RegulationAccelerated Approval (United States), Orphan Drug (United States), Special Review Project (China), Orphan Drug (South Korea), Orphan Drug (Australia), Fast Track (Japan), Priority Review (United States), Breakthrough Therapy (United States), Orphan Drug (Japan)

Structure/Sequence

Molecular FormulaC29H31ClN6O3

InChIKeyKZVOMLRKFJUTLK-UHFFFAOYSA-N

CAS Registry1946826-82-9

Clinical Trials associated with Tepotinib Hydrochloride Hydrate

NCT06031688

/ RecruitingPhase 2IIT

A Randomized Phase II Study of Tepotinib With or Without Ramucirumab in Participants With MET Exon 14 Skipping Positive Stage IV or Recurrent Non-Small Cell Lung Cancer (LUNG-MAP SUB-STUDY)

This phase II Expanded Lung-MAP treatment trial tests tepotinib with or without ramucirumab for the treatment of patients with advanced non-small cell lung cancer that has spread from where it first started (primary site) to other places in the body (stage IV) or that has come back after a period of improvement (recurrent). Tepotinib is used in patients whose cancer has a mutated (changed) form of a gene called MET. It is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal MET protein that signals tumor cells to multiply. This helps slow or stop the spread of tumor cells. Ramucirumab is a monoclonal antibody that may prevent the growth of new blood vessels that tumors need to grow. Giving tepotinib with ramucirumab may lower the chance of the cancer from growing or spreading in patients with stage IV or recurrent non-small cell lung cancer.

Start Date08 Aug 2024

Sponsor / Collaborator

Eli Lilly & Co.

[+2]

NCT06083857

/ RecruitingPhase 1/2IIT

An Open-Label Phase I/II Study to Evaluate the Safety and PrelimiBasnary Efficacy of Amivantamab and Tepotinib Combination in MET-altered Non-small Cell Lung Cancer (NSCLC)

To learn if the combination of amivantamab and tepotinib can help to control NSCLC. The safety of this drug combination will also be studied.

Start Date18 Jun 2024

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

NCT06106802

/ Not yet recruitingPhase 2IIT

Lazertinib and Tepotinib for EGFR Mutant NSCLC in MET Overexpressed or Amplified Who Progressed After Lazertinib Treatment: A Phase II Multi-center Trial

As the 3rd generation, EGFR TKI has become a standard treatment option for the 1st line therapy in EGFR mutated patients, the necessity for evaluating resistant mechanism to determine the matched subsequent therapeutic option has been highlighted. From the 1st line Osimertinib treatment, the heterogenous resistance mechanism has been observed showing most commonly by MET amplification (7-15%) followed by additional on-target EGFR mutation (6-10%), BRAF, PI3KCA, KRAS, HER2 mutation (13-14%) and still 40 to 50% remain unknown for the mechanism. (A. Leonetti et al.British Journal of Cancer(2019))
Based on the observation showing the MET amplification as the most common resistance mechanism to the 3rd generation EGFR TKI treatment, the "TATTON" study, a multi-arm, phase IB trial, demonstrated early clinical data of Osimertinib in combined with savolitinib. Among the patients, c-MET amplified patients who were previously treated with 3rd generation EGFR TKI, a combination of Osimertinib and savolitinib, showed an objective response rate of 33% and median PFS of 5.5 months. (G. Oxnard et al. Annals of Oncology(2020))
The clinical efficacy of Osimertinib with savolitinib in MET overexpressed or amplification patients are reported from the global phase II, "SAVANNAH" study. The preliminary results from the SAVANNAH trial showed that Osimertinib plus savolitinib demonstrated an objective response rate of 49% in patients with a high level of MET overexpression and/or amplification, defined as IHC90+ and/or FISH 10+, whose disease progressed on treatment with Osimertinib. The highest ORR was observed in patients with a high level of MET who were not treated with prior chemotherapy (52%). In patients whose tumors did not show a high level of MET, the ORR was 9% (MJ Ahn, WCLC, 2022). There are ongoing global Phase III SAFFRON study to validate the outcome from SAVANNAH study.
It has been reported that around 62% of tumor in Osimertinib progressed sample has MET overexpression and/or amplification, and more than one-third (34%) met the defined high MET level cut-off.
As Lazertinib is about to be approved as the treatment option for the treatment naïve EGFR mutated NSCLC, it is also becoming important to develop a further treatment plan based on the MET amplification status. In this study, the investigators designed a phase II study based on the MET amplification status to evaluate the clinical efficacy of Lazertinib + tepotinib.

Start Date02 Feb 2024

Sponsor / Collaborator

Samsung Medical Center

100 Clinical Results associated with Tepotinib Hydrochloride Hydrate

100 Translational Medicine associated with Tepotinib Hydrochloride Hydrate

100 Patents (Medical) associated with Tepotinib Hydrochloride Hydrate

290

Literatures (Medical) associated with Tepotinib Hydrochloride Hydrate

13 Feb 2025·JOURNAL OF MEDICINAL CHEMISTRY

Rational Design, Synthesis, and Biological Evaluation of Novel c-Met Degraders for Lung Cancer Therapy

Article

Author: Peng, Yong ; Luo, Dongdong ; Zhang, Tingting ; Qiu, Xingyang ; Ai, Min ; He, Jianhua ; Ming, Yue ; Pu, Wenchen ; Zheng, Qingquan

Cellular-mesenchymal epithelial transition factor (c-Met) is an attractive target for treating multiple cancers. Despite plentiful c-Met inhibitors have been developed, some issues, including the acquired drug resistance to c-Met inhibitors, have emerged to hamper their application in clinical treatment. Degradation of c-Met offers an opportunity to solve these issues. In this study, we developed a series of c-Met degraders, and the optimal compound 22b can efficiently degrade c-Met with a DC₅₀ value of 0.59 nM in EBC-1 cells. Mechanistic studies revealed that compound 22b induced c-Met degradation via proteasome-mediated pathway. In addition, compound 22b suppressed the proliferation and also induced apoptosis of EBC-1 cells, outperforming the corresponding inhibitor tepotinib. Importantly, compound 22b showed favorable pharmacokinetic properties and significantly induced tumor regression in a xenograft model without obvious toxicity. In brief, this study provided compound 22b as a novel c-Met degrader for lung cancer therapy.

17 Jan 2025·ONCOLOGIST

Prolonged complete response to adjuvant tepotinib in a patient with newly diagnosed disseminated glioblastoma harboring mesenchymal-epithelial transition fusion

Article

Author: Swanson, Todd ; Highsmith, Kaitlin ; Schumacher, Karl Maria ; O’Brien, Barbara J ; Nash, Sebnem ; Weller, Lauryn ; Vlassak, Soetkin ; Aaroe, Ashley ; Pham, Lily C ; Gann, Claudia N ; Majd, Nazanin K ; de Groot, John F

Abstract:

The prognosis of patients with glioblastoma (GBM) remains poor despite current treatments. Targeted therapy in GBM has been the subject of intense investigation but has not been successful in clinical trials. The reasons for the failure of targeted therapy in GBM are multifold and include a lack of patient selection in trials, the failure to identify driver mutations, and poor blood-brain barrier penetration of investigational drugs. Here, we describe a case of a durable complete response in a newly diagnosed patient with GBM with leptomeningeal dissemination and PTPRZ1-MET fusion who was treated with tepotinib, a brain-penetrant MET inhibitor. This case of successful targeted therapy in a patient with GBM demonstrates that early molecular testing, identification of driver molecular alterations, and treatment with brain-penetrant small molecule inhibitors have the potential to change the outcome in select patients with GBM.

01 Jan 2025·INTERNAL MEDICINE

Kidney Injury in Patient with Non-small-cell Lung Cancer Receiving Tepotinib

Article

Author: Mitani, Reo ; Oda, Naohiro ; Takata, Ichiro ; Tokura, Takehiko ; Onishi, Akifumi

We herein report a 68-year-old man with advanced non-small-cell lung cancer treated with tepotinib who showed marked general edema, hypoalbuminemia, and an elevated serum creatinine level. Although tepotinib-induced kidney injury due to creatinine transporter inhibition has been reported, renal biopsy findings suggested tubulointerstitial injury due to decreased renal blood flow, likely secondary to refractory fluid retention. This case highlights the potential for true kidney injury during tepotinib therapy and underscores the importance of careful monitoring and management of adverse renal effects.

News (Medical) associated with Tepotinib Hydrochloride Hydrate

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

18 Nov 2024

·www.businesswire.com

U.S. Food and Drug Administration Approves FoundationOne®Liquid CDx as a Companion Diagnostic for TEPMETKO® (tepotinib) to Identify Patients with MET Exon 14 Skipping Alterations in Non-Small Cell Lung Cancer

BOSTON--( BUSINESS WIRE )-- Foundation Medicine, Inc. today announced that it has received approval from the U.S. Food and Drug Administration (FDA) for FoundationOne ® Liquid CDx to be used as a companion diagnostic for TEPMETKO ® (tepotinib) developed by EMD Serono, the healthcare business of Merck KGaA, Darmstadt, Germany in the U.S. and Canada. TEPMETKO received accelerated approval from the FDA in February 2021 and traditional approval in February 2024 for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition ( MET ) exon 14 skipping alterations ( MET ex14). 1 FoundationOne Liquid CDx is the first FDA-approved companion diagnostic to identify patients who may be eligible for TEPMETKO. NSCLC accounts for approximately 85% of lung cancers, 2 of which 3-4% are associated with MET ex14. 3 MET ex14 skipping alterations in patients have been associated with advanced disease and a poor prognosis. 4 “Access to a high-quality liquid biopsy, like FoundationOne Liquid CDx, can help unlock the power of precision medicine for more patients with non-small cell lung cancer,” said Mia Levy, M.D., Ph.D., chief medical officer at Foundation Medicine. “We’re proud that our liquid biopsy is the first companion diagnostic approved in the U.S. for TEPMETKO as it will help identify more patients with MET ex14 skipping alterations who may be appropriate for targeted treatment.” Foundation Medicine is the only company with an FDA-approved portfolio of tissue and blood-based comprehensive genomic profiling tests. From a routine blood sample, FoundationOne Liquid CDx analyzes more than 300 cancer-related genes to provide genomic insights. With today’s approval, Foundation Medicine has more than 19 FDA-approved companion diagnostic indications for NSCLC, the most of any company. 5 “Targeted therapies have led a revolution to how lung cancer is treated,” said GO2 for Lung Cancer President and CEO Laurie Ambrose. “Biomarker testing plays a crucial part in getting these treatments into the hands of patients. We’re excited to see that patients with advanced NSCLC have more access to treatment options because of non-invasive liquid biopsies.” Foundation Medicine is the global leader in approved companion diagnostic indications, with 50% of all approved companion diagnostic indications for next-generation sequencing (NGS) testing in the United States and Japan. 6 Foundation Medicine ® and FoundationOne ® are registered trademarks of Foundation Medicine, Inc. About Foundation Medicine: Your Essential Partner in Cancer Care Foundation Medicine is a pioneer in molecular profiling for cancer, working to shape the future of clinical care and research. We collaborate with a broad range of partners across the cancer community and strive to set the standard for quality, scientific excellence, and regulatory leadership. Our deep understanding of cancer biology helps physicians make informed treatment decisions for their patients and empowers researchers to develop new medicines. Every day, we are driven to help our partners find answers and take action, enabling more people around the world to benefit from precision cancer care. For more information, please visit us on www.FoundationMedicine.com and follow us on LinkedIn and X . About FoundationOne ® Liquid CDx FoundationOne ® Liquid CDx is a qualitative next generation sequencing based in vitro diagnostic test for prescription use only that uses targeted high throughput hybridization-based capture technology to analyze 324 genes utilizing circulating cell-free DNA (cfDNA) isolated from plasma derived from anti-coagulated peripheral whole blood of advanced cancer patients. The test is FDA-approved to report short variants in over 300 genes and is a companion diagnostic to identify patients who may benefit from treatment with specific therapies (listed in Table 1 of the Intended Use) in accordance with the approved therapeutic product labeling. Additional genomic findings may be reported and are not prescriptive or conclusive for labeled use of any specific therapeutic product. Use of the test does not guarantee a patient will be matched to a treatment. A negative result does not rule out the presence of an alteration. Patients who are negative for companion diagnostic mutations should be reflexed to tumor tissue testing and genomic alteration status confirmed using an FDA-approved tumor tissue test, if feasible. For the complete label, including companion diagnostic indications and complete risk information, please visit www.F1LCDxLabel.com . ____________________ 1 TEPMETKO. Prescribing Information. EMD Serono; 2024. Accessed May 24, 2024. https://www.emdserono.com/us-en/pi/tepmetko-pi.pdf 2 American Cancer Society. Key Statistics for Lung Cancer. Updated January 29, 2024. Accessed May 22, 2024. https://www.cancer.org/cancer/types/lung-cancer/about/what-is.html 3 The Cancer Genome Atlas Research Network. Comprehensive molecular profiling of lung adenocarcinoma. Nature . 2014;511:543-550. https://doi-org.libproxy1.nus.edu.sg/10.1038/nature13385 4 Awad MM, Leonardi GC, Kravets S, et al. Impact of MET inhibitors on survival among patients with non-small cell lung cancer harboring MET exon 14 mutations: a retrospective analysis. Lung Cancer . 2019;133:96-102. https://doi-org.libproxy1.nus.edu.sg/10.1016/j.lungcan.2019.05.011 5 Data on File, Foundation Medicine, Inc. 2024 6 Data on File, Foundation Medicine, Inc. 2024

Drug Approval

09 Aug 2024

·www.fda.gov

FDA approves tepotinib for metastatic non-small cell lung cancer

FDA approves tepotinib for metastatic non-small cell lung cancer On February 15, 2024, the Food and Drug Administration granted traditional approval to tepotinib (Tepmetko, EMD Serono, Inc.) for adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations. View full prescribing information for Tepmetko. Tepotinib was previously granted accelerated approval for this indication on February 3, 2021, based on initial overall response rate (ORR) and duration of response (DOR) in the VISION trial (NCT02864992), a multicenter, non-randomized, open-label, multicohort study. The conversion to traditional approval was based on an additional 161 patients and an added 28 months of follow-up time to assess DOR. Efficacy was demonstrated in a total of 313 patients with metastatic NSCLC harboring MET exon skipping alterations. Patients received tepotinib 450 mg once daily until disease progression or unacceptable toxicity. The primary efficacy measures were ORR and DOR, determined by a Blinded Independent Review Committee. Among 164 treatment-naïve patients, ORR was 57% (95% CI: 49, 65), with 40% of responders having a DOR ≥12 months. Among 149 previously treated patients, ORR was 45% (95% CI: 37, 53), with 36% of responders having a DOR ≥12 months. The most common adverse reactions (≥20%) were edema, nausea, fatigue, musculoskeletal pain, diarrhea, dyspnea, decreased appetite, and rash. The recommended tepotinib dose is 450 mg orally once daily with food. This review used the Assessment Aid, a voluntary submission from the applicant to facilitate the FDA’s assessment. This application was granted breakthrough designation and orphan drug designation. FDA expedited programs are described in the Guidance for Industry: Expedited Programs for Serious Conditions-Drugs and Biologics. Healthcare professionals should report all serious adverse events suspected to be associated with the use of any medicine and device to FDA’s MedWatch Reporting System or by calling 1-800-FDA-1088. For assistance with single-patient INDs for investigational oncology products, healthcare professionals may contact OCE’s Project Facilitate at 240-402-0004 or email OncProjectFacilitate@fda.hhs.gov. Follow the Oncology Center of Excellence on X (formerly Twitter) @FDAOncologyExternal Link Disclaimer.

Drug ApprovalOrphan DrugAccelerated ApprovalClinical ResultBreakthrough Therapy

100 Deals associated with Tepotinib Hydrochloride Hydrate

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	L01XE	DB15133

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer	South Korea	Merck & Co., Inc.	23 Nov 2021
Non-Small Cell Lung Cancer	United States	EMD Serono, Inc.	03 Feb 2021
c-Met positive non-small cell lung cancer	Japan	Merck KGaA	25 Mar 2020

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	United States	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Belgium	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Czechia	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	France	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Italy	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Russia	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Spain	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	United Kingdom	EMD Serono Research & Development Institute, Inc.	28 Jan 2021
Neoplasm Metastasis	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Solid tumor	Phase 2	South Korea	Merck KGaA	16 Jan 2020

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03940703 (INSIGHT 2, Pubmed) Manual	Phase 2	Non-Small Cell Lung Cancer Second line EGFR Mutation \| MET Amplification	128	Tepotinib plus osimertinib (progression on first-line osimertinib)	wbkaffldtw(enwftbghlo) = adxpbntglv giwacfdhfe (vrlglxujvu, 39.7 - 60.3) View more	Positive	25 Aug 2024
NCT03546608 (CTgov)	Phase 1	Hepatic Insufficiency	18	Tepotinib (Healthy Participants (Control))	nwnicdepkl(aptfbyubtw) = dibkteakbn hkdvyuzzqh (kdhlwwjase, 13.4) View more	-	12 Aug 2024
				Tepotinib (Mild Hepatic Impairment (Child-Pugh Class A))	nwnicdepkl(aptfbyubtw) = jkxgovxpag hkdvyuzzqh (kdhlwwjase, 63.9) View more
NCT02864992 (VISION, ASCO2024) Manual	Phase 2	Non-Small Cell Lung Cancer MET Exon 14 Skipping	248	tepotinib (Brain metastases)	pykpwszpeb(atzelkrjon) = misbzaptfi vuyelfbxqw (uffbszklox, 2.41) View more	Positive	24 May 2024
				tepotinib (Liver metastases)	pykpwszpeb(atzelkrjon) = dihddrwqfw vuyelfbxqw (uffbszklox, 2.27) View more
NCT04647838 (KCSG AL19-17, ASCO2024)	Phase 2	Solid tumor \| Neoplasm Metastasis \| Non-Small Cell Lung Cancer ctDNA \| METex14 \| METamplification ... View more	35	Tepotinib	guyunaszor(limkjrhzlk) = hclhadkuzo kyoleajxhu (hrojvigpcu ) View more	Positive	24 May 2024
				Placebo	guyunaszor(limkjrhzlk) = rqscvujtmt kyoleajxhu (hrojvigpcu ) View more
NCT02864992 (VISION, Pubmed \| Br J Cancer)	Phase 2	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer	106	tepotinib 500 mg	jvlymbhwqi(pipfbmdkui) = lqbtfieshl glytvehdpx (volcnauoin ) View more	Positive	04 Apr 2024
NCT05213481 (CTgov)	Phase 1	-	18	Carbamazepine+Tepotinib	htevivujds(qmwahpsnqc) = hdqlfevbox vbwaehikon (qzlfgudvmo, 14.1) View more	-	08 Mar 2024
NCT05203822 (CTgov)	Phase 1	-	18	Tepotinib (Tepotinib)	rfrubmtzmr(zmwbkurhqs) = seyrpsfbgs hechtlekbw (silydbbbmv, 28.2) View more	-	20 Feb 2024
				Itraconazole+Tepotinib (Tepotinib and Itraconazole)	rfrubmtzmr(zmwbkurhqs) = zkosuclzuh hechtlekbw (silydbbbmv, 29.9) View more
NCT04204902 (CTgov)	Phase 1	-	18	Tepotinib (Tepotinib Test Treatment)	otjiyxvloa(ppdlvlaylx) = isyhqtwoyf gqfqxbhokf (jvqnyqhxli, 28) View more	-	08 Nov 2023
				Tepotinib (Tepotinib Reference Treatment)	otjiyxvloa(ppdlvlaylx) = rtfqepjvyh gqfqxbhokf (jvqnyqhxli, 37.6) View more
NCT02864992 (VISION, ESMO 12023 \| ESMO 22023) Manual	Phase 2	Advanced Lung Non-Small Cell Carcinoma MET Exon 14 Skipping	313	tepotinib (Treatment-naive; T+/L–)	wnfpgrzvbp(xefuzpzmrf) = pfovnjisqc sltqiqdokw (esajhjaclv, 43.2 - 71.3) View more	Positive	23 Oct 2023
				tepotinib (Treatment-naive; T+/L+)	wnfpgrzvbp(xefuzpzmrf) = aifwxwytho sltqiqdokw (esajhjaclv, 48.0 - 78.4) View more
NCT02864992 (VISION, ESMO 12023 \| ESMO 22023) Manual	Phase 2	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer MET Exon 14 Skipping	149	Tepotinib 500 mg	lfgtushqtl(mepdtovuap) = gzpirozetu tdypneabjm (lkjvoakztk ) View more	Positive	23 Oct 2023
				Tepotinib 500 mg (2L+)	lfgtushqtl(mepdtovuap) = ycemwpzayw tdypneabjm (lkjvoakztk ) View more

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