RegulationPriority Review (United States), Breakthrough Therapy (United States), Fast Track (United States), Breakthrough Therapy (China), Orphan Drug (Japan), Priority Review (China)

Structure/Sequence

Molecular FormulaC29H29N9O2

InChIKeyYSGNGFPNTLERCR-UHFFFAOYSA-N

CAS Registry2728667-27-2

Clinical Trials associated with Zongertinib

NCT06692322

/ RecruitingPhase 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）联合德曲妥珠单抗（T-DXd）静脉给药或联合恩美曲妥珠单抗（T-DM1）静脉给药用于治疗晚期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) in combination with intravenous trastuzumab dexmedetomidine (T-DXd) or intravenous trastuzumab emtansine (T-DM1) 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与德曲妥珠单抗或恩美曲妥珠单抗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与T-DXd或T-DM1联合使用是否可以使肿瘤缩小。Zongertinib 抑制 HER2。HER2 导致癌细胞生长。

[Translation]

The goal of this study is to determine the best tolerated dose of zongertinib when combined with either trastuzumab dextran or trastuzumab emtansine for people with different types of HER2+ cancer that has spread. Another goal is to check whether zongertinib combined with T-DXd or T-DM1 can shrink tumors. Zongertinib inhibits HER2. HER2 causes cancer cells to grow.

Start Date25 Oct 2024

Sponsor / Collaborator

Boehringer Ingelheim (China) Investment Co., Ltd.

[+5]

NCT06581432

/ RecruitingPhase 2

Beamion PANTUMOR-1: A Phase II, Multicentre, Multicohort, Open-label Trial to Evaluate the Efficacy and Safety of Oral Zongertinib (BI 1810631) for the Treatment of Selected HER2-mutated or Overexpressed/Amplified Solid Tumours

This is a study for people with advanced cancer for whom previous treatment was not successful. Adults aged 18 and over with advanced cancer with HER2 alterations can join the study. The purpose of this study is to find out whether a medicine called zongertinib helps people with advanced cancers with HER2 alterations. HER2 alterations can cause cancer. Zongertinib inhibits HER2.
Participants are put into 13 groups based on the type of advanced cancer and the type of HER2 alterations they have. All participants take one dose of zongertinib each day. Participants can continue the treatment as long as they benefit from it and can tolerate it.
Participants visit the study site regularly. During many of the visits, the doctors check the size of the tumour and whether it has spread to other parts of the body. During all the visits, the doctors check participants' health and take note of any unwanted effects.

Start Date11 Oct 2024

Sponsor / Collaborator

C.H. Boehringer Sohn AG & Co. KG

100 Clinical Results associated with Zongertinib

100 Translational Medicine associated with Zongertinib

100 Patents (Medical) associated with Zongertinib

Literatures (Medical) associated with Zongertinib

10 Apr 2025·JOURNAL OF CLINICAL ONCOLOGY

HER2-Selective Tyrosine Kinase Inhibitor, Zongertinib (BI 1810631), in Patients With Advanced/Metastatic Solid Tumors With HER2 Alterations: A Phase Ia Dose-Escalation Study

Article

Author: Serra, Josep ; Schröter, Lukas ; Yoh, Kiyotaka ; Sadrolhefazi, Behbood ; Barve, Minal ; Heymach, John V. ; Wu, Yi-Long ; Berz, David ; Botilde, Yanick ; Yamamoto, Noboru ; Opdam, Frans ; Tu, Hai-Yan

PURPOSE:

Human epidermal growth factor receptor 2 (HER2) alterations occur in many solid cancers, including non–small cell lung cancer (NSCLC). Beamion LUNG-1 (ClinicalTrials.gov identifier: NCT04886804 ) is assessing the safety/efficacy of zongertinib (BI 1810631), a novel HER2-selective tyrosine kinase inhibitor that spares epidermal growth factor receptor, in patients with HER2-altered solid tumors.

MATERIALS AND METHODS:

Beamion LUNG-1 is an ongoing multicenter, multicohort phase Ia/Ib trial. Phase Ia assessed zongertinib administered twice a day (15-150 mg) or once daily (60-360 mg) in pretreated patients with various tumors, including NSCLC. Primary end points were maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs); tumor response was a secondary end point.

RESULTS:

As of May 23, 2024, 105 patients were treated. Two DLTs occurred during the MTD evaluation period; MTD was not reached (NR). The recommended doses for expansion were 120 mg once daily and 240 mg once daily. Treatment-related adverse events (TRAEs; any/grade ≥3) occurred in 82%/10% of patients. The most common TRAEs (any/grade ≥3) included diarrhea (50%/1%), rash (16%/2%), anemia (10%/0%), decreased appetite (10%/1%), and increased alanine transaminase (10%/4%). The confirmed investigator-assessed overall response rate (ORR) across all doses/tumors was 30% (95% CI, 23 to 40); median duration of response was 12.7 months (95% CI, 6.9 to NR). In 54 patients with NSCLC, confirmed ORR was 35% (95% CI, 24 to 49). Activity was observed in patients with A775_G776insYVMA (ORR, 38%) and those who had received previous HER2-directed therapy (ORR, 28%). In patients with NSCLC receiving zongertinib once daily, median progression-free survival was 17.2 months (95% CI, 8.3 to NR).

CONCLUSION:

Zongertinib had a manageable safety profile and demonstrated preliminary antitumor activity in patients with HER2-altered tumors, including those with HER2 -mutant NSCLC.

01 Feb 2025·PHARMACOTHERAPY

The effect of carbamazepine, a strong CYP3A inducer, on the pharmacokinetics of zongertinib in healthy male volunteers

Article

Author: Chan, Tom S. ; Roessner, Philipp M. ; Minich, David ; Esmaeili, Habib ; Wind, Sven ; Gan, Guanfa ; Grempler, Rolf ; Sadrolhefazi, Behbood ; Seitz, Friedeborg ; Tian, Xiaofan ; Müller, Fabian ; Mahmoudi, Mazyar

Abstract:

Introduction:

Zongertinib (BI 1810631) is a potent, selective, and epidermal growth factor receptor (EGFR) wild‐type sparing human epidermal growth factor receptor 2 (HER2) inhibitor. Based on in vitro data, the oxidative hepatic metabolism of zongertinib is principally driven by cytochrome P450 (CYP) 3A4/5. Therefore, zongertinib may be affected by strong CYP3A inducers, like carbamazepine.

Objective:

This study aimed to investigate the effect of multiple oral doses of carbamazepine on the pharmacokinetics of a single oral dose of zongertinib in healthy male subjects.

Methods:

This open‐label, two‐period, fixed‐sequence clinical drug–drug interaction study examined the pharmacokinetics of a single 60‐mg oral dose of zongertinib in the absence or presence of multiple oral doses of carbamazepine. The extent of drug–drug interaction was estimated using the adjusted geometric mean ratios (and 90% confidence intervals [CIs]) for the test treatment (zongertinib in the presence of carbamazepine) versus the reference treatment (zongertinib alone) for areas under the plasma concentration–time curve from time 0 to infinity and to the last quantifiable time point (AUC0–∞, AUC0–tz) and maximum measured plasma concentration (Cmax).

Results:

Sixteen subjects (all Caucasian males) received zongertinib alone in Study Period 1, and 15 of them received both zongertinib and carbamazepine in Study Period 2. Upon co‐administration with carbamazepine in Study Period 2, AUC0–∞ and AUC0–tz of zongertinib were both reduced to 36.5% (90% CI: 32.0%–41.6% for AUC0–∞ and 31.9%–41.7% for AUC0–tz). The Cmax of zongertinib was reduced to 56.4% (90% CI: 45.1%–70.6%).

Conclusion:

Zongertinib exposure was reduced by 63.5% when coadministered with the strong CYP3A inducer, carbamazepine.

13 Jan 2025·Cancer Discovery

Zongertinib (BI 1810631), an Irreversible HER2 TKI, Spares EGFR Signaling and Improves Therapeutic Response in Preclinical Models and Patients with HER2-Driven Cancers

Article

Author: Obenauf, Anna C. ; Chylinski, Krzysztof ; Solca, Flavio ; Baum, Anke ; Gibson, Neil ; Yamamoto, Noboru ; Woelflingseder, Lydia ; Kraut, Norbert ; Augsten, Martin ; Neumüller, Ralph A. ; Scharn, Dirk ; Ikegami, Masachika ; Popow, Johannes ; Gerlach, Daniel ; Kondo, Shunsuke ; Kohsaka, Shinji ; Waizenegger, Irene C. ; Bruining, Annemarie ; Spreitzer, Fiona ; Tilandyová, Sylvia ; Wilding, Birgit ; Pearson, Mark A. ; Vainorius, Gintautas ; Shirai, Yukina ; Opdam, Frans L. ; Heymach, John V.

Abstract:

Mutations in ERBB2 (encoding HER2) occur in 2% to 4% of non–small cell lung cancer (NSCLC) and confer poor prognosis. ERBB-targeting tyrosine kinase inhibitors, approved for treating other HER2-dependent cancers, are ineffective in HER2-mutant NSCLC due to dose-limiting toxicities or suboptimal potency. We report the discovery of zongertinib (BI 1810631), a covalent HER2 inhibitor. Zongertinib potently and selectively blocks HER2, while sparing EGFR, and inhibits the growth of cells dependent on HER2 oncogenic driver events, including HER2-dependent human cancer cells resistant to trastuzumab deruxtecan. Zongertinib displays potent antitumor activity in HER2-dependent human NSCLC xenograft models and enhances the activities of antibody–drug conjugates and KRASG12C inhibitors without causing obvious toxicities. The preclinical efficacy of zongertinib translates in objective responses in patients with HER2-dependent tumors, including cholangiocarcinoma (SDC4–NRG1 fusion) and breast cancer (V777L HER2 mutation), thus supporting the ongoing clinical development of zongertinib.Significance: HER2-mutant NSCLC poses a challenge in the clinic due to limited options for targeted therapies. Pan-ERBB blockers are limited by wild-type EGFR–mediated toxicity. Zongertinib is a highly potent and wild-type EGFR–sparing HER2 inhibitor that is active in HER2-driven tumors in the preclinical and clinical settings.

News (Medical) associated with Zongertinib

22 May 2025

·www.prnewswire.com

Boehringer Ingelheim Showcases Bold Vision for the Future of Cancer Care at ASCO 2025

Data to be presented at ASCO reflect Boehringer's broad pipeline and growing body of evidence supporting innovative therapies for various cancers Patient-reported outcomes from the Beamion LUNG-1 study in previously treated patients with HER2 (ERRB2)-mutant advanced non-small cell lung cancer (NSCLC) reported physical function and disease-related symptom improvement while being treated with zongertinib1 New data from a study of T-cell engager, obrixtamig, show encouraging findings in the treatment of extrapulmonary neuroendocrine carcinomas in patients with high DLL3 expression2 RIDGEFIELD, Conn., May 22, 2025 /PRNewswire/ --Boehringer Ingelheim will present the latest data in its robust oncology pipeline at the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting, including patient-reported outcomes (PRO) from the Beamion LUNG-1 study evaluating zongertinib as an orally administered targeted therapy for previously treated patients with HER2 (ERBB2)-mutant advanced non-small cell lung cancer (NSCLC). In addition, new data evaluating the efficacy and safety of obrixtamig for the treatment of extrapulmonary neuroendocrine carcinomas with high or low DLL3 expression will be featured in an oral session. "Tackling difficult-to-treat cancers requires a multi-pronged approach, which is why we're exploring multiple pathways to address key cancer drivers, including HER2 and DLL3, to deliver meaningful advancements for the patients who need them most," said Vicky Brown, U.S. Senior Vice President and Head of Oncology, Immunology & Eye Health, Boehringer Ingelheim. "Our data at ASCO underscore our generational commitment to pioneering critical innovations that address patients' greatest needs." Developing zongertinib for the treatment of HER2-mutant advanced NSCLC Patient reported outcomes (N=30) from the Beamion LUNG-1 study (NCT04886804) evaluating zongertinib, showed improvements in physical functioning and disease-related symptoms in previously treated patients with HER2 (ERBB2)-mutant advanced NSCLC, identified through the following surveys: EORTC IL46/Q168 Survey (side effect burden): 80% to 90% (24 to 27) of patients reported "not at all" or "a little" side-effect trouble across all visits.1 PRO-CTCAE: Patient-reported symptomatic adverse events assessed were in line with the previously reported safety profile of zongertinib in the Beamion LUNG-1 study; the majority of patients who reported they experienced diarrhea stated "rarely" or "occasionally".1 NSCLC Symptom Assessment Questionnaire: At weeks 15 and 27, over 50% of patients reported "no coughing at all" – a key disease-related symptom – double the proportion at baseline with remaining patients responding with "mild to moderate" coughing.1 EORTC QLQ-C30 Physical Functioning: After 15 weeks of treatment with zongertinib, participants showed a 60% improvement in physical functioning from baseline (95% CI: 6.3-12.9).1 This improvement was sustained throughout the PRO data collection period.1 Physical functioning was measured by the ability to complete strenuous activities, go on long or short walks, ability to sit in a chair (versus need to stay in bed), and need for assistance completing daily tasks.1 "In treating HER2-mutant advanced non-small cell lung cancer – a disease with limited options and a poor prognosis – patient reported outcomes are critical in understanding not only how well a treatment works, but also how it is received by patients," said Dr. Joshua K. Sabari, study investigator and Associate Professor, Department of Medicine, New York University (NYU) Grossman School of Medicine; Medical Director, Thoracic Medical Oncology, NYU Langone Health's Perlmutter Cancer Center. "The study's reported outcomes provide further confidence in the potential of zongertinib to have a meaningful impact on the lives of patients living with this aggressive disease." Exploring precision medicine through DLL3 targeted therapy, obrixtamig New data will be presented from the ongoing, Phase I dose escalation study (NCT04429087) evaluating T-cell engager, obrixtamig, in previously treated patients with extrapulmonary neuroendocrine carcinomas with high or low DLL3 expression (N=60). In the study, obrixtamig demonstrated efficacy in patients with high DLL3 expression.2 The objective response rate was 40% (95% CI: 24.6-57.7) in patients with high DLL3 expression compared to 3.3% (95% CI: 0.6-16.7) in patients with low DLL3 expression.2 The median duration of response was 7.9 months (95% CI: 6.2-not calculable [NC]) in patients with high DLL3 expression compared to 2.8 months (95% CI: NC-NC) in patients with low DLL3 expression.2 The disease control rate was 66.7% (95% CI: 48.8-80.8) in patients with high DLL3 expression compared to 26.7% (95% CI: 14.2-44.4) in patients with low DLL3 expression.2 Most treatment-related adverse events (AEs) were mild to moderate in both groups. Grade ≥3 treatment-related AEs occurred in 23.3% of patients with high DLL3 expression and 20% of those with low DLL3 expression.2 "Neuroendocrine carcinomas are a relatively rare form of cancer that are unfortunately often diagnosed at advanced stages, leading to poor outcomes for patients due to both the nature of the disease and the lack of standard of care, with limited treatment options," said Dr. Jonathan Strosberg, Professor and Medical Oncologist, Neuroendocrine Tumor Division & Department of Gastrointestinal Oncology Research Program, Moffitt Cancer Center. "DLL3 is highly expressed in neuroendocrine carcinomas, making DLL3 an important biomarker in precision medicine. Findings from this study, including a 40% objective response rate, underscore the potential of obrixtamig to produce an effective and durable response in patients with high DLL3 expression, and offer a targeted approach to treating this cancer." An ongoing Phase II DAREON®-5 trial (NCT04429087) is assessing obrixtamig in patients with relapsed/refractory DLL3-high extrapulmonary neuroendocrine carcinomas.2 Additionally, new clinical data from two early-stage trials evaluating BI 765063 and BI 770371 will be presented, strengthening Boehringer's partnership with OSE Immunotherapeutics. Presentations at ASCO 2025 from Boehringer Ingelheim's innovative pipeline highlight vision of transforming cancer care: About non-small cell lung cancer (NSCLC) Lung cancer claims more lives than any other cancer type3 and the incidence is set to increase to over 3 million cases worldwide by 2040.4 NSCLC is the most common type of lung cancer.5 The condition is often diagnosed at a late stage,6 and fewer than 3 in 10 patients are alive five years after diagnosis.7 People living with advanced NSCLC can experience a detrimental physical, psychological, and emotional impact on their daily lives. There remains a high unmet need for additional treatment options for people living with advanced NSCLC. Up to 4% of lung cancers are driven by HER2 mutations (or gene alterations).8 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.9 About zongertinib Zongertinib is an investigational irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 while sparing wild-type EGFR, thereby limiting associated toxicities. This orally administered, targeted therapy was granted FDA Fast Track Designation in 2023, followed by Breakthrough Therapy Designation in the U.S. and China for the treatment of adult patients with unresectable or metastatic NSCLC whose tumors have activating HER2 mutations and who have received prior systemic therapy. An application for accelerated approval was granted Priority Review status by the FDA in February 2025. In addition, Japan's Pharmaceuticals and Medical Devices Agency granted Orphan Drug Designation to zongertinib. A recent study has shown pre-clinically that the investigational compound zongertinib has potential for further clinical study in HER2 dependent solid cancers as monotherapy and as concurrent treatment with ADC therapy. In addition, zongertinib is being evaluated in Beamion LUNG-2 (NCT06151574)4, a global Phase III trial, compared to standard of care as first-line treatment in patients with unresectable, locally advanced or metastatic NSCLC who have activating HER2 TKD mutations. About the Beamion clinical trial program Beamion LUNG-1 (NCT04886804) is an open-label, Phase I dose escalation trial, with dose confirmation and expansion of zongertinib as monotherapy in people with advanced or metastatic solid tumors and NSCLC with activating HER2 alterations. The study has 2 parts. The first part is open to adults with different types of advanced cancer (solid tumors with changes in the HER2 gene) for whom previous treatment was not successful. The second part is open to people with advanced non-small cell lung cancer with a specific mutation in the HER2 gene. Beamion LUNG-2 is a Phase III, open label, randomized, active-controlled study in patients with unresectable, locally advanced or metastatic non-squamous NSCLC harboring HER2 TKD mutations to evaluate zongertinib compared with standard of care. About obrixtamig Obrixtamig is an investigational novel Immunoglobin G (IgG)-like bispecific T-cell engager designed to bind concomitantly to DLL3 on tumor cells and CD3 on T-cells.10 By creating a physical link between T-cells and tumor cells, the T-cell engager could potentially activate T-cells against DLL3-expressing tumor cells, potentially resulting in their destruction by the body's own immune system. Activated T-cells could indirectly stimulate other immune cells to broaden the immune response against the tumor tissue. NCT04429087 is a Phase I trial evaluating obrixtamig in patients whose tumors are positive for DLL3. The aim of the study is to determine the highest dose of obrixtamig that can be tolerated by patients before reaching the maximum tolerated dose. The study also aims to assess the side effects of obrixtamig to evaluate early evidence of antitumor activity. In addition, obrixtamig is being evaluated in additional tumor types, including an ongoing Phase II trial (DAREON®-5) in patients with relapsed/refractory DLL3-high epNECs. About extrapulmonary neuroendocrine carcinomas Extrapulmonary neuroendocrine carcinomas (epNECs) are rare, aggressive cancers arising outside the lungs, from neuroendocrine cells present in various organs such as the gastrointestinal tract, pancreas, and others.11 Delta-like ligand 3 (DLL3) is a protein that is expressed specifically on the surface of up 77% of NECs. In normal tissue, DLL3 is minimally expressed, which makes it an ideal therapeutic target. These cancers are often diagnosed at an advanced stage, leading to poor survival rates. Like other aggressive cancers, epNECs can significantly impact patients' physical, psychological, and emotional well-being.12 There remains a high unmet need for effective treatment options for individuals with advanced epNECs. Research is ongoing to identify molecular targets and develop new therapies.13 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 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. More than 53,500 employees serve over 130 markets to build a healthier, more sustainable, and equitable tomorrow. Learn more at . 1Sabari JK, Ruiter G, Nadal E, et al. Patient-reported outcomes evaluating physical functioning and symptoms in patients with pretreated HER2-mutant advanced non-small cell lung cancer (NSCLC) – results from the Beamion LUNG-1 trial. Presented at: 2025 American Society of Clinical Oncology (ASCO) Annual Meeting; Chicago, IL. 2Capdevila J. Efficacy and safety of the DLL3/CD3 T-cell engager obrixtamig in patients with extrapulmonary neuroendocrine carcinomas with high or low DLL3 expression: results from an ongoing phase I trial . The 2025 American Society of Clinical Oncology (ASCO) Annual Meeting. Published online 2025. 3World Health Organization Cancer Factsheet. (Accessed April 2025). 4International Agency for Research on Cancer – World Health Organization. Rates of trachea, bronchus and lung cancer. Available at: (Accessed August 2024). 5Zappa C & Mousa Non-small cell lung cancer: current treatment and future advances, Transl Lung Cancer Res. 2016 Jun; 5(3): 288–300. 6Polanco D et al. Prognostic value of symptoms at lung cancer diagnosis: a three-year observational study. J Thorac Dis 2021;13:1485–1494 7National Cancer Institute Surveillance, Epidemiology, and End Results (SEER). (Accessed: August 2024). 8Arcila, M. E. et al. Prevalence, clinicopathologic associations, and molecular spectrum of ERBB2 (HER2) tyrosine kinase mutations in lung adenocarcinomas. Clin. cancer Res. an Off. J. Am. Assoc. Cancer Res. 18, 4910–4918 (2012). 9Galogre M, et al. A review of HER2 overexpression and somatic mutations in cancers, Critical Reviews in Oncology/Hematology, Volume 186, 2023, 103997. 10Hallet, J. et. al. 2015 Feb 15;121(4):589-97. doi: 10.1002/cncr.29099. Epub 2014 Oct 11Liu Y, Li X, Zhang Y, et al. A novel approach to cancer therapy: targeting the tumor microenvironment. Cancer Res. 2024;84(2):123-134. doi:10.1158/0008-5472.CAN-23-4567. 12Pellegrini CA, Bodei L, Papi M, et al. Impact of neuroendocrine tumors on patients' personal and work lives. J Global Oncol. 2015;1(1):37-42. doi:10.1200/JGO.2015.002980. 13Muğlu H, Sünger E, Mıldanoğlu MM, Engin Delipoyraz E, Yücel MH, Özçelik H, Hamdard J, Açıkgöz Ö, Ölmez ÖF, Yıldız Ö, et al. Clinicopathological Characteristics of Extrapulmonary Neuroendocrine Carcinomas: Treatment Responses and Survival Outcomes: Single-Center Experience. Journal of Clinical Medicine. 2025;14(7):2264. doi:10.3390/jcm14072264. 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

ASCOClinical ResultPhase 2Fast TrackPhase 1

14 May 2025

·firstwordpharma.com

Boehringer Ingelheim expands oncology pipeline with real-world data from Tempus AI

Boehringer Ingelheim has entered a multi-year partnership with Tempus AI to leverage its real-world data and AI platform in support of Boehringer's expanding oncology pipeline. Through the partnership, Boehringer will gain access to Tempus' de-identified data and its advanced data analytics platform, Lens."Leveraging real-world patient data is crucial for strengthening our data foundation and harnessing advanced AI methodologies, ultimately accelerating drug development," said Jan Nygaard Jensen, head of computational innovation at Boehringer Ingelheim. "Integrating these comprehensive datasets with our internal data and techniques not only drives innovation but also enhances the precision and efficiency of pharmaceutical research, paving the way for groundbreaking medical advancements."Tempus' database comprises over eight million research records. Its AI-enabled Lens platform allows researchers to define patient cohorts using molecular and clinical filters, or to automatically build cohorts using Tempus One, an AI-enabled assistant that applies inclusion and exclusion criteria. Researchers can visualise or download datasets for in-depth analysis. These insights can support biomarker discovery, patient stratification, novel target identification, hypotheses for combination therapies and patient education. Boehringer currently markets three oncology drugs — Gilotrif (afatinib) and Ofev (nintedanib) for non-small-cell-lung cancer (NSCLC) and Tevimbra (tislelizumab) for oesophageal and gastric cancers. Its oncology pipeline includes a broad portfolio of investigational agents, such as anti-DLL3 T-cell engager BI 764532 in phase II trials for small cell lung cancer and neuroendocrine cancers; HER2 exon 20 inhibitor zongertinib in phase III trials for NSCLC and MDM2-p53 antagonist brigimadlin in phase III trials for de-differentiated liposarcoma and soft tissue sarcoma, and phase II trials for NSCLC and bile duct cancer. Additional early-stage assets target a variety of solid tumours."By combining internal, pre-clinical experimental data, with real-world data from Tempus on its AI-powered platform, we can profoundly deepen our understanding of cancer biology and accelerate our drug discovery and development efforts," said Mark Paul Petronczki, head of oncology research at Boehringer Ingelheim.

Phase 2Phase 3ASCO

01 May 2025

·pharma.economictimes.indiatimes.com

Boehringer drug delivers 'unprecedented' result in lung cancer study

London: An experimental Boehringer Ingelheim drug achieved "unprecedented" benefits in patients with an advanced form of lung cancer who had already received other treatments for their disease, researchers said at the American Association for Cancer Research meeting in Chicago. The drug, zongertinib, targets the HER2 protein on cancer cell surfaces. Among 75 patients with pretreated non-small cell lung cancer and mutations in HER2 known as tyrosine kinase domain (TKD) mutations, 71% had significant tumor shrinkage during treatment with zongertinib. NSCLC is the most common type of lung cancer. "A 71% response rate is unprecedented in this cancer subtype, and not only is the data strong in showing that this treatment works, but zongertinib has the added convenience of being a once-daily oral therapy," study leader Dr. John Heymach of the M.D. Anderson Cancer Center in Houston said in a statement. "When you also consider the improved safety profile compared to less selective inhibitors, this suggests a promising approach for patients in need of new treatments," Heymach said. "That's exciting because just a few years ago these patients had no effective targeted therapies." On average, patients' disease remained stable, without getting worse, for more than a year, according to a report of the study published in The New England Journal of Medicine. "This new data is particularly encouraging for patients who had disease progression after prior therapies, because it indicates that the resistance mechanisms to those therapies does not necessarily confer cross-resistance to zongertinib," Heymach said. His team also reported early positive results in 20 patients with non-TKD mutations and 31 patients with TKD mutations who previously were treated with a different HER2-targeting drug, although these patients haven't been followed long enough to draw firm conclusions. GSK CANCER DRUG HELPS PATIENTS AVOID SURGERY A GSK drug given to treat certain early-stage cancers caused tumors to disappear in 80 per cent of patients in a mid-stage trial, allowing them to avoid surgery, researchers reported at the AACR meeting. The study participants had so-called mismatch repair deficient, or microsatellite instability-high, cancers, in which the body's DNA repair system, responsible for fixing errors in cell structure and function, is not working properly. About half of the patients had rectal cancers; the rest had other malignancies including esophagogastric, colon, hepatobiliary, genitourinary, and gynecologic tumors. About two-thirds had evidence of cancer spread to their lymph nodes. All were good candidates for surgery, but instead received GSK's immunotherapy Jemperli (dostarlimab) for 6 months. Among the 103 patients who completed the treatment, 84 had a clinical complete response, meaning no sign of cancer, and 82 did not undergo surgery, according to a report of the study published in The New England Journal of Medicine. Two years later, 92 per cent remained free of cancer recurrence. Three patients with rectal cancer were able to conceive and deliver healthy children. The majority of patients with incomplete responses still had significant tumor shrinkage, the researchers found. Overall, 95 per cent of the patients had no or only mild side effects. Jemperli, which is approved to treat a type of endometrial cancer that has recurred or spread, helps the immune system to recognize and attack cancer cells. If the results are confirmed in larger trials, "immunotherapy alone could potentially replace more invasive treatments, such as surgery, chemotherapy, and radiation, offering patients a significantly improved quality of life," study leader Dr. Andrea Cercek of Memorial Sloan-Kettering Cancer Center in New York said in a statement. ADDING KEYTRUDA TO SURGERY BENEFICIAL IN HEAD/NECK CANCER Adding Merck's blockbuster immunotherapy Keytruda before and after surgery to usual treatments improves outcomes for patients with newly diagnosed head and neck squamous cell carcinoma, according to trial results presented at the meeting. Typically, these patients undergo surgery followed by radiation with or without chemotherapy. "This paradigm has been in place for more than two decades, and unfortunately outcomes for many patients continue to be unsatisfactory," study leader Dr. Ravindra Uppaluri of the Brigham and Women's Hospital in Boston said in a statement. The new trial results show that before surgery, treatment with Keytruda can enhance immune responses and start to act on tumor killing. And after surgery the drug "can address any leftover cancer cells that may still be present," Uppaluri said. In the trial, 714 patients undergoing surgery for stage 3-4 HNSCC including in the larynx, hypopharynx , and oral cavity received either Keytruda before and after surgery, or usual care. Patients who received Keytruda were more likely to have at least a 90 per cent reduction in the size of their tumor before undergoing surgery, compared to those in the control group, the researchers found. The median time to cancer progression, relapse, or death was 51.8 months for patients treated with Keytruda compared with 30.4 months with usual care alone. Among patients with the highest level of the PD-1 cell-surface protein targeted by Keytruda, the median time to those events was 59.7 months in the Keytruda group and 26.9 months in the standard-of-care group. After accounting for individual patient characteristics, and with half of patients having at least 38.3 months of follow-up, those treated with Keytruda were at least 27 per cent less likely to have experienced recurrence. Furthermore, treatment with Keytruda (pembrolizumab) reduced the risk of adverse events by 34 per cent researchers reported. Keytruda, the world's biggest-selling prescription medicine, is approved for many types of cancer. "This new information supports changing the current standard of care" to now give Keytruda pre- and post-operatively, Uppaluri said. "For the first time in more than 20 years, patients with this challenging disease have a new therapeutic approach." (Reporting by Nancy Lapid; editing by Bill Berkrot)

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100 Deals associated with Zongertinib

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Indication	Highest Phase	Country/Location	Organization	Date
HER2 mutant non-small cell lung cancer	NDA/BLA	China	Boehringer Ingelheim International GmbH	15 Jan 2025
Advanced cancer	Phase 2	United States	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	China	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Japan	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Australia	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Belgium	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Canada	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	France	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Germany	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024
Advanced cancer	Phase 2	Italy	C.H. Boehringer Sohn AG & Co. KG	11 Oct 2024

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04886804 (Phase Ia dose escalation/expansion trial, ASCO2025)	Phase 1	HER2-negative breast cancer HER2	121	Zongertinib	dpiyvxrato(tivjowhmie) = The MTD was not reached luksfcrnln (tuvfrcires )	Positive	30 May 2025
				Tucatinib
AACR2025	Not Applicable	HER2 mutations	-	Zongertinib	oktrjtjhrg(qxsrruvmdd) = xxvvtlieom pporhfzeoq (cpneutglou )	-	30 Apr 2025
				Poziotinib	oktrjtjhrg(qxsrruvmdd) = mruzkfhfhv pporhfzeoq (cpneutglou )
Phase I study (AACR2025)	Phase 1	HER2 mutations	-	Zongertinib 60 mg (C-14)-zongertinib solution	dptcrbkkyb(ukcsvpuewf) = tasppefxbp dqcecwoqok (qxvwgrvqjw ) View more	Positive	29 Apr 2025
				Zongertinib 60 mg film-coated tablet	fftxhmxypg(dzmxcxdovd) = bptwjsiggn wnxbfpzupg (whljiedzxd )
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)	lytpmbjigs(rxfedeqhhc) = elmqizbqfw ueefqwpfmf (nwxmflnajq, 60 - 80) View more	Positive	28 Apr 2025
				Zongertinib (cohort 3; pretreated HER2-mutant NSCLC with TKD or non-TKD mutations)	lytpmbjigs(rxfedeqhhc) = dcuzpwalmu ueefqwpfmf (nwxmflnajq, 15 - 52) View more
NCT04886804 (Beamion LUNG-1, Pubmed \| N Engl J Med)	Phase 1	Metastatic Solid Tumor \| Non-Small Cell Lung Cancer \| Squamous non-small cell lung cancer ... HER2 View more	-	Zongertinib 120 mg	tvsvwdjual(jbejspspvl) = bvrjwdlbgy ksnidaqkmb (ljerbdfpeb, 60 - 80) View more	Positive	28 Apr 2025
				HER2-directed antibody-drug conjugate	tvsvwdjual(jbejspspvl) = wtdujpabfj ksnidaqkmb (ljerbdfpeb, 32 - 65)
NCT04886804 (Beamion LUNG-1, Pubmed \| J Clin Oncol)	Phase 1	Metastatic Solid Tumor \| Non-Small Cell Lung Cancer \| Squamous non-small cell lung cancer ... HER2 View more	105	Zongertinib 120 mg once daily	tpfmjcpelf(lkxrmohrql) = MTD was not reached pymdssvibc (vfhoyiurar ) View more	Positive	10 Apr 2025
				Zongertinib 240 mg once daily
NCT04886804 (Beamion Lung 1, NEWS \| Pubmed) Manual	Phase 1	Solid tumor \| Non-Small Cell Lung Cancer ERBB2 Mutation (Activating)	105	宗格替尼	jcpkslrtpb(vayrecrvis) = Two DLTs occurred during the MTD evaluation period. bwtjqmeqvd (rykwugmtdv ) View more	Positive	11 Mar 2025
				宗格替尼 (NSCLC)
NCT04886804 (BEAMION LUNG-1, PRNewswire) Manual	Phase 1	HER2 mutant non-small cell lung cancer HER2	-	zongertinib (每日120毫克，单次服用)	uyenlqbgda(odybutsslv) = pdexdrwlkq povkazzxxz (dadfueikff ) View more	Positive	10 Dec 2024
NCT04886804 (Beamion LUNG-1, ESMO_ASIA2024) Manual	Phase 1	HER2 Positive Solid Tumors HER2 Positive	105	Zongertinib	lkuvqamfbv(maxmydkcce) = MTD was not reached for BID or QD schedules. aawnamonfp (smogvzuysy ) View more	Positive	07 Dec 2024
				Zongertinib (Asian pts)
NCT04886804 (Beamion LUNG-1, WCLC2024) Manual	Phase 1	HER2 Positive Solid Tumors HER2 Positive	83	Zongertinib BID	quoopfjcie(vgngwamwth) = plbfwljjnp vvywmofmgc (krhliimrbe ) View more	Positive	10 Sep 2024
				Zongertinib QD	qntppicxxx(rdzvwyucmp) = eefmxhidzf uejyddeilc (qbwsztcjmb ) View more

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