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.

[+3]

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 or no treatment exists. 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 10 groups based on the type of advanced cancer and the type of HER2 alterations they have. All participants take one dose of zongertinib. 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

01 Feb 2025·Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy

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

Article

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

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

AbstractMutations 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.

01 Jan 2024·Cancer Treatment and Research Communications

Very first real-world data on zongertinib use in non-small cell lung cancer patients with HER2 mutations: A brief report

Article

Author: Illini, Oliver ; Fabikan, Hannah ; Valipour, Arschang ; Weinlinger, Christoph ; Lang-Stöberl, Anna Sophie ; Hochmair, Maximilian J

INTRODUCTIONTreatment options for HER2-mutant patients with non-small cell lung cancer (NSCLC) are limited. New agents, including zongertinib, a HER2-selective tyrosine kinase inhibitor (TKI), are being investigated in clinical trials. However, published clinical data on the efficacy and safety of zongertinib are limited to data from a single phase I trial including only 36 patients with NSCLC.METHODSWe report real-world data on six consecutive patients with HER2-mutant NSCLC who received zongertinib through a named patient use program between December 2023 and June 2024. Radiological response evaluation and blood testing were routinely performed every two to three months, and adverse events were graded according to the Common Terminology Criteria for Adverse Events (CTCAE) version 5.RESULTSAll patients were diagnosed with a metastatic adenocarcinoma, had previously progressed on at least one line of chemotherapy and had been previously treated with trastuzumab-deruxtecan (two had to stop treatment because of pneumonitis). Three patients (50%) presented with an Eastern Cooperative Oncology Group (ECOG) performance status of ≥2. A clinical and radiological benefit was achieved in all patients (complete response (1), partial response (4), and stable disease (1)). In one patient with brain metastases, a complete response was achieved. Treatment with zongertinib is ongoing in all patients. Adverse events were reported in one patient (elevated blood pressure (grade 1).CONCLUSIONZongertinib may be an effective and well-tolerated treatment option for HER2-mutant NSCLC patients even if they are heavily pretreated, have a reduced performance status or have a history of pneumonitis and brain metastases.

News (Medical) associated with Zongertinib

06 Mar 2025

·www.prnewswire.com

TEPMETKO Continues to Strengthens its Position as a Leading METex14 Skipping NSCLC Therapy | DelveInsight

With increasing biomarker-driven cancer treatments, TEPMETKO benefits from growing adoption in precision oncology. Competition from other MET inhibitors like TABRECTA (capmatinib) exists, but TEPMETKO's once-daily dosing and efficacy profile offer differentiation. LAS VEGAS, March 6, 2025 /PRNewswire/ -- DelveInsight's " TEPMETKO Market Size, Forecast, and Market Insight Report" highlights the details around TEPMETKO, a kinase inhibitor indicated for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of TEPMETKO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan]. EMD Serono's TEPMETKO (tepotinib) Overview TEPMETKO is a kinase inhibitor prescribed for adult patients with metastatic non-small cell lung cancer (NSCLC) carrying MET exon 14 skipping alterations. The active component is Tepotinib (as hydrochloride monohydrate), administered orally. Patients should be cautioned about the heightened risk of severe or fatal interstitial lung disease/pneumonitis, liver toxicity, and potential embryo-fetal toxicity, necessitating effective contraception during and shortly after treatment. Tepotinib specifically targets MET, including variants with exon 14 skipping mutations. It blocks HGF-dependent and independent MET phosphorylation, disrupting MET-driven signaling pathways. Additionally, at clinically relevant concentrations, Tepotinib inhibits melatonin 2 and imidazoline 1 receptors. In vitro studies show that it suppresses tumor cell proliferation, anchorage-independent growth, and migration of MET-dependent cancer cells. In mouse models with MET-driven tumors, including those with MET exon 14 skipping alterations, Tepotinib reduced tumor growth, sustained MET phosphorylation inhibition, and, in one case, decreased metastasis formation. The recommended dose of TEPMETKO is 450 mg taken orally once daily until disease progression or intolerable toxicity occurs. Patients should take it at the same time each day, swallowing tablets whole without chewing, crushing, or splitting them. If a dose is missed and less than eight hours remain until the next scheduled dose, patients should skip it. In cases of vomiting after taking TEPMETKO, the next dose should be taken at the usual time. Learn more about TEPMETKO projected market size for NSCLC @ TEPMETKO Market Potential Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for 81% of all diagnosed cases. Early detection greatly improves outcomes, but diagnosing NSCLC and other lung cancers is challenging because their symptoms are often mistaken for common illnesses or the long-term effects of smoking. Consequently, 80% of NSCLC cases are already at advanced stages by the time they are identified, making treatment more difficult. Around 80% of EGFR mutations in NSCLC involve either exon 19 deletions or the exon 21 L858R substitution, both of which are classified as sensitizing mutations. Until the last decade, chemotherapy was the primary treatment for advanced and metastatic lung cancer. However, this changed in 2015 with the approval of the first immune checkpoint inhibitor (ICI), KEYTRUDA (pembrolizumab), as a second-line therapy for advanced cases. This was followed by TECENTRIQ (atezolizumab) in 2016. Both therapies were later approved for first-line treatment, broadening their use to a larger patient population. In 2020, the combination of OPDIVO (nivolumab) and ipilimumab also received approval as a first-line treatment for metastatic NSCLC. According to DelveInsight, the NSCLC market size across the 7MM is projected to grow from USD 30 billion in 2024, with a substantial CAGR through 2034. This growth is largely driven by the introduction of emerging therapies during the forecast period (2025–2034). Discover more about the NSCLC market in detail @ Non-small Cell Lung Cancer Market Report Emerging Competitors of TEPMETKO The NSCLC pipeline is very robust with the promising therapies such as Telisotuzumab vedotin (AbbVie), Patritumab deruxtecan (Daiichi Sankyo/AstraZeneca), Datopotamab deruxtecan (Daiichi Sankyo/AstraZeneca), Eftilagimod alpha (Immutep), BNT311/GEN1046 (acasunlimab) (Genmab), V940 (mRNA-4157) + Pembrolizumab (Moderna Therapeutics/Merck), Plinabulin + Docetaxel (BeyondSpring), Olomorasib (LY3537982) (Eli Lilly and Company), Zipalertinib (Cullinan Oncology/Taiho Pharma), Ceralasertib (AZD6738) (AstraZeneca), TEDOPI (EP-2101; IDM 2101; OSE-2101) (OSE Immuno-therapeutics), Sigvotatug vedotin (PF08046047) (Pfizer), ANKTIVA (N-803) (ImmunityBio), Aumolertinib/Almonertinib/HS-10206 (Jiangsu Hansoh Pharmaceutical), Niraparib (GSK), Savolitinib (AstraZeneca/Hutchison MediPharma), TRODELVY (Gilead Sciences), Pyrotinib (Jiangsu HengRui Medicine), Ociperlimab (BGB-A1217) (BieGene), Volrustomig (AstraZeneca), Gotistobart (BNT316/ONC-392) (OncoC4/BioNTech), Ivonescimab (AK112/SMT112) (Akeso Biopharma/Summit Therapeutics), ZYNYZ (retifanlimab/INCMGA00012) (Incyte/Macrogenics), Divarasib (GDC-6036) (Roche/Genentech), Tiragolumab (RG6058) (Roche), Sacituzumab Tirumotecan (Merck and Kelun-Biotech), JEMPERLI (dostarlimab/TSR-042) (GSK and AnaptysBio), Zongertinib (BI-1810631) (Boehringer Ingelheim), BAY 2927088 (Bayer), Serplulimab (HLX10) (Shanghai Henlius Biotech), Rilvegostomig (AZD2936) (AstraZeneca), MK-1084 (Merck, Taiho Pharmaceutical, and Astex), Domvanalimab (Arcus Biosciences and Gilead Sciences), OPDUALAG (nivolumab and relatlimab) (Bristol-Myers Squibb), Belrestotug + JEMPERLI (iTeos Therapeutics and GSK), Firmonertinib (ArriVent BioPharma), Sunvozertinib (DZD9008) (Dizal Pharmaceutical), Cobolimab (GSK), Livmoniplimab (AbbVie), Fianlimab (REGN3767) (Regeneron Pharmaceuticals), BNT327/PM8002 (Biotheus/BioNTech), HS-20117 (Hansoh BioMedical), IO102-IO103 + Pembrolizumab (IO Biotech), Naptumomab estafenatox (NeoTX Therapeutics/Active Biotech), FF-10832 (FUJIFILM Corporation), BNT116 (BioNTechSE/Regeneron Pharmaceuticals), CAN-2409 (Candel Therapeutics), Mecbotamab Vedotin (BA3011/CAB-AXL-ADC) (BioAtla), Bemcentinib (BGB 324/BGB-3234/R-428) (BerGenBio/Rigel Pharmaceuticals), DOVBLERON (taletrectinib/AB-106/IBI-344) (Nuvation Bio/Innovent Biologics/Daiichi Sankyo/Nippon Kayaku), Lifileucel (Iovance Biotherapeutics), IBI363 (Innovent Biologics), Sotevtamab (AB-16B5) (Alethia Biotherapeutics), Avutometinib (VS6766) (Verastem Oncology), Vebreltinib (APL-101) (Apollomics), LP-300 (Lantern Pharma), JNJ-90301900 (Johnson & Johnson Innovative Medicine), AMG 193 (Amgen), Luveltamab tazevibulin (Sutro Biopharma), PRT3789 (Prelude Therapeutics), Disitamab vedotin (Seagen), PADCEV (enfortumab vedotin) (Astellas Pharma), RP1 (Replimune), TIVDAK (tisotumab vedotin) (Seagen), Zanidatamab (Jazz Pharmaceuticals), Utidelone injectable (UTD1) (Beijing Biostar Pharmaceuticals), REGN5093-M114 (Regeneron Pharmaceuticals), SLC-391 (SignalChem Lifesciences), fulzerasib (GenFleet), Davutamig (REGN5093) (Regeneron Pharmaceuticals), TAS3351 (Taiho Oncology), H002 (RedCloud Bio), JIN-A02 (J INTS BIO), FWD1509 (Forward Pharma), Sabestomig (AZD7789) (AstraZeneca), Sasanlimab (Pfizer), Selvigaltin (GB1211) (Galecto Biotech), Vepafestinib Helsinn (Healthcare/Taiho Pharmaceutical), EP0031 (A400/ KL590586) (Ellipses Pharma/Kelun-Biotech), Pamvatamig (MCLA-129) (Merus), Zidesamtinib (NVL-520) (Nuvalent), NVL-655 (Nuvalent), RMC-4630 (Revolution Medicines), REQORSA (quaratusugene ozeplasmid) (Genprex), PDC*lung01 (PDC*line Pharma), Evalstotug (BA3071) (BioAtla and BeiGene), PT-112 (Promontory Therapeutics), MRT-2359 (Monte Rosa Therapeutics), GAIA-102 (GAIA BioMedicine), Rigosertib (Traws Pharma), HMBD-001 (Hummingbird Bioscience), PLB1004 (Avistone Biotechnology), ANS03 (Avistone Biotechnology), MYTX-011 (Mythic Therapeutics), A166 (Sichuan Kelun-Biotech Bio-pharmaceutical), Atamparib (BN-2397) (Ribon Therapeutics), DELTACEL (KB-GDT-01) (Kiromic BioPharma), Carotuximab (ENV-105) (Kairos Pharma), YL202 (MediLink Therapeutics), and others. To know more about the number of competing drugs in development, visit @ TEPMETKO Market Positioning Compared to Other Drugs Key Milestones of TEPMETKO In February 2024, the FDA granted traditional approval to TEPMETKO for adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. In February 2022, the EC approved TEPMETKO as monotherapy for the treatment of adult patients with advanced NSCLC harboring alterations leading to METex14 skipping who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy. In February 2021, Merck announced that the US FDA has approved TEPMETKO following priority review for the treatment of adult patients with metastatic NSCLC harboring MET exon 14 skipping alterations. This indication was approved under accelerated approval based on ORR and DOR. In October 2020, TEPMETKO received ODD for treating NSCLC with MET genomic tumor aberrations In March 2020, EMD Serono (the biopharmaceutical business of Merck KGaA), announced that the MHLW approved TEPMETKO for the treatment of patients with unresectable, advanced, or recurrent NSCLC with METex14 skipping alterations. In September 2019, the US FDA granted BTD for tepotinib in patients with metastatic NSCLC harboring METex14 skipping alterations who progressed following platinum-based cancer therapy Discover how TEPMETKO is shaping the NSCLC treatment landscape @ TEPMETKO NSCLC TEPMETKO Market Dynamics TEPMETKO competes in a growing but highly specialized market where MET-targeted therapies are gaining traction due to their efficacy in addressing MET-altered tumors. The market for MET inhibitors is expanding as precision oncology advances and molecular diagnostics become more widely available, enabling better identification of patients who would benefit from targeted treatments like TEPMETKO. A key factor shaping TEPMETKO's market dynamics is competition. It directly competes with Novartis' TABRECTA (capmatinib), another MET inhibitor approved for the same indication. While TEPMETKO offers the advantage of once-daily dosing compared to TABRECTA's twice-daily regimen, both drugs have similar efficacy profiles, making physician and patient preference an important differentiator. Additionally, broader competition from next-generation MET inhibitors and combination therapies in clinical trials could impact TEPMETKO's long-term market position. Regulatory approvals and market access play a crucial role in TEPMETKO's adoption. The drug has been approved in multiple regions, including the U.S., Europe, and Japan, but reimbursement and pricing strategies vary by market. Payer policies, along with the cost-benefit analysis of MET inhibitors compared to other targeted therapies, influence prescription trends. Furthermore, real-world evidence and post-marketing studies will be critical in demonstrating TEPMETKO's sustained effectiveness and safety, which could support expanded indications and increased market penetration. Looking ahead, the MET inhibitor market is expected to grow with advances in biomarker-driven therapy, further refining patient selection. TEPMETKO's success will depend on continued clinical development, potential label expansions, and strategic partnerships to strengthen its competitive edge. As new entrants emerge, Merck KGaA's ability to differentiate TEPMETKO through combination strategies or enhanced formulations may determine its long-term sustainability in this evolving landscape. Dive deeper to get more insight into TEPMETKO's strengths & weaknesses relative to competitors @ TEPMETKO Market Drug Report Table of Contents Related Reports Non-small Cell Lung Cancer Market Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key NSCLC companies including Daiichi Sankyo, AstraZeneca, Gilead Sciences, BieGene, AbbVie, Roche, Merck, Novartis, Pfizer, Takeda Pharmaceuticals, Eli Lilly, BerGenBio, GlaxoSmithKline, Duality biologics, among others. Non-small Cell Lung Cancer Pipeline Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key non-small cell lung cancer companies, including BridgeBio Pharma, Daiichi Sankyo, EMD Serono, Merck, BridgeBio Pharma, Abbvie, Pfizer, Eli Lilly and Company BioNTech SE, Shenzhen TargetRx, Taiho Pharmaceutical, Chong Kun Dang, Bristol Myers Squibb, Innovent Biologics, Xuanzhu Biopharmaceutical, Bayer, GeneScience Pharmaceuticals, InventisBio, Apollomics, Imugene, Ono Pharmaceutical, Pierre Fabre, Jiangsu Hengrui Medicine Co., Bristol-Myers Squibb, Surface Oncology, Inhibrx, Sinocelltech, Mirati Therapeutics, REVOLUTION Medicines, Yong Shun Technology Development, Iovance Biotherapeutics, Galecto Biotech, among others. C-MET Metastatic Non-small Cell Lung Cancer Market C-MET Metastatic Non-small Cell Lung Cancer Market Insights, Epidemiology, and Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key C-MET mNSCLC companies, including Novartis, Merck, EMD Serono, AbbVie, Regeneron Pharmaceuticals, Mythic Therapeutics, Apollomics, Johnson & Johnson Innovation, Haihe Biopharma, among others. C-MET Non-small Cell Lung Cancer Pipeline C-MET Non-small Cell Lung Cancer Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key C-MET non-small cell lung cancer companies, including AbbVie, Janssen Research & Development, Beijing Pearl Biotechnology Limited Liability Company, Novartis, among others. About DelveInsight DelveInsight is a leading Business Consultant and Market Research firm focused exclusively on life sciences. It supports pharma companies by providing comprehensive end-to-end solutions to improve their performance. Get hassle-free access to all the healthcare and pharma market research reports through our subscription-based platform PharmDelve . Contact Us Shruti Thakur [email protected] +14699457679 Logo: SOURCE DelveInsight Business Research, LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Drug ApprovalImmunotherapyPriority Review

20 Feb 2025

·www.pharmaceutical-technology.com

FDA grants priority review for Boehringer’s zongertinib NDA in NSCLC

The therapy is being developed for HER2-mutant advanced NSCLC. Credit: Jo Panuwat D/Shutterstock. The US Food and Drug Administration (FDA) has granted priority review to Boehringer Ingelheim’s new drug application (NDA) for zongertinib to treat unresectable or metastatic non-small cell lung cancer (NSCLC). The decision is intended for individuals who have undergone a previous systemic therapy and have tumours with human epidermal growth factor receptor 2 (HER2) (ERBB2) mutations. A Prescription Drug User Fee Act (PDUFA) action date was set by the agency for the third quarter of 2025. Boehringer Ingelheim Human Pharma head and member of the board of managing directors Shashank Deshpande stated: “We believe zongertinib has the potential to transform the care of previously treated patients with HER2 (ERBB2)-mutant advanced non-small cell lung cancer and are hopeful about the continued research in other tumour types and lines of therapy. “Priority review illustrates the urgent need in this patient population and the possibility for zongertinib to be a groundbreaking innovation for patients with limited treatment options.” The NDA was based on the positive outcomes from the Phase Ib Beamion LUNG-1 trial. Cohort 1 comprised 75 subjects with mutations in the HER2 tyrosine kinase domain. The data from this cohort showed a 71% objective response rate, a six-month progression-free survival rate of 69% and a duration of response rate of 73%. The safety profile of the therapy was determined with only 5% of subjects requiring dose reductions and 3% discontinuing treatment due to adverse effects. The FDA had previously granted breakthrough therapy and fast-track status and Japan’s Pharmaceuticals and Medical Devices Agency had awarded orphan drug designation. An irreversible tyrosine kinase inhibitor, zongertinib selectively targets HER2 mutations while sparing epidermal growth factor receptor, minimising toxicity. Administered orally, it is being developed not only for HER2-mutant advanced NSCLC and evaluated in studies for other solid tumours with HER2 alterations. Boehringer Ingelheim opened a €60m ($66.8m) research building in Vienna, Austria , in September 2024, signalling the company’s intention to expand its presence in the oncology sector.

Priority ReviewFast TrackClinical ResultBreakthrough TherapyNDA

19 Feb 2025

·www.prnewswire.com

Boehringer's zongertinib receives Priority Review from U.S. FDA for the treatment of HER2 (ERBB2)-mutant advanced non-small cell lung cancer

Zongertinib would be the first orally administered, targeted therapy for previously treated patients with HER2 (ERBB2)-mutant advanced non-small cell lung cancer (NSCLC), if approved The application for this investigational treatment is based on positive results from the Phase Ib Beamion LUNG-1, Cohort 1 trial that demonstrated an objective response rate of 71% in 75 previously treated patients with advanced NSCLC HER2 (ERBB2)-mutant advanced NSCLC is linked to poor prognosis and currently has limited treatment optionsi RIDGEFIELD, Conn. and INGELHEIM, Germany, Feb. 19, 2025 /PRNewswire/ -- Boehringer Ingelheim today announced that the U.S. Food and Drug Administration (FDA) has granted Priority Review to its new drug application for zongertinib (BI 1810631) for the treatment of adult patients with unresectable or metastatic non-small cell lung cancer (NSCLC) whose tumors have HER2 (ERBB2) mutations and who have received prior systemic therapy. The FDA grants Priority Review to applications for drugs that would offer significant improvements in the treatment, diagnosis, or prevention of serious conditions, with action expected within six months compared to 10 months under standard review. The Prescription Drug User Fee Act (PDUFA) action date is in the third quarter of 2025. "We believe zongertinib has the potential to transform the care of previously treated patients with HER2 (ERBB2)-mutant advanced non-small cell lung cancer and are hopeful about the continued research in other tumor types and lines of therapy," said Shashank Deshpande, Member of the Board of Managing Directors and Head of Human Pharma at Boehringer Ingelheim. "Priority Review illustrates the urgent need in this patient population and the possibility for zongertinib to be a groundbreaking innovation for patients with limited treatment options." The application was based on results from the positive Phase Ib Beamion LUNG-1 trial. Data from Cohort 1 (N=75) of the study demonstrated an objective response rate (ORR) of 71% with six-month progression-free survival (PFS) and duration of response (DoR) rates of 69% and 73%, respectively, in patients with mutations in the HER2 tyrosine kinase domain. Zongertinib had a safety profile with a low incidence of dose reductions (5%) and treatment discontinuations (3%). The majority of treatment-related adverse events (TRAEs) with zongertinib were mild in nature with diarrhea and rash being the most common all grade TRAEs, at 51% and 27% respectively. No new safety signals were observed. Grade 3 or higher TRAEs occurred in one patient treated with zongertinib. No treatment-related interstitial lung disease (ILD) cases were reported. "Personalized medicine has revolutionized cancer treatment," said GO2 for Lung Cancer's Chief Scientific Officer, Courtney Granville. "Early screening and biomarker testing for mutations provide critical information to guide targeted therapies in personalized medicine. This filing acceptance represents a significant step toward offering another option for individuals with a HER2 (ERBB2) diagnosis, bringing hope and direction to cancer patients." Zongertinib was previously granted Breakthrough Therapy Designation and Fast Track Designation by the FDA. The FDA's Breakthrough Therapy designation is intended to expedite the development and review of a medicine that is intended to treat a serious or life-threatening disease, and preliminary clinical evidence indicates the drug may demonstrate substantial improvement over available treatments. The FDA's Fast Track program is designed to facilitate the development and expedite the review of drugs to treat serious conditions and fill an unmet medical need. In addition to the FDA designations, Japan's Pharmaceuticals and Medical Devices Agency recently granted Orphan Drug Designation to zongertinib. 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 unresectable or metastatic solid tumors with HER2 (ERBB2) alterations. Beamion LUNG-2 is a Phase III, open label, randomized, active-controlled study that is enrolling patients with unresectable or metastatic non-squamous non-small cell lung cancer (NSCLC) harboring HER2 (ERBB2) tyrosine kinase domain mutations to evaluate zongertinib compared with standard of care. About zongertinib Zongertinib (also known as BI 1810631) is an investigational, irreversible tyrosine kinase inhibitor (TKI) that selectively inhibits HER2 (ERBB2) while sparing EGFR, thereby limiting associated toxicities. This orally administered, targeted treatment is being developed for HER2 (ERRB2)-mutant advanced non-small cell lung cancer (NSCLC) and additional clinical studies with zongertinib are ongoing in solid tumors with HER2 alterations. 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.ii NSCLC is the most common type of lung cancer.iii Due to a lack of symptoms and misdiagnoses,iv most patients diagnosed with NSCLC present at stage III or IV, where the disease has metastasized locally or to other organs.v Fewer than 3 in 10 patients are alive five years after a diagnosis of HER2 (ERBB2)-mutant advanced NSCLC.vi 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. HER2 (ERBB2) mutations occur in approximately 2–4% of NSCLC cases and are associated with a poor prognosis and higher incidence of brain metastases.vii,viii Mutations in HER2 (ERBB2) 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.ix 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 . MPR-US-103453 i Nützinger J, Lee JB, Low JL, et al. Lung Cancer. 2023;186:107385. doi:10.1016/j.lungcan.2023.107385 ii International Agency for Research on Cancer – World Health Organization. Rates of trachea, bronchus and lung cancer. Available at: (Accessed: January 2025). iii Zappa C & Mousa Non-small cell lung cancer: current treatment and future advances, Transl Lung Cancer Res. 2016 Jun; 5(3): 288–300. iv American Cancer Society. Signs and Symptoms of Lung Cancer Available at: (Accessed: January 2025). v 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. vi National Cancer Institute Surveillance, Epidemiology, and End Results (SEER). (Accessed: January 2025). vii Baraibar I, et al. Novel drugs targeting EGFR and HER2 exon 20 mutations in metastatic NSCLC. Crit Rev Oncol Hematol. 2020;148:102906. viii Li, B.T. et al. Trastuzumab Deruxtecan in HER2-Mutant Non–Small-Cell Lung Cancer. N Engl J Med. 2022;386:241–51. ix Galogre M, et al. A review of HER2 overexpression and somatic mutations in cancers, Critical Reviews in Oncology/Hematology, Volume 186, 2023, 103997 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

Phase 3Breakthrough TherapyPriority ReviewClinical ResultPhase 1

100 Deals associated with Zongertinib

R&D Status

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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
Adenocarcinoma of Esophagus	Phase 2	Italy	Boehringer Ingelheim GmbH	28 Jun 2024
Adenocarcinoma of Esophagus	Phase 2	Japan	Boehringer Ingelheim GmbH	28 Jun 2024
Adenocarcinoma of Esophagus	Phase 2	Belgium	Boehringer Ingelheim GmbH	28 Jun 2024
Adenocarcinoma of Esophagus	Phase 2	United States	Boehringer Ingelheim GmbH	28 Jun 2024
HER2 Positive Adenocarcinoma of Esophagus	Phase 2	Japan	Boehringer Ingelheim International GmbH	28 Jun 2024
HER2 Positive Adenocarcinoma of Esophagus	Phase 2	Belgium	Boehringer Ingelheim International GmbH	28 Jun 2024
HER2 Positive Adenocarcinoma of Esophagus	Phase 2	United States	Boehringer Ingelheim International GmbH	28 Jun 2024
HER2 Positive Adenocarcinoma of Esophagus	Phase 2	Italy	Boehringer Ingelheim International GmbH	28 Jun 2024
HER2 Positive Adenocarcinoma of Esophagus	Phase 2	Spain	Boehringer Ingelheim International GmbH	28 Jun 2024

Clinical Result

Indication

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04886804 (BEAMION LUNG-1, PRNewswire) Manual	Phase 1	HER2 mutant non-small cell lung cancer	-	zongertinib (每日120毫克，单次服用)	(dylcltrtai) = qpxmmpzwnq ewzpnizybo (vynalezuwz ) View more	Positive	10 Dec 2024
NCT04886804 (Beamion LUNG-1, ESMO_ASIA2024) Manual	Phase 1	HER2 Positive Solid Tumors	105	Zongertinib	(hkcdzdrrfp) = MTD was not reached for BID or QD schedules. wyjlykdtye (dhoqxnqoej ) View more	Positive	07 Dec 2024
				Zongertinib (Asian pts)
NCT04886804 (Beamion LUNG-1, WCLC2024) Manual	Phase 1	HER2 Positive Solid Tumors	83	Zongertinib BID	(ttczyxhjxl) = uhyjczhaai lllbfsfveq (hhamglqjim ) View more	Positive	10 Sep 2024
				Zongertinib QD	(lqrunrroko) = okculwsjlf fvrberkffi (qyfhlbpkkj ) View more
NCT04886804 (Beamion LUNG-1, ASCO2024) Manual	Phase 1	HER2 Positive Solid Tumors	61	Zongertinib 15/30/60/100/150 mg BID	(syuedzalwx) = psamgojonk kqoygwbxqr (hdfcnikipg ) View more	Positive	24 May 2024
				Zongertinib 60/120/180/240/300/360 mg QD	(syuedzalwx) = klgonpmvih kqoygwbxqr (hdfcnikipg ) View more
NCT04886804 (Beamion LUNG-1, ESMO_ELCC2024) Manual	Phase 1	HER2 Positive Solid Tumors \| HER2 mutant non-small cell lung cancer	103	Zongertinib	(dzflgyfjgf) = qlfuulvudf okftpvcwpw (hmgkqazmvy ) View more	Positive	22 Mar 2024
				Zongertinib (Ph Ib)	(ndgpuihxrv) = xlqhcytnrj gmxsnflugt (lvvvltzncn ) View more
NCT04886804 (Beamion Lung 1, WCLC2023) Manual	Phase 1	HER2 Positive Solid Tumors HER2 Positive	43	BI 1810631	(npbuygouzn) = 4 DLTs have been observed (all outside of the MTD evaluation period; grade [G] 2 edema [60 mg BID], G2 diarrhea [150 mg BID], G3 anemia [60 mg QD], G3 increased ALT [180 mg QD]). dfiwbaujeb (hrookvrjbt ) View more	Positive	11 Sep 2023
NCT04886804 (ESMO_ELCC2023) Manual	Phase 1	HER2 Positive Solid Tumors HER2 positive	34	BI 1810631	(uvlbyssdtv) = dzqhxlwuuv rnewpatmwh (kprxmnjfri ) View more	Positive	31 Mar 2023
				BI 1810631 (NSCLC)	(cqrwbupjmh) = ryrpgfmvql szsgomujbp (ovfpkgplcn ) View more

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