Nagasaka, Misako

Human epidermal growth factor receptor 2 (HER2) mutations are rare in NSCLC and the only FDA approved agent until recently, was trastuzumab deruxtecan in the second line setting. HER2 mutated NSCLC has historically shown worse prognosis compared to other NSCLC and represent an unmet clinical need. Almost 50 % of patients with HER2-mutated non-small cell lung cancer (NSCLC) have brain metastases at diagnosis. Thus, developing an efficacious agent with good blood brain penetration is key. Zongertinib is a HER2 selective tyrosine kinase inhibitor that covalently binds to HER2 receptors, including exon20ins mutations. Zongertinib is safe and effective for patients with HER2-mutated NSCLC based on initial results from preclinical studies and the phase I Beamion LUNG-1 trial showing promising response rates and safety profile ultimately leading to the FDA accelerated approval on August 8, 2025.

28 Jul 2025·Cureus Journal of Medical Science

Targeted Therapy in HER2 Exon 20-Mutant Non-small Cell Lung Cancer With Leptomeningeal Disease: A Case-Based Approach to Treatment Decision-Making

Article

Author: Elzaafarany, Osama

A rare and clinically challenging case of leptomeningeal disease (LMD) secondary to HER2-mutated non-small cell lung cancer (NSCLC), marked by both exon 20 insertion and gene amplification, is presented. In the absence of LMD-specific therapeutic guidelines for HER2-driven NSCLC, treatment was initiated with trastuzumab deruxtecan (Enhertu), based on extrapolated evidence from clinical trials in systemic NSCLC and HER2-positive breast cancer with central nervous system involvement. The patient, a 69-year-old woman with good performance status, developed LMD following prior systemic therapy and local CNS treatments. MRI and CSF cytology confirmed the diagnosis. Given the lack of approved therapies for HER2-mutant NSCLC with LMD, the treatment strategy was informed by available clinical data and supporting literature on the CNS activity of Enhertu. Other options such as poziotinib and zongertinib were considered but not pursued. This case underscores the urgent need for inclusive clinical trials addressing CNS complications in molecularly defined NSCLC and demonstrates the real-world application of precision oncology beyond trial populations.

19 Jun 2025·NEW ENGLAND JOURNAL OF MEDICINE

Zongertinib in Previously Treated HER2 -Mutant Non–Small-Cell Lung Cancer

Article

Author: Yoh, Kiyotaka ; Zugazagoitia, Jon ; Sabari, Joshua K. ; Nadal, Ernest ; Eigenbrod-Giese, Sabina ; Wu, Yi-Long ; Heymach, John V. ; Smit, Egbert F. ; Sadrolhefazi, Behbood ; Cho, Byoung Chul ; Ahn, Myung-Ju ; von Wangenheim, Ute ; Planchard, David ; Girard, Nicolas ; Ruiter, Gerrina ; Zhao, Yanqiu ; Tu, Hai-Yan ; Rohrbacher, Maren ; Yamamoto, Noboru

BACKGROUND:

Innovative oral targeted therapies are warranted for patients with human epidermal growth factor receptor 2 (HER2)-mutant non-small-cell lung cancer (NSCLC). Zongertinib is an oral, irreversible, HER2-selective tyrosine kinase inhibitor that has been shown to have efficacy in persons with advanced or metastatic solid tumors with HER2 alterations in a phase 1 study.

METHODS:

We evaluated zongertinib in a multicohort, phase 1a-1b trial involving patients with advanced or metastatic HER2-mutant NSCLC. Here we report the primary analysis of zongertinib in previously treated patients: those with tumors harboring a mutation in the tyrosine kinase domain (cohort 1), those with tumors harboring a mutation in the tyrosine kinase domain previously treated with a HER2-directed antibody-drug conjugate (cohort 5), and those with tumors harboring a non-tyrosine kinase domain mutation (cohort 3). In cohort 1, patients were initially randomly assigned to receive zongertinib at a dose of 120 mg or 240 mg once daily. Patients in cohorts 5 and 3 initially received 240 mg daily. After an interim analysis of data from cohort 1, subsequently recruited patients across all cohorts received zongertinib at a dose of 120 mg. The primary end point was an objective response assessed by blinded independent central review (cohorts 1 and 5) or by investigator review (cohort 3). Secondary end points included the duration of response and progression-free survival.

RESULTS:

In cohort 1, a total of 75 patients received zongertinib at a dose of 120 mg. At the data cutoff (November 29, 2024), 71% of these patients (95% confidence interval [CI], 60 to 80; P<0.001 against a ≤30% benchmark) had a confirmed objective response; the median duration of response was 14.1 months (95% CI, 6.9 to not evaluable), and the median progression-free survival was 12.4 months (95% CI, 8.2 to not evaluable). Grade 3 or higher drug-related adverse events occurred in 13 patients (17%). In cohort 5 (31 patients), 48% of the patients (95% CI, 32 to 65) had a confirmed objective response. Grade 3 or higher drug-related adverse events occurred in 1 patient (3%). In cohort 3 (20 patients), 30% of the patients (95% CI, 15 to 52) had a confirmed objective response. Grade 3 or higher drug-related adverse events occurred in 5 patients (25%). Across all three cohorts, no cases of drug-related interstitial lung disease occurred.

CONCLUSIONS:

Zongertinib showed clinical benefit with mainly low-grade adverse events in patients with previously treated HER2-mutant NSCLC. (Funded by Boehringer Ingelheim; Beamion LUNG-1 ClinicalTrials.gov number, NCT04886804.).

News (Medical) associated with Zongertinib

03 Sep 2025

·www.prnewswire.com

FDA grants HERNEXEOS® Breakthrough Therapy Designation for first line use in HER2 (ERBB2)-mutant advanced NSCLC

Breakthrough Therapy Designation is based on results from the Beamion-LUNG 1 clinical trial evaluating HERNEXEOS® (zongertinib tablets) as a first-line treatment in HER2 (ERBB2)-mutant advanced NSCLC Follows recent accelerated approval of HERNEXEOS for previously treated patients with HER2 (ERBB2)-mutant advanced NSCLC from the U.S. Food and Drug Administration RIDGEFIELD, Conn., Sept. 3, 2025 /PRNewswire/ -- Boehringer Ingelheim today announced HERNEXEOS® (zongertinib tablets) has been granted Breakthrough Therapy Designation by the U.S. Food and Drug Administration (FDA) for first-line treatment of adult patients with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) whose tumors have HER2 (ERBB2) tyrosine kinase domain activating mutations. "Exploring accelerated review pathways is part of Boehringer's strategy to have an unprecedented and generational impact on people facing cancer. We are incredibly pleased that HERNEXEOS has received Breakthrough Therapy Designation for first-line use in patients living with HER2-mutant non-small cell lung cancer," said Vicky Brown, Senior Vice President and Head of Immunology, Oncology, and Eye Health, Boehringer Ingelheim. "This pathway was designed to expedite the development and review of promising medicines for serious diseases, and clearly highlights the potential of HERNEXEOS." Breakthrough Therapy Designation is given to expedite the development and review of medicines for serious conditions where preliminary clinical evidence indicates that the medicine may demonstrate substantial improvement over currently available therapies. HERNEXEOS was recently approved by the U.S. FDA for adult patients with unresectable or metastatic non-squamous NSCLC whose tumors have HER2 (ERBB2) tyrosine kinase domain (TKD) activating mutations, as detected by an FDA-approved test, and who have received prior systemic therapy. This indication is approved under accelerated approval based on objective response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial. Boehringer will present new and updated HERNEXEOS data at the upcoming World Conference on Lung Cancer (WCLC) in September and European Society for Medical Oncology (ESMO) in October. About HERNEXEOS® HERNEXEOS is an irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby limiting associated toxicities. Boehringer Ingelheim is investigating HERNEXEOS across a range of advanced solid tumors with HER2 alterations. The therapy was conditionally approved for use as a monotherapy by China's National Medical Products Administration (NMPA) for the treatment of adult patients with unresectable, locally advanced or metastatic NSCLC whose tumors have activating HER2 (ERBB2) mutations and who have received at least one line of prior systemic therapy. It also recently received Breakthrough Therapy Designation from the Center for Drug Evaluation (CDE) of China's NMPA for the first line treatment of adult patients with unresectable or metastatic NSCLC harboring activating mutations in the HER2 TKD. This orally administered, targeted therapy has also been granted Orphan Drug Designation in Japan. 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 2040.1,2 NSCLC is the most common type of lung cancer.3 Due to a lack of symptoms and misdiagnoses,4 most patients with NSCLC present at stage III or IV, where the disease has metastasized locally or to other organs.5 The estimated 5-year survival rate historically has been less than 10% for metastatic disease.6,7,8 People living with advanced NSCLC can experience a detrimental physical, psychological, and emotional impact on their daily lives.9,10,11 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. What is HERNEXEOS (zongertinib tablets)? HERNEXEOS is a prescription medicine used to treat adults with a type of lung cancer called non-squamous non-small cell lung cancer (NSCLC) that: cannot be removed by surgery or that has spread to other parts of your body (metastatic), and has a certain mutation in the human epidermal growth factor receptor 2 (HER2) gene, and who have previously received treatment by mouth or injection (systemic therapy). Your healthcare provider will perform a test to make sure HERNEXEOS is right for you. It is not known if HERNEXEOS is safe and effective in children. IMPORTANT SAFETY INFORMATION Before taking HERNEXEOS, tell your healthcare provider about all of your medical conditions, including if you: have liver problems. have heart problems. have lung or breathing problems other than lung cancer. are pregnant or plan to become pregnant. HERNEXEOS can harm your unborn baby. Females who are able to become pregnant: Your healthcare provider will do a pregnancy test before you start treatment with HERNEXEOS. Use an effective form of birth control (contraception) during treatment with HERNEXEOS and for 2 weeks after your last dose. Talk to your healthcare provider about birth control methods that might be right for you during this time. Tell your healthcare provider right away if you become pregnant or think you are pregnant during treatment with HERNEXEOS. are breastfeeding or plan to breastfeed. It is not known if HERNEXEOS passes into your breastmilk. Do not breastfeed during treatment and for 2 weeks after your last dose of HERNEXEOS. Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. HERNEXEOS may affect the way other medicines work, and other medicines may affect how HERNEXEOS works. Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine. What are the possible side effects of HERNEXEOS? HERNEXEOS may cause serious side effects, including: liver problems. Liver problems are common with HERNEXEOS and can be severe and life-threatening. Your healthcare provider will do blood tests to check your liver function before you start taking HERNEXEOS and during your treatment. Tell your healthcare provider right away if you develop any signs and symptoms of liver problems, including: yellowing of your skin or the white part of your eyes (jaundice) dark or brown (tea colored) urine pain on the upper right side of your stomach area (abdomen) bleeding or bruising more easily than normal feeling very tired loss of appetite nausea or vomiting heart problems that may affect your heart's ability to pump blood. HERNEXEOS can cause heart problems. Your healthcare provider will do tests to check your heart function before you start taking HERNEXEOS and during treatment. Tell your healthcare provider right away if you have any new or worsening symptoms of heart problems, including: feeling like your heart is pounding or racing dizziness tiredness feeling lightheaded shortness of breath loss of consciousness coughing swelling of your legs, ankles, or feet lung problems. HERNEXEOS can cause lung problems that are severe or life-threatening. Tell your healthcare provider right away if you have any new or worsening symptoms of lung problems, including trouble breathing, shortness of breath, cough, or fever. Your healthcare provider may temporarily stop, decrease your dose, or permanently stop treatment with HERNEXEOS if you have serious side effects. The most common side effects of HERNEXEOS include: diarrhea. HERNEXEOS can cause severe diarrhea. Tell your healthcare provider right away if you have diarrhea. liver problems rash feeling tired nausea The most common severe abnormal blood tests include decreased white blood cell count, increased liver function tests, and decreased potassium levels. HERNEXEOS may cause fertility problems in females and males, which may affect your ability to have children. Talk to your healthcare provider if this is a concern for you. These are not all of the possible side effects of HERNEXEOS. Call your doctor for medical advice about side effects. For more information, ask your healthcare provider or pharmacist. You are encouraged to report negative side effects of prescription drugs to the FDA. Visit or call 1‑800‑FDA‑1088. CL--100065 07.28.2025 For U.S. Healthcare Professionals, please see full Prescribing Information. MPR-US-103736 References: 1 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. 2 International Agency for Research on Cancer – World Health Organization. Rates of trachea, bronchus and lung cancer. Available at:  (Accessed: January 2025). 3 Baraibar I, et al. Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC. Crit Rev Oncol Hematol. 2020;148:102906. 4 American Cancer Society. Lung Cancer Early Detection, Diagnosis, and Staging. Available at: (Accessed: January 2025). 5 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. 6 National Cancer Institute Surveillance, Epidemiology, and End Results (SEER). 5-Year Survival Rates. (Accessed July 2025). 7 Belaroussi, 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. 8 Simeone, 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. 9 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. 10 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. 11 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. SOURCE Boehringer Ingelheim WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Breakthrough TherapyPhase 3Drug ApprovalOrphan DrugPhase 1

22 Aug 2025

·pmlive.com

Boehringer’s Hernexeos granted FDA accelerated approval for lung cancer patients

Boehringer Ingelheim’s Hernexeos (zongertinib) has been granted accelerated approval by the US Food and Drug Administration (FDA) to treat a subset of non-small cell lung cancer (NSCLC) patients. The kinase inhibitor has been authorised to treat unresectable or metastatic NSCLC in adults whose tumours have HER2 (ERBB2) tyrosine kinase domain activating mutations and who have previously received systemic therapy. Approximately 226,650 people are expected to be diagnosed with lung cancer in the US this year, with NSCLC accounting for around 87% of cases. HER2 (ERBB2) mutations affect up to 4% of NSCLC patients and are associated with a poor prognosis and higher incidence of brain metastases. Boehringer’s Hernexeos is designed to selectively inhibit HER2 (ERBB2) and is now the first orally administered targeted therapy approved by the FDA for this patient population, the company said. The US regulator’s decision was supported by results from the phase 1b Beamion-LUNG 1 trial, in which Hernexeos demonstrated an objective response rate (ORR) of 75% in patients who had received prior platinum-based chemotherapy but not a HER2-targeted tyrosine kinase inhibitor or antibody-drug conjugate (ADC), with 58% experiencing a duration of response (DOR) of at least six months. Among a smaller cohort of patients previously treated with platinum-based chemotherapy and a HER2-targeted ADC, ORR was 44% and 27% had a DOR of at least six months. Coordinating investigator for Beamion-LUNG 1, John Heymach, said: “With the approval of [Hernexeos], we have an effective, targeted, orally administered treatment option for patients with HER2 (ERBB2)-mutant NSCLC in the US that not only elicits a durable response but, importantly, has a manageable safety profile. “In a patient population where there are currently limited treatment options, this approval represents a significant advancement in cancer care.” In line with the FDA’s accelerated approval pathway, continued approval for Hernexeos in this indication may be contingent on the verification of clinical benefit in a confirmatory trial. Shashank Deshpande, chairman of the board of managing directors and head of human pharma at Boehringer Ingelheim, added: “We are grateful to be able to bring forward Hernexeos, which has the potential to reset the benchmark for those living with HER2-mutant advanced NSCLC, a condition associated with a particularly poor prognosis.”

Clinical ResultDrug ApprovalPhase 1Accelerated Approval

11 Aug 2025

·www.pharmaceutical-technology.com

Boehringer’s Hernexeos receives fast-tracked FDA approval

Boehringer Ingelheim’s oral tyrosine kinase inhibitor, Hernexeos, has received accelerated approval from the FDA. Image credit: create jobs 51 via Shutterstock.com. Boehringer Ingelheim has received fast-track approval from the US Food and Drug Administration (FDA) for its targeted therapy, Hernexeos (zongertinib tablets) , to treat non-small cell lung cancer (NSCLC). This approval succeeds the positive results of the Phase Ib Beamion-LUNG 1 trial (NCT04886804), with the oral tyrosine kinase inhibitor (TKI) demonstrating an objective response rate (ORR) of 75% in patients with HER2-positive NSCLC who had received prior lines of platinum-based chemotherapy. Its FDA approval makes it the first oral treatment for HER2-positive NSCLC. Hernexeos also triggered a duration of response (DOR) of more than six months in 58% of the 71 patients previously treated with chemotherapy alone, while 27% of the 34 individuals with prior exposure to chemotherapy and a HER2 targeted therapy experienced a DOR of this length. Impacting 2%-4% of patients diagnosed with NSCLC, HER2 mutations are associated with poor prognosis and a higher risk of brain metastasis, while treatment options are highly limited in this population. Due to Hernexeos’ potential to fulfil unmet needs in this indication, the FDA granted Boehringer priority review and breakthrough therapy designation last year. The therapy’s full approval will likely rely on verification of clinical benefit in a confirmatory trial. GlobalData Strategic Intelligence US Tariffs are shifting - will you react or anticipate? Don’t let policy changes catch you off guard. Stay proactive with real-time data and expert analysis. By GlobalData Learn more about Strategic Intelligence Dr John Heymach, co-ordinating investigator on the Beamion-LUNG 1 trial and chair of thoracic/head and neck medical oncology at the MD Anderson Cancer Centre, said: “The approval of zongertinib offers an effective and targeted treatment option for patients with HER2-mutant NSCLC in the US that not only elicits a durable response, but also has a manageable safety profile. “In a patient population where there are currently limited treatment options, this approval represents a significant advancement in cancer care.” HER2-targeted therapy race heats up Though the current standard of care (SoC) for patients with HER2-mutated NSCLC still revolves around a platinum-based chemotherapy regimen, physicians are increasingly prescribing targeted therapies to improve outcomes. A notable example of this is AstraZeneca and Daiichi Sankyo’s antibody-drug conjugate (ADC ) Enhertu (trastuzumab deruxtecan), which became the first HER2-targeting therapy to receive approval for NSCLC in 2022. Following its accelerated FDA approval, the drug has already reached blockbuster status – raking in $4.1bn in 2024 for the company, according to Pharmaceutical Technology ’s parent company, GlobalData. GlobalData predicts that the drug is on track to pull in $14.6bn by 2031, highlighting the lucrative nature of the targeted oncology market. However, Hernexeos has demonstrated a higher ORR of 75% compared with Enhertu’s 56% in the DESTINY-Lung02 trial. The TKI has also proved efficacious in patients who had previously received treatment with an ADC, suggesting that the TKI could absorb some of Enhertu’s market share. Looking ahead, the drug may also face competition from other targeted therapies currently in Phase III clinical trials, with GlobalData giving Bayer’s TKI sevabertinib a likelihood of approval (LoA) score of 81% in this indication. Pharmaceutical Technology Excellence Awards - The Benefits of Entering Gain the recognition you deserve! The Pharmaceutical Technology Excellence Awards celebrate innovation, leadership, and impact. By entering, you showcase your achievements, elevate your industry profile, and position yourself among top leaders driving pharmaceutical advancements. Don’t miss your chance to stand out—submit your entry today! Nominate Now

Drug ApprovalClinical ResultPhase 3Priority ReviewAccelerated Approval

100 Deals associated with Zongertinib

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
HER2 mutant non-small cell lung cancer	China	Boehringer Ingelheim International GmbH	26 Aug 2025
HER2-positive Non-squamous non-small cell lung cancer	United States	Boehringer Ingelheim Pharmaceuticals, Inc.	08 Aug 2025

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Non-small cell lung cancer stage IIIB	Phase 3	United States	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	China	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Japan	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Argentina	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Austria	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Belgium	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Brazil	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Canada	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Chile	Boehringer Ingelheim GmbH	05 Dec 2025
Non-small cell lung cancer stage IIIB	Phase 3	Denmark	Boehringer Ingelheim GmbH	05 Dec 2025

Clinical Result

Indication

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06075277 (CTgov)	Phase 1	-	16	Zongertinib (Zongertinib iCF Fed (Test (T)))	maidmsciew(xtiteqjrta) = mznivmwftf asebcoukyi (knexwbcpcr, NA) View more	-	22 Sep 2025
				Zongertinib (Zongertinib iCF Fasted (Reference (R)))	maidmsciew(xtiteqjrta) = zhdelowkoz asebcoukyi (knexwbcpcr, NA) View more
NCT05879991 (CTgov)	Phase 1	-	15	zongertinib (C-14) (Part A - Zongertinib (C-14) (T1))	pjqknngxss(vkwvvsgsey) = pkbmjcewtr fzmrcmbobr (sbktzsqbjj, 16.8) View more	-	22 Sep 2025
				zongertinib (C-14) (Part B - Zongertinib (T2), Then Zongertinib (C-14) (R))	vsobnknmuo(krjoztwfmk) = aaaboubkrj qlvqzojrol (dnsxapszov, NA) View more
NCT06360081 (CTgov)	Phase 1	-	56	Zongertinib (Zongertinib Test Treatment (T))	ulqfbjarqm(kmwgtjezqt) = xrkvgxqpmh sbyafigyxo (napvlfrbht, NA) View more	-	22 Sep 2025
				Zongertinib (Zongertinib Reference Treatment (R))	ulqfbjarqm(kmwgtjezqt) = uhjblsethq sbyafigyxo (napvlfrbht, NA) View more
NCT05833139 (CTgov)	Phase 1	-	16	Zongertinib (Zongertinib Alone)	yfeeesbdpf(gdtavxowyg) = zupcthweis pkrkmknnkb (xbcemtefeb, NA) View more	-	22 Sep 2025
				Itraconazole+Zongertinib (Zongertinib + Itraconazole)	yfeeesbdpf(gdtavxowyg) = rsykndturx pkrkmknnkb (xbcemtefeb, NA) View more
NCT04886804 (Beamion LUNG-1, WCLC2025) Manual	Phase 1	HER2 mutant non-small cell lung cancer Second line \| Last line \| Third line HER2-mutant	75	Zongertinib 120 mg (stable/asymptomatic BMs at baseline)	grcydhknko(bxazxclair) = latsydztqh qowodwcblp (doddtfrlcq, 46 - 79) View more	Positive	09 Sep 2025
				Zongertinib 120 mg (without BMs at baseline)	grcydhknko(bxazxclair) = ayqscgmxuf qowodwcblp (doddtfrlcq, 61 - 85) View more
NCT04886804 (Beamion LUNG-1, FDA_CDER) Manual	Phase 1	HER2-positive Non-squamous non-small cell lung cancer ERBB2 Mutation (Activating)	71	HERNEXEOS	rcqfbamrsz(scozsybimj) = tvtrcgnhpg ppgqbvfjqi (dfxvtujcic, 63 - 83) View more	Positive	08 Aug 2025
				HERNEXEOS (previous treatment with platinum-based chemotherapy and a HER2-targeted ADC)	rcqfbamrsz(scozsybimj) = psibznlifl ppgqbvfjqi (dfxvtujcic, 29 - 61) View more
NCT04886804 (Beamion LUNG-1, Pubmed \| N Engl J Med)	Phase 1	Liver metastases \| Neoplasm Metastasis \| Metastatic Solid Tumor ... HER2 View more	-	Zongertinib 120 mg	hjineiapgy(rypwtrjhxj) = ewuoxbkuyp hvqvytrern (csggnpuxac, 60 - 80) View more	Positive	19 Jun 2025
				HER2-directed antibody-drug conjugate	hjineiapgy(rypwtrjhxj) = eymwffbvpd hvqvytrern (csggnpuxac, 32 - 65)
NCT04886804 (Phase Ia dose escalation/expansion trial, ASCO2025)	Phase 1	HER2-negative breast cancer HER2	121	Zongertinib	dfbxfekgmw(nujsugxexm) = The MTD was not reached dynqpspfcm (otwhdfamly )	Positive	30 May 2025
				Tucatinib
Phase I study (AACR2025)	Phase 1	HER2 mutations	-	Zongertinib 60 mg (C-14)-zongertinib solution	dupvissatl(ndbufhipab) = tncevpwqxe gcochvfahz (jhywpbvgyo ) View more	Positive	29 Apr 2025
				Zongertinib 60 mg film-coated tablet	dntpugqihz(sgrxsfcann) = oydwrsmrqu ylizrqjyye (jmtqndrwcf )
NCT04886804 (Beamion LUNG-1, GlobeNewswire \| Pubmed \| AACR2025) Manual	Phase 1	HER2 mutant non-small cell lung cancer ERBB2 Mutation (Activating)	126	Zongertinib (cohort 1; pretreated HER2-mutant NSCLC within the TKD)	gybhygscxf(wixpjnaldo) = zewseptsbk lfrgttnhfw (jnejpissuo, 60 - 80) View more	Positive	28 Apr 2025
				Zongertinib (cohort 3; pretreated HER2-mutant NSCLC with TKD or non-TKD mutations)	gybhygscxf(wixpjnaldo) = qsgjshqdsz lfrgttnhfw (jnejpissuo, 15 - 52) View more

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