RegulationSpecial Review Project (China), Orphan Drug (Japan), Fast Track (Japan), Breakthrough Therapy (United States), Priority Review (United States), Accelerated Approval (United States)

Structure/Sequence

Molecular FormulaC29H28N6O2

InChIKeyAHYMHWXQRWRBKT-UHFFFAOYSA-N

CAS Registry1100598-32-0

View All Structures (2)

Clinical Trials associated with Tepotinib Hydrochloride Hydrate

NCT06908993

/ Not yet recruitingPhase 3IIT

A Randomized Controlled Trial of Tepotinib vs Standard Treatment in Patients With Advanced MET Exon 14 Mutated Non-Small Cell Lung Cancer

We hypothesize that tepotinib is more effective than the investigator's choice of treatment in patients with MET-mutated NSCLC who have progressed after at least one first-line treatment.
The main benefit concerns patient access to tepotinib. There is currently no access to a new-generation MET TKI in France for METex14 patients, due to lack of comparative data. There are no phase III RCTs underway anywhere in the world. This study is the only opportunity, perhaps the last, to generate comparative data which, if positive, will enable the drug to be reimbursed. With this in mind, the methodology of this study was discussed with the HAS on several occasions beforehand, to ensure that it met their expectations. With a response rate of around 50% and a median progression-free survival of 11 months in previously-treated subjects based on clinical trials data, tepotinib is a key drug for METex14 NSCLC patients, who are generally elderly and frail, and for whom therapeutic options are limited.
We expect to observe a benefit for patients treated with tepotinib compared to the control arm in terms of PFS, quality of life, objective response rate and duration of response. The overall survival benefit may be compromised by allowing patients in the control arm to cross over to tepotinib once they have progressed. However, we have decided to maintain this crossover and consequently use PFS as the primary endpoint, as there is no clinical equipoise regarding the efficacy of tepotinib in METex14 NSCLC patients. The EMA has already approved tepotinib based on efficacy and safety data from clinical trials, and patients and investigators already consider this treatment as an important therapeutic option. Indeed, both ESMO and ASCO guidelines recommend the use of MET TKIs in these patients. In France, although neither tepotinib nor capmatinib are available, crizotinib, a multi-target TKI also active on MET, can be used off-label. If cross-over to tepotinib was not allowed in this trial, most patients would still benefit from cross-over to a MET TKI by receiving off-label crizotinib, which would in any case lead to a misinterpretation of the OS data. Therefore, we believe it is preferable to control for cross-over and expose progressive patients in the control arm to tepotinib and use PFS as the primary endpoint.
Toxicity of MET TKIs is considered as manageable. In the VISION trial, of 313 patients treated with tepotinib (median age: 72 years), 109 (34.8%) experienced grade ≥3 treatment-related adverse events, leading to discontinuation in 46 patients (14.7%). Rates of adverse events (AE) were broadly consistent irrespective of prior therapies. Edema, the most common adverse event of clinical interest (AECI), was reported in 67.1% (grade ≥ 3, 11.2%). Median time to first edema onset was 7.9 weeks (range: 0.1-58.3). Edema was manageable with supportive measures, dose reduction (18.8%), and/or treatment interruption (23.1%), and rarely prompted discontinuation (4.3%). Other AECIs were also manageable and predominantly mild/moderate: hypoalbuminemia, 23.6% (grade ≥ 3, 3.5%); creatinine increase, 22.0% (grade ≥ 3, 1.0%); nausea, 23.3% (grade ≥ 3, 0.6%), diarrhea, 22.4% (grade ≥ 3, 0.3%), decreased appetite (grade ≥ 3, 0.3%), and ALT increase, 14.1% (grade ≥ 3, 2.2%). GI AEs typically occurred early and resolved in the first weeks10,13.
Given the efficacy of tepotinib, the manageable safety profile, and the oral administration of tepotinib, we anticipate that treatment with tepotinib will be associated with improved quality of life.
Treatments offered in the control group correspond to standard treatments for advanced NSCLC in second line or beyond. In terms of prior lines of treatment, the eligibility criteria of the trial are aligned with the EMA label of tepotinib: "indicated for the treatment of adult patients with advanced non-small cell lung cancer (NSCLC) harboring alterations leading to MET gene exon 14 (METex14) skipping, who require systemic therapy following prior treatment with immunotherapy and/or platinum-based chemotherapy". We have not included platinum-based chemotherapy as a treatment option in the control arm, considering that patients who are eligible to platinum-based chemotherapy should have received this regimen in first-line, as per ESMO guidelines14. Given the low efficacy of immunotherapy in patients with oncogene addiction, it is unlikely that some patients would receive immunotherapy alone as first-line treatment. Thus, the absence of platinum-based chemotherapy as a treatment choice in the control arm seems reasonable and will reduce the heterogeneity of this arm.

Start Date15 Jul 2025

Sponsor / Collaborator

Intergroupe Francophone Cancerologie Thoracique

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

100 Clinical Results associated with Tepotinib Hydrochloride Hydrate

100 Translational Medicine associated with Tepotinib Hydrochloride Hydrate

100 Patents (Medical) associated with Tepotinib Hydrochloride Hydrate

298

Literatures (Medical) associated with Tepotinib Hydrochloride Hydrate

01 May 2025·Clinical Lung Cancer

A Phase II, Open Label, Single-Arm Study on the Efficacy of Cabozantinib in Patients With Advanced/Metastatic Nonsmall Cell Lung Cancer Harboring MET Exon 14 Alterations who Developed Acquired Resistance to Tepotinib or Capmatinib (CAPTURE Trial)

Article

Author: Ota, Masahide ; Nogami, Naoyuki ; Masuda, Takeshi ; Tanaka, Hiroshi ; Takahama, Takayuki ; Shimokawa, Mototsugu ; Shukuya, Takehito ; Iwama, Eiji ; Oki, Masahide ; Takeda, Masayuki ; Umemura, Shigeki ; Sugawara, Shunichi

BACKGROUNDMET gene exon 14 skipping was identified as a potential driver mutation that occurs in approximately 3%-4% of patients with nonsmall cell lung cancer (NSCLC), typically in the absence of other driver mutations. Capmatinib and tepotinib were the first MET- tyrosine kinase inhibitors (MET-TKIs) approved by the FDA and PMDA, specifically for patients with metastatic NSCLC. Several studies have reported acquired resistance after MET-TKI treatment for MET mutation-positive NSCLC. Sequencing of the MET kinase region of resistant cell lines revealed secondary mutations at residues D1228 and Y1230 that were sensitive to type II MET-TKIs, such as cabozantinib. This suggested that sequential administration of other MET-TKIs may overcome the development of secondary mutations after acquired resistance in MET exon 14 mutation-positive NSCLC.METHODSWe designed the single arm phase II study CAPTURE Trial to assess the efficacy of cabozantinib in patients with advanced/metastatic NSCLC with activating MET exon 14 alterations who developed acquired resistance to tepotinib or capmatinib, as well as after 2 prior chemotherapy regimens that included platinum and docetaxel. The primary endpoint was objective response rate by independent review committees. The sample size (n = 30) is calculated by assuming a threshold response rate of 5% and an expected response rate of 25%. Recruitment began in August 2024.RESULTSThis ongoing study aimed to evaluate the safety and efficacy of cabozantinib after acquired resistance to tepotinib or capmatinib.

01 Apr 2025·International Journal of Biological Macromolecules

Tepotinib interaction triggers a slight effect on the overall stability of hemoglobin protein, reinforcing the potential suitability as a drug candidate against gastric cancer

Article

Author: Wu, Donghao ; Wu, Xiangyuan ; Wen, Jingyun ; Lin, Zexiao

The interaction of anticancer agents with blood proteins can significantly impact their pharmacokinetics and pharmacodynamics. This study investigates the interaction of tepotinib, a MET inhibitor, with human hemoglobin (Hb) and its anticancer effects on SNU-620 gastric cancer (GC) cells. UV-visible spectroscopy revealed a slight reduction in Hb stability upon tepotinib binding, with a decrease in melting temperature (Tm) from 62 °C to 60 °C. Circular dichroism (CD) analysis showed a minor decrease in Hb's α-helical content, while fluorescence spectroscopy confirmed a strong binding affinity with spontaneous and exothermic interaction. Molecular docking identified Trp 37 at the α1β2 interface as the primary binding site, stabilized by Arg 141, Thr 137, Lys 127, and Ser 131 through hydrogen bonding. Molecular dynamics simulations (200 ns) confirmed the stability of the Hb-tepotinib complex. Cellular assays demonstrated that tepotinib effectively inhibited SNU-620 GC cell proliferation (IC₅₀ = 10 nM) by promoting apoptosis, with caspase-3 upregulation and anti-apoptotic protein downregulation. Since drug-protein interactions play a crucial role in drug bioavailability, stability, and therapeutic efficacy, understanding these interactions is essential for optimizing tepotinib's clinical application.

01 Apr 2025·Molecular Diversity

Targeting AFP-RARβ complex formation: a potential strategy for treating AFP-positive hepatocellular carcinoma

Article

Author: Raju, Rajesh ; Abhinand, Chandran S ; Kalath, Haritha ; Ramakrishnan, Krishnapriya ; Revikumar, Amjesh ; Vishwakarma, Riya ; Banjan, Bhavya ; Rehman, Niyas ; Dev, Radul R ; Soman, Sowmya ; Kumar, Pankaj

Alpha-fetoprotein (AFP) is a glycoprotein primarily expressed during embryogenesis, with declining levels postnatally. Elevated AFP levels correlate with pathological conditions such as liver fibrosis, cirrhosis, and hepatocellular carcinoma (HCC). Recent investigations underscore AFP's intracellular role in HCC progression, wherein it forms complexes with proteins like Phosphatase and tensin homolog (PTEN), Caspase 3 (CASP3), and Retinoic acid receptors and Retinoid X receptors (RAR/RXR). RAR and RXR regulate gene expression linked to cell death and tumorigenesis in normal physiology. AFP impedes RAR/RXR dimerization, nuclear translocation, and function, promoting gene expression favoring cancer progression in HCC that provoked us to target AFP as a drug candidate. Despite extensive studies, inhibitors targeting AFP to disrupt complex formation and activities remain scarce. In this study, employing protein-protein docking, amino acid residues involved in AFP-RARβ interaction were identified, guiding the definition of AFP's active site for potential inhibitor screening. Currently, kinase inhibitors play a significant role in cancer treatment and, the present study explores the potential of repurposing FDA-approved protein kinase inhibitors to target AFP. Molecular docking with kinase inhibitors revealed Lapatinib as a candidate drug of the AFP-RARβ complex. Molecular dynamics simulations and binding energy calculations, employing Mechanic/Poisson-Boltzmann Surface Area (MM-PBSA), confirmed Lapatinib's stability with AFP. The study suggests Lapatinib's potential in disrupting the AFP-RARβ complex, providing a promising avenue for treating molecularly stratified AFP-positive HCC or its early stages.

News (Medical) associated with Tepotinib Hydrochloride Hydrate

31 Mar 2025

·www.echemi.com

Merck and Roche Join Forces for Tepotinib Commercialization in China

On March 26, 2025, Merck and Roche Pharmaceuticals officially announced a strategic partnership aimed at accelerating the commercialization of Tepotinib (brand name: Togetican®) in the mainland Chinese market. Industry analysts suggest that Merck is leveraging Roche's distribution network in China to expedite the launch of this groundbreaking drug. Tepotinib is the world's first approved MET inhibitor, developed by Merck in Germany. It is an oral, highly selective MET tyrosine kinase inhibitor designed to block cancer signaling pathways caused by MET gene mutations. The drug received approval in Japan in March 2020 for treating patients with unresectable, advanced, or recurrent non-small cell lung cancer (NSCLC) harboring MET exon 14 skipping mutations. In February 2021, Tepotinib gained accelerated approval from the FDA for treating adult patients with metastatic NSCLC who also have these mutations. In December 2023, the drug was officially approved for use in mainland China, targeting locally advanced or metastatic NSCLC patients with MET exon 14 skipping mutations. It was included in the national health insurance catalog by the end of 2024, with implementation starting January 1, 2025. Clinical trials have validated Tepotinib's efficacy, demonstrating its high selectivity and good tolerability, particularly in Asian populations. The drug has received endorsements from prestigious guidelines like NCCN and CSCO. Currently, several MET inhibitors have received global approval, including: Capmatinib (developed by Novartis), which was approved by the FDA in May 2020 as the first targeted therapy for MET exon 14 skipping mutations in NSCLC. In clinical trials, it showed an objective response rate (ORR) of 67.9% in treatment-naive patients. Savolitinib (developed by Hutchison China MediTech), the only MET inhibitor approved in China, also demonstrated encouraging efficacy in patients with MET exon 14 skipping mutations. However, Tepotinib will face competition from domestic MET inhibitors such as Gumetinib from Allergan, which is currently in late-stage clinical trials and could enter the market at a lower price point. Lung cancer remains a leading cause of morbidity and mortality globally, with non-small cell lung cancer (NSCLC) accounting for approximately 85%-90% of cases. The incidence of MET exon 14 skipping mutations in NSCLC patients is about 1%-4%, which, while relatively rare, translates to a significant number of patients given the large patient population and limited treatment options. This partnership is pivotal for Roche, enabling it to expand its footprint in lung cancer treatment. By incorporating Tepotinib into its portfolio, Roche enhances its competitive edge in the precision treatment market for lung cancer, moving beyond its existing focus on ALK and NTRK/ROS1 mutations. Merck's expertise in drug development and innovation combined with Roche's rich experience in commercialization will likely bolster Tepotinib's market competitiveness, promising substantial commercial value for both companies. The success of this collaboration could set a new benchmark in the treatment of lung cancer.

Drug Approval

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/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/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

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
Advanced Hepatocellular Carcinoma	Discovery	Taiwan Province	Merck KGaA	06 Jan 2014
Advanced Hepatocellular Carcinoma	Discovery	China	Merck KGaA	06 Jan 2014
Advanced Hepatocellular Carcinoma	Discovery	South Korea	Merck KGaA	06 Jan 2014
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	Taiwan Province	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	Italy	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	China	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	Spain	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	Malaysia	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	South Korea	Merck KGaA	23 Dec 2013
EGFR mutation MET positive Non-small Cell Lung Cancer	Discovery	Singapore	Merck KGaA	23 Dec 2013

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02864992 (VISION study, ESMO_ELCC2025)	Phase 2	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer First line METex14 skipping \| METamp	313	Tepotinib 500 mg	kqzzbgokpf(rbphissdbj) = 15.7% of pts discontinued treatment due to TRAEs urocifaeco (lpnfgpizli ) View more	Positive	26 Mar 2025
NCT03940703 (INSIGHT 2, Pubmed) Manual	Phase 2	Non-Small Cell Lung Cancer Second line \|	128	Tepotinib plus osimertinib (progression on first-line osimertinib)	(etlevqrxub) = djtchzkpnx mwwxjialjm (awjldrnybn, 39.7 - 60.3) View more	Positive	25 Aug 2024
NCT03546608 (CTgov)	Phase 1	Hepatic Insufficiency	18	Tepotinib (Healthy Participants (Control))	aydtwgdfde(ydncxumpam) = mdkyqexank nwamjdlvyv (itjfiuvlsd, xloeijajkc - ngjunrkfyp) View more	-	12 Aug 2024
				Tepotinib (Mild Hepatic Impairment (Child-Pugh Class A))	aydtwgdfde(ydncxumpam) = gcjhtdubae nwamjdlvyv (itjfiuvlsd, jojqgoofjx - gokgcdxupz) View more
NCT02864992 (VISION, ASCO2024) Manual	Phase 2	Non-Small Cell Lung Cancer	248	tepotinib (Brain metastases)	(awnbuhwqlx) = azpnxfoysd fkkrhjooah (ogtwimssxh, 2.41) View more	Positive	24 May 2024
				tepotinib (Liver metastases)	(awnbuhwqlx) = ikjcsttnlk fkkrhjooah (ogtwimssxh, 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	(xveizeljcq) = kwzloudgcr fqmxnjpbzn (pklseyugez ) View more	Positive	24 May 2024
				Placebo	(xveizeljcq) = hwvragafcg fqmxnjpbzn (pklseyugez ) View more
NCT02864992 (VISION, Pubmed \| Br J Cancer)	Phase 2	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer	106	tepotinib 500 mg	(epfvbzvqve) = jyghzbsnkv euujujntgp (kaxipcsusu ) View more	Positive	04 Apr 2024
NCT05213481 (CTgov)	Phase 1	-	18	Carbamazepine+Tepotinib	qhrlfsihcc(zhcwdanamd) = eaivbbubes kttqcubqgm (mrbjgmgzrs, acdcrvwmnw - lrxdzebyod) View more	-	08 Mar 2024
NCT05203822 (CTgov)	Phase 1	-	18	Tepotinib (Tepotinib)	gzexjxojnz(mngntridgr) = cnksdyadnt bfhzkcfvuq (qnfzkadspp, zycuafrqpb - ntxyfaurkb) View more	-	20 Feb 2024
				Itraconazole+Tepotinib (Tepotinib and Itraconazole)	gzexjxojnz(mngntridgr) = ifokrpdgvb bfhzkcfvuq (qnfzkadspp, qruwzdwutc - jdizvddlnm) View more
NCT04204902 (CTgov)	Phase 1	-	18	Tepotinib (Tepotinib Test Treatment)	rjnpytkoae(qxeqqjwqws) = nlbwqgxypz tnsbvlpvut (hbyaitkibo, kvmvnwvkyf - agvbeiqcgx) View more	-	08 Nov 2023
				Tepotinib (Tepotinib Reference Treatment)	rjnpytkoae(qxeqqjwqws) = qphwlgnixx tnsbvlpvut (hbyaitkibo, zumjvzgdrb - ggzueoudhy) View more
NCT02864992 (VISION, ESMO 12023 \| ESMO 22023) Manual	Phase 2	Advanced Lung Non-Small Cell Carcinoma	313	tepotinib (Treatment-naive; T+/L–)	(nhjsxuzvub) = eytteptqvt pimvhgyvwo (tyhcdzhkth, 43.2 - 71.3) View more	Positive	23 Oct 2023
				tepotinib (Treatment-naive; T+/L+)	(nhjsxuzvub) = eluklqwmef pimvhgyvwo (tyhcdzhkth, 48.0 - 78.4) View more

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis