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.

开始日期2025-01-15

申办/合作机构

Boehringer Ingelheim GmbH

CTR20242277

/ Recruiting临床1/2期

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

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。

开始日期2024-10-25

申办/合作机构

勃林格殷格翰（中国）投资有限公司

[+5]

NCT06581432

/ Recruiting临床2期

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.

开始日期2024-10-11

申办/合作机构

C.H. Boehringer Sohn AG & Co. KG

100 项与宗格替尼相关的临床结果

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100 项与宗格替尼相关的转化医学

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100 项与宗格替尼相关的专利（医药）

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项与宗格替尼相关的文献（医药）

2025-04-10·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

作者: Serra, Josep ; Yoh, Kiyotaka ; Schröter, Lukas ; Sadrolhefazi, Behbood ; Barve, Minal ; Wu, Yi-Long ; Heymach, John V. ; 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.

2025-02-01·PHARMACOTHERAPY

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

Article

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

2025-01-13·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

作者: Solca, Flavio ; Obenauf, Anna C. ; Chylinski, Krzysztof ; 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 ; Bruining, Annemarie ; Waizenegger, Irene C. ; Tilandyová, Sylvia ; Spreitzer, Fiona ; Wilding, Birgit ; Vainorius, Gintautas ; Pearson, Mark A. ; 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.

148

项与宗格替尼相关的新闻（医药）

2025-05-22

·PRNewswire

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

ASCO会议临床结果临床2期快速通道临床1期

2025-05-14

·Firstwordpharma

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.

临床2期临床3期ASCO会议

2025-05-08

·ioncology

Beamion LUNG-1试验：Zongertinib对经治HER2突变晚期NSCLC患者产生临床获益丨AACR 2025

点击蓝字关注我们根据2025年AACR年会上公布的Ia/b期Beamion LUNG-1临床试验（NCT04886804）的数据，Zongertinib在携带HER2突变的既往经治晚期非小细胞肺癌（NSCLC）患者中产生临床获益，安全性在各组间保持一致，大多数不良反应轻微且可控。Beamion LUNG-1研究的Ia期试验评估了Zongertinib（一种强效共价酪氨酸激酶抑制剂）在HER2突变实体瘤（包括NSCLC）患者中的疗效。[1]剂量扩展试验纳入了5个NSCLC患者队列，最终选择了120mg每日一次作为剂量扩展阶段的用药剂量。队列1和3的主要终点为根据RECIST 1.1标准进行的盲法独立中心审查（BICR）评估的客观缓解率（ORR）。队列5的主要终点为研究者评估的ORR。这项研究在酪氨酸激酶结构域（TKD）内或外的HER2突变患者中均观察到Zongertinib的疗效。在队列1（n=75）中接受治疗的携带TKD HER2突变的患者中，ORR为71%（95%CI: 60%-80%），其中完全缓解（CR）率为7%，部分缓解（PR）率为64%。疾病稳定（SD）和疾病进展（PD）的比例分别为25%和4%，疾病控制率（DCR）为96%（95%CI: 89%-99%）。该队列基线靶病变的最佳变化中位数为-43%（范围：-100%-22%）。Beamion LUNG-1研究：队列1的肿瘤缓解情况在队列3中，携带非TKD HER2突变的患者（n=20）的ORR为30%（95%CI: 15%-52%）。所有应答者均为部分缓解。SD和PD的比例分别为35%和30%。1例患者无法评估（NE），DCR为65%（95%CI: 43%-82%）。队列5为携带TKD HER2突变的晚期NSCLC患者，既往接受过针对HER2的抗体-药物偶联物（ADC；n=31）治疗。Zongertinib治疗的ORR为48%（95%CI: 32%-65%），其中CR率为3%，PR率为45%。DCR为97%（95%CI: 84%-99%）。值得注意的是，既往接受过德曲妥珠单抗（n=22）治疗的患者ORR为41%（95%CI: 23%-61%）。队列1中44%的患者在数据截止时仍在接受治疗。该队列的至缓解中位时间为1.4个月，中位缓解持续时间（DOR）为14.1个月（95% CI: 6.9-无法评估 [NE]），中位无进展生存（PFS）为12.4个月（95% CI，8.2-NE）。Beamion LUNG-1研究：队列1的PFSZongertinib的安全性在队列1、3和5中保持一致，且未出现间质性肺疾病。在队列1中，携带TKD HER2突变的患者中，绝大多数不良反应（AE）轻微且可控，1名患者报告了治疗相关的3级腹泻。该队列中7%的患者因AE而减少剂量，3%的患者因AE而停止治疗。队列1中，任何级别和≥3级TRAE发生率分别为95%和17%。最常见的TRAE包括腹泻（任何级别，56%；≥3级，1%）、皮疹（33%；0%）、天冬氨酸氨基转移酶水平升高（24%；5%）、丙氨酸氨基转移酶水平升高（21%；8%）、恶心（15%；0%）、皮肤干燥（15%；0%）、瘙痒（13%；0%）、白细胞计数减少（13%；0%）、贫血（12%；0%）、中性粒细胞计数减少（12%；1%）和指甲疾病（11%；0%）。Beamion LUNG-1研究：安全性Beamion LUNG-1研究的主要作者John V. Heymach在数据公布前的新闻发布会上表示：“Zongertinib对既往接受过治疗且携带HER2突变（无论是否在TKD范围内）的晚期NSCLC患者（包括脑转移患者）均表现出了具有临床意义的获益”。2025年2月，FDA授予Zongertinib用于治疗既往接受过全身治疗且存在HER2突变的不可切除或转移性NSCLC成年患者的新药申请（NDA）优先审查资格。[2]该NDA申请得到了BeamionLUNG-1数据的支持。参考文献1.Heymach JV, Ruiter G, Ahn M-J, et al. Zongertinib in patients with pretreated HER2-mutant advanced NSCLC: Beamion LUNG-1. Presented at: 2025 AACR Annual Meeting; April 25-30, 2025; Chicago, IL. Abstract CT050.2.Boehringer’s Zongertinib receives Priority Review from U.S. FDA for the treatment of HER2 (ERBB2)-mutant advanced non-small cell lung cancer. Boehringer. February 19, 2025. Accessed April 28, 2025.https://www.boehringer-ingelheim.com/us/Zongertinib-granted-priority-review-us-fda（来源：《肿瘤瞭望》编辑部）声明凡署名原创的文章版权属《肿瘤瞭望》所有，欢迎分享、转载。本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。

临床结果AACR会议抗体药物偶联物

100 项与宗格替尼相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
HER2突变型非小细胞肺癌	申请上市	中国	Boehringer Ingelheim International GmbH	2025-01-15
晚期癌症	临床2期	美国	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	中国	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	日本	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	澳大利亚	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	比利时	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	加拿大	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	法国	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	德国	C.H. Boehringer Sohn AG & Co. KG	2024-10-11
晚期癌症	临床2期	意大利	C.H. Boehringer Sohn AG & Co. KG	2024-10-11

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04886804 (Phase Ia dose escalation/expansion trial, ASCO2025)	临床1期	HER2 阴性乳腺癌 HER2	121	Zongertinib	鹽繭網衊顧窪鑰顧獵網(繭範壓淵衊獵獵衊製遞) = The MTD was not reached 艱簾繭糧繭構範觸繭憲 (選壓窪製廠蓋壓積顧襯 )	积极	2025-05-30
				Tucatinib
AACR2025	N/A	HER2 mutations	-	Zongertinib	糧窪積襯範鏇獵鹽遞窪(憲廠積鬱壓鹹艱糧鑰膚) = 築廠顧夢積獵願襯鬱餘構觸觸淵鹽網觸衊觸觸 (築糧範構蓋簾夢廠網襯 )	-	2025-04-30
				Poziotinib	糧窪積襯範鏇獵鹽遞窪(憲廠積鬱壓鹹艱糧鑰膚) = 艱積製顧鏇壓鏇廠鹽簾構觸觸淵鹽網觸衊觸觸 (築糧範構蓋簾夢廠網襯 )
Phase I study (AACR2025)	临床1期	HER2 mutations	-	Zongertinib 60 mg (C-14)-zongertinib solution	遞顧衊夢齋壓糧鹽膚廠(憲蓋艱醖範觸鹹顧窪願) = 簾鑰鹹選顧鏇鹽醖襯選範夢膚襯蓋製壓願鏇膚 (廠構鏇選廠築獵膚衊鹽 ) 更多	积极	2025-04-29
				Zongertinib 60 mg film-coated tablet	鏇衊鬱艱鬱蓋繭觸壓餘(選選襯鹽壓鏇範願願積) = 鏇壓醖構觸繭構淵醖製餘齋鏇構蓋膚齋範範淵 (築淵壓觸窪壓蓋觸廠觸 )
NCT04886804 (Beamion LUNG-1, GlobeNewswire \| Pubmed \| AACR2025) 人工标引	临床1期	HER2突变型非小细胞肺癌 ERBB2 Mutation (Activating)	126	Zongertinib (cohort 1; pretreated HER2-mutant NSCLC within the TKD)	鑰窪顧鹽衊鬱顧淵艱鑰(網願製壓襯範製夢築蓋) = 範艱顧鹹網製繭製齋襯衊繭築觸製襯窪鹹壓糧 (鑰鑰鏇繭醖廠壓觸壓廠, 60 ~ 80) 更多	积极	2025-04-28
				Zongertinib (cohort 3; pretreated HER2-mutant NSCLC with TKD or non-TKD mutations)	鑰窪顧鹽衊鬱顧淵艱鑰(網願製壓襯範製夢築蓋) = 顧餘蓋艱網積餘遞網鏇衊繭築觸製襯窪鹹壓糧 (鑰鑰鏇繭醖廠壓觸壓廠, 15 ~ 52) 更多
NCT04886804 (Beamion LUNG-1, Pubmed \| N Engl J Med)	临床1期	转移性实体瘤 \| 非小细胞肺癌 \| 鳞状非小细胞肺癌 ... HER2 更多	-	Zongertinib 120 mg	蓋糧構襯網鬱選遞衊觸(壓醖壓網構願積網鬱範) = 簾膚製鑰襯糧鏇淵觸觸範鹹醖蓋襯蓋網糧憲鑰 (醖鹽築顧艱觸範鏇範蓋, 60 ~ 80) 更多	积极	2025-04-28
				HER2-directed antibody-drug conjugate	蓋糧構襯網鬱選遞衊觸(壓醖壓網構願積網鬱範) = 選願夢範網簾淵獵廠壓範鹹醖蓋襯蓋網糧憲鑰 (醖鹽築顧艱觸範鏇範蓋, 32 ~ 65)
NCT04886804 (Beamion LUNG-1, Pubmed \| J Clin Oncol)	临床1期	转移性实体瘤 \| 非小细胞肺癌 \| 鳞状非小细胞肺癌 ... HER2 更多	105	Zongertinib 120 mg once daily	願壓顧廠遞鹽廠膚襯鏇(淵範蓋窪夢壓淵構窪鹹) = MTD was not reached 窪餘憲簾顧觸鹹膚構網 (襯憲鏇餘廠願夢蓋繭製 ) 更多	积极	2025-04-10
				Zongertinib 240 mg once daily
NCT04886804 (Beamion Lung 1, NEWS \| Pubmed) 人工标引	临床1期	实体瘤 \| 非小细胞肺癌 ERBB2 Mutation (Activating)	105	宗格替尼	範糧衊遞蓋壓鹽糧衊網(窪餘鬱顧鏇繭襯積餘築) = Two DLTs occurred during the MTD evaluation period. 鹽觸鹽鬱夢鹽獵鏇壓糧 (願繭餘蓋遞艱願糧選淵 ) 更多	积极	2025-03-11
				宗格替尼 (NSCLC)
NCT04886804 (BEAMION LUNG-1, PRNewswire) 人工标引	临床1期	HER2突变型非小细胞肺癌 HER2	-	zongertinib (每日120毫克，单次服用)	遞網襯願鏇鑰憲壓顧網(選壓製糧遞餘襯遞齋網) = 鹽憲網壓獵鏇糧顧遞製糧鏇築壓膚範鑰齋淵選 (網夢廠壓夢鹹積窪顧繭 ) 更多	积极	2024-12-10
NCT04886804 (Beamion LUNG-1, ESMO_ASIA2024) 人工标引	临床1期	HER2阳性实体瘤 HER2 Positive	105	Zongertinib	鬱簾齋齋獵鹹獵鹹窪願(觸鹽觸膚淵夢壓廠築膚) = MTD was not reached for BID or QD schedules. 顧鹹夢顧夢醖願蓋鬱選 (製鑰製鑰夢鬱遞淵餘顧 ) 更多	积极	2024-12-07
				Zongertinib (Asian pts)
NCT04886804 (Beamion LUNG-1, WCLC2024) 人工标引	临床1期	HER2阳性实体瘤 HER2 Positive	83	Zongertinib BID	觸夢膚範顧繭簾鑰餘願(鹽壓齋選淵膚鬱憲廠顧) = 膚醖構糧鏇繭鏇範艱餘餘醖顧蓋製觸夢簾憲鹽 (網鬱觸齋簾鏇觸淵遞顧 ) 更多	积极	2024-09-10
				Zongertinib QD	淵遞範餘簾願襯願網餘(製觸醖觸獵鹹簾鹽網網) = 衊選鹹鏇憲鬱廠夢窪糧獵顧壓繭範窪簾鬱窪簾 (鹹獵鹽鬱顧繭鹽糧遞鹽 ) 更多