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

Structure/Sequence

Molecular FormulaC29H31ClN6O3

InChIKeyKZVOMLRKFJUTLK-UHFFFAOYSA-N

CAS Registry1946826-82-9

Clinical Trials associated with Tepotinib Hydrochloride Hydrate

CTR20255027

/ Active, not recruitingNot Applicable

评估受试制剂盐酸特泊替尼片与参比制剂盐酸特泊替尼片（拓得康®）在餐后状态下作用于健康成年受试者的单中心、开放、随机、单剂量、交叉生物等效性研究

[Translation] A single-center, open-label, randomized, single-dose, crossover bioequivalence study evaluating the effects of the investigational formulation terpoltinib hydrochloride tablets and the reference formulation terpoltinib hydrochloride tablets (Tordecan®) on healthy adult subjects in a postprandial state.

主要研究目的研究餐后状态下单次口服受试制剂盐酸特泊替尼片与参比制剂盐酸特泊替尼片（拓得康®）在健康成年受试者体内的药代动力学，评价餐后状态下口服两种制剂的生物等效性。次要研究目的研究受试制剂盐酸特泊替尼片和参比制剂“拓得康®”在健康受试者中的安全性。

[Translation]

Primary Study Objective: To investigate the pharmacokinetics of a single oral dose of the test formulation terpoxtinib hydrochloride tablets and the reference formulation terpoxtinib hydrochloride tablets (Tordecan®) in healthy adult subjects after a meal, and to evaluate the bioequivalence of the two formulations after an oral dose. Secondary Study Objective: To investigate the safety of the test formulation terpoxtinib hydrochloride tablets and the reference formulation "Tordecan®" in healthy subjects.

Start Date15 Jan 2026

Sponsor / Collaborator

Qilu Pharmaceutica Hainanco Ltd.

CTR20255024

/ Active, not recruitingNot Applicable

评估受试制剂盐酸特泊替尼片与参比制剂盐酸特泊替尼片（拓得康®）在空腹状态下作用于健康成年受试者的单中心、开放、随机、单剂量、交叉生物等效性研究

[Translation] A single-center, open-label, randomized, single-dose, crossover bioequivalence study evaluating the test formulation terpoltinib hydrochloride tablets versus the reference formulation terpoltinib hydrochloride tablets (Tordecan®) in healthy adult subjects under fasting conditions.

主要研究目的研究空腹状态下单次口服受试制剂盐酸特泊替尼片与参比制剂盐酸特泊替尼片（拓得康®）在健康成年受试者体内的药代动力学，评价空腹状态下口服两种制剂的生物等效性。次要研究目的研究受试制剂盐酸特泊替尼片和参比制剂“拓得康®”在健康受试者中的安全性。

[Translation]

Primary Study Objective: To investigate the pharmacokinetics of a single oral dose of the test formulation terpoxtinib hydrochloride tablets and the reference formulation terpoxtinib hydrochloride tablets (Tordecan®) in healthy adult subjects under fasting conditions, and to evaluate the bioequivalence of the two formulations under fasting conditions. Secondary Study Objective: To investigate the safety of the test formulation terpoxtinib hydrochloride tablets and the reference formulation "Tordecan®" in healthy subjects.

Start Date14 Jan 2026

Sponsor / Collaborator

Qilu Pharmaceutica Hainanco Ltd.

NCT06908993

/ RecruitingPhase 3IIT

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

The hypothesize is 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.
The investigators 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, the investigators 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, the investigators 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, the investigators 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". The investigators 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 Date09 Dec 2025

Sponsor / Collaborator

Intergroupe Francophone Cancerologie Thoracique

100 Clinical Results associated with Tepotinib Hydrochloride Hydrate

100 Translational Medicine associated with Tepotinib Hydrochloride Hydrate

100 Patents (Medical) associated with Tepotinib Hydrochloride Hydrate

264

Literatures (Medical) associated with Tepotinib Hydrochloride Hydrate

31 Dec 2026·RENAL FAILURE

A tri-scale in silico framework integrating pharmacovigilance and mechanistic modeling suggests tepotinib-associated acute kidney injury risk

Article

Author: Bai, Zhixun ; Wang, Qin ; Zheng, Rubin ; Han, Jinfen ; Lyu, Jiayi ; Lu, Jing ; Deng, Miao ; Chen, Jiaxi

Proactive safety evaluation of molecularly targeted therapies requires generalizable frameworks that integrate real-world evidence with mechanistic insights. As a case in point, tepotinib, a mesenchymal-epithelial transition (MET) inhibitor for non-small cell lung cancer, has a known pulmonary toxicity profile, but its link to acute kidney injury (AKI) and underlying mechanism remain unclear. We devised a tri-scale in silico strategy encompassing population-scale pharmacovigilance signal extraction from the FDA Adverse Event Reporting System (FAERS) (2020-2025) via disproportionality analysis (Reporting Odds Ratio, ROR, and Proportional Reporting Ratio, PRR), network toxicology-based multi-target exploration for shared target and hub gene identification, and mechanistic docking-based molecular plausibility assessment using the Cavity-detection guided Blind Docking (CB-Dock2) platform. Pharmacovigilance analysis identified a significant renal impairment signal (ROR = 20.60). Network toxicology suggested potential nephrotoxicity and revealed 173 shared targets and prioritizing six hub genes (HSP90AA1, AKT1, EGFR, CASP3, TNF, SRC). These genes were shown to be critically involved in PI3K-Akt and MAPK pathways. Molecular docking revealed high-affinity binding between tepotiniband all six hub targets (Vina scores: -8.0 to -10.6 kcal/mol), providing a structural basis for the postulated mechanistic link to AKI. These findings not only highlight the necessity for enhanced renal monitoring in tepotinib-treated patients but, more broadly, establish the FAERS-NetDock Pipeline as a reusable, generalizable and hypothesis-generating framework for evaluating tyrosine kinase inhibitors (TKIs)-induced nephrotoxicity; this framework is immediately applicable to profiling the safety of other TKIs (e.g. crizotinib, capmatinib, savolitinib, afatinib and osimertinib) and is readily adaptable for de-risking a wider spectrum of targeted therapies.

01 Feb 2026·EUROPEAN JOURNAL OF CANCER

Targeting driver mutations in lung cancer with interstitial pneumonia: A nationwide study in Japan

Article

Author: Waseda, Yuko ; Tanino, Yoshinori ; Inomata, Minehiko ; Amimoto, Hisanori ; Ogura, Takashi ; Yamauchi, Hiroyoshi ; Ichikado, Kazuya ; Ikeda, Satoshi ; Kinoshita, Yoshiaki ; Hashimoto, Naozumi ; Ozasa, Hiroaki ; Nakamura, Yutaro ; Hashimoto, Seishu ; Murakami, Koji ; Itoh, Taku ; Karayama, Masato ; Isshiki, Takuma ; Kato, Motoyasu ; Sakamoto, Noriho ; Nishioka, Yasuhiko ; Kishi, Kazuma ; Yanagihara, Toyoshi ; Okishio, Kyoichi ; Fukuizumi, Aya ; Nishikiori, Hirotaka ; Sato, Yuki ; Honda, Takayuki ; Kishaba, Tomoo ; Ishida, Yuriko ; Koyama, Junji ; Tsurumaki, Nozomu ; Yamaguchi, Kakuhiro ; Tamura, Kentaro ; Miyamoto, Atsushi ; Yamane, Mayuka ; Takata, Saori ; Kikuchi, Ryota ; Misumi, Toshihiro ; Matsumoto, Masaru ; Yatera, Kazuhiro

INTRODUCTION:

Non-small cell lung cancer (NSCLC) patients with comorbid interstitial pneumonia (IP) are at high risk for drug-induced pneumonitis, and previous reports suggest a lower frequency of common driver mutations such as EGFR. This may discourage genetic testing, potentially overlooking prevalent, targetable mutations like KRAS, BRAF, and MET. This study aimed to elucidate the real-world status of genetic testing, the frequency of oncogenic drivers, and the safety and efficacy of targeted therapies in patients with NSCLC and comorbid IP.

METHODS:

This multicenter, retrospective study analyzed 1256 patients with advanced or recurrent NSCLC and comorbid chronic fibrosing IP from 37 Japanese institutions (Registry number: UMIN000055609).

RESULTS:

The rate of any genetic testing was 59.2 % (95 % confidence interval [CI], 56.5-62.0), with multigene testing performed in only 41.0 % (95 %CI, 38.3-43.8). Among patients with NSCLC undergoing multigene testing (N = 515), the most frequent mutations were KRAS (4.7 %; G12C, 1.9 %), followed by EGFR (2.9 %), BRAF V600E (1.6 %), and MET exon 14 skipping (1.6 %). The incidence of drug-induced pneumonitis was 0 % (0/6) for sotorasib, 50 % (4/8) for osimertinib, 33 % (1/3) for alectinib, and 25 % (1/4) for both dabrafenib plus trametinib and tepotinib. Patients with actionable oncogenic drivers receiving targeted therapy had the longest overall survival, followed by those not receiving it, and then driver-negative/unknown patients (median: 39.2, 24.0, and 13.8 months, respectively).

CONCLUSIONS:

Multigene testing is underutilized in this population. While many targeted therapies carry a high risk of pneumonitis, sotorasib appeared relatively safe. Despite the risks, identifying and treating actionable oncogenic drivers may improve survival.

01 Feb 2026·ANTICANCER RESEARCH

Clinical Activity of MET-TKIs in METex14 Skipping NSCLC With Poor Performance Status.

Article

Author: Okuma, Yusuke ; Goto, Yasushi ; Horinouchi, Hidehito ; Shinno, Yuki ; Ohe, Yuichiro ; Yoshida, Tatsuya ; Yamaguchi, Yoh ; Higashiyama, Ryoko Inaba ; Yamamoto, Noboru ; Masuda, Ken

BACKGROUND/AIM:

The mesenchymal-epithelial transition (MET) receptor plays a key role in cell growth and survival. The MET exon 14 (METex14) skipping mutation occurs in 3% to 4% of patients with non-small cell lung cancer (NSCLC) and leads to prolonged MET signaling and oncogenesis. MET tyrosine kinase inhibitors (TKIs), such as tepotinib and capmatinib, are effective for METex14-altered NSCLC; however, their impact on patients with a poor performance status (PS) is unclear. We retrospectively analyzed clinical outcomes of MET-TKI treatment for NSCLC with the METex14 skipping mutation.

PATIENTS AND METHODS:

We reviewed 59 cases of NSCLC with the METex14 skipping mutation diagnosed at the National Cancer Center Hospital between June 2020 and April 2024. Clinical data included demographics, PS, histology, PD-L1 expression, treatment response, progression-free survival (PFS), and overall survival (OS).

RESULTS:

Forty-nine patients (median age, 72 years; range=50-87 years; 53.1% male) received MET-TKIs (tepotinib or capmatinib). Thirty-seven patients and 12 patients had PS scores of 0 or 1 and ≥2, respectively. The median PFS and median OS of patients who received MET-TKI treatment were 5.6 months and 18.7 months, respectively. Thirty-seven patients who received first-line MET-TKI treatment had median PFS, median OS, and a median overall response rate (ORR) of 5.6 months, 21.3 months, and 48.6%, respectively. For patients with a PS score ≥2 (n=9), the median PFS, median OS, and median ORR were 0.95 months, 1.3 months, and 11.1%, respectively. A PS score ≥2 was strongly associated with shorter OS. Two of nine (22.2%) patients with a poor PS experienced improvement.

CONCLUSION:

MET-TKIs are effective for NSCLC with the METex14 skipping mutation; however, their efficacy for patients with a poor PS is limited.

News (Medical) associated with Tepotinib Hydrochloride Hydrate

03 Sep 2025

·pharma.economictimes.indiatimes.com

GST waiver for 36 drugs; formulations under 5% slab

New Delhi: Executing the much-awaited overhaul of the Goods and Services Tax (GST) regime, the GST Council has brought a major relief for patients by reducing the indirect tax on medicines to 5 per cent, along with exempting as many as 36 life-saving medicines and other critical drugs. The GST council—a statutory body highest decision making body on indirect taxes led by the Union Finance Ministry at its 56th meeting in the national capital has recommended to reduce the GST on all drugs and medicines (finished formulations) from 12 per cent to 5 per cent under the new two-tier tax structure of 5 and 18 per cent slabs to be effective from September 22. Additionally the body has also recommended to exempt GST on 33 lifesaving drugs and on 3 other medicines used for treatment of cancer, rare diseases and other severe chronic diseases. Speaking at a press briefing after the council 10.5-hour long marathon meet, Finance Minister Nirmala Sitharaman said, “all recommendations have been cleared with zero reservations and have corrected various inverted duty structure problems, classification related issues and that this rationalization exercise will bring predictability and stability of GST.” “These reforms have been carried out with a focus on the common man, and after a rigorous evaluation process in most sectors including healthcare, the rates have come down drastically, she added. Previously, medicines in India were taxed at 5 per cent for life-saving and essential drugs, and at 12 per cent for others but following the announcement all medicines will attract a standard duty of 5 per cent with extensions for several medicines specified at the end of this article. Welcoming the move, Sudarshan Jain, Secretary General, IPA said, “the decision to exempt life-saving and cancer medicines from GST, is a step that will bring direct relief to patients and their families. and, the reduction in GST on a wide range of medicines from 12 per cent to 5 per cent will further help to ease the overall treatment burden and make essential therapies more affordable.” Meanwhile, for companies, the clarity on a 5 per cent slab and exemptions removes long-standing ambiguity, enabling transparent pricing and better market planning. The move will expand access in semi-urban and rural markets, ease litigation, and free up resources for innovation, said Manoj Mishra, Partner and Tax Controversy Management Leader, Grant Thornton Bharat LLP. Notably, on the issue of inverted duty involving APIs and key starting materials—which are currently taxed at 18 per cent against 12 or 5 per cent for finished formulations—further clarity is awaited from the industry. ETPharma earlier reported that, in a letter to the Finance Minister, the national chemist body, the All India Organisation of Chemists and Druggists (AIOCD) had urged, “to bring all medicines including vitamins, probiotics, nutritional, food supplements under the 5 per cent GST slab. The rate rationalization comes days after Prime Minister Narendra Modi had pitched for introducing next-gen reforms across sectors to “increase ease of living for the common man and strengthen the economy.” However, this rationalization brings a revenue shortfall challenge for governments with states likely to bear a greater share of the burden, as they receive over 40 percent of the inter-state inflows in addition to their own SGST collections. Responding to a media query at the media briefing Arvind Shrivastava, Revenue Secretary said that, based on the consumption of FY23-24 the ministry has estimated that the net revenue implication of this proposal will be around Rs 48,000 crore. “However the exercise will trigger buoyancy effects and will have a positive impact on consumer and compliance. And therefore we believe this proposal will be fiscally sustainable both for centers and the states,” Shrivastava noted. ' S.no. Drug Indication Brand name and (Company) 1 Onasemnogene abeparvovec SMA (One-time gene therapy) Zolgensma (Novartis) 2 Asciminib Blood Cancer Scemblix (Novartis) 3 Mepolizumab Asthma Nucala (GSK) 4 Pegylated Liposomal Irinotecan Pancreatic Cancer Onivyde (Ipsen) 5 Daratumumab Cancer Darzalex (J&J subsidiary) 6 Daratumumab subcutaneous Cancer Darzalex Faspro (J&J subsidiary) 7 Teclistamab Blood Cancer Tecvayli (J&J subsidiary) 8 Amivantamab Lung Cancer Rybrevant (J&J subsidiary) 9 Alectinib Lung Cancer Alecensa (Roche) 10 Risdiplam SMA Evrysdi (Roche) 11 Obinutuzumab Blood Cancer Gazyva (Roche) 12 Polatuzumab vedotin Blood Cancer Polivy (Roche) 13 Entrectinib Cancer Rozlytrek (Roche) 14 Atezolizumab Cancer (PD-L1 immunotherapy) Tecentriq (Roche) 15 Spesolimab GPP flares Spevigo (Boehringer Ingelheim) 16 Velaglucerase Alpha Gaucher Vpriv (Takeda) 17 Agalsidase Alfa Fabry disease Replagal (Takeda) 18 Rurioctocog Alpha Pegol Hemophilia Adynovate (Takeda) 19 Idursulphatase Type II Mucopolysaccharidosis Elaprase (Takeda) 20 Alglucosidase Alfa Pompe Myozyme (Sanofi) 21 Laronidase Type I Mucopolysaccharidosis Aldurazyme (Sanofi) 22 Olipudase Alfa ASMD Xenpozyme (Sanofi) 23 Tepotinib Lung Cancer Tepmetko (Maerck KGaA) 24 Avelumab Cancer (PDL-1 immunotherapy) Bavencio (Pfizer) 25 Emicizumab Hemophilia Hemlibra (Roche subsidiary) 26 Belumosudil cGVHD - 27 Miglustat Gaucher Zavesca (J&J subsidiary) 28 Velmanase Alfa Alpha-mannosidosis - 29 Alirocumab Cholesterol lowering drug (LDL-C) Praluent (Sanofi) 30 Evolocumab Cholesterol lowering drug (LDL-C) Repatha (Amgen) 31 Cystamine Bitartrate Cystagon - 32 CI-Inhibitor injection Hereditary Angioedema - 33 Inclisiran Cholesterol lowering drug (LDL-C) Leqvio (Novartis) 34 Agalsidase Beta Fabry disease Fabrazyme (Sanofi) 35 Imiglucerase Gaucher Cerezyme (Sanofi) 36 Eptacog alfa activated recombinant coagulation factor VIIa Hemophilia NovoSeven Note: Above is the list of medicines exempted from GST tax recommended by the 56th GST Council Meet/ Source: PIB By Abhijeet Singh ,

Gene Therapy

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

100 Deals associated with Tepotinib Hydrochloride Hydrate

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R&D Status

Approved

10 top approved records.

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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.

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic Colorectal Carcinoma	Phase 2	Italy	Merck Healthcare KGaA	24 Sep 2020
RAS/BRAF Wild Type Colorectal Cancer	Phase 2	Italy	Merck Healthcare KGaA	24 Sep 2020
Advanced Malignant Solid Neoplasm	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Breast Cancer	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Colorectal Cancer	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Head and Neck Neoplasms	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Hepatocellular Carcinoma	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Neoplasm Metastasis	Phase 2	South Korea	Merck KGaA	16 Jan 2020
Renal Cell Carcinoma	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


ESMO_ASIA2025	Not Applicable	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer MET exon 14 skipping mutations	55	Tepotinib	lvgeqzrggt(jdqadhaixj) = dbposzaxlb utdpffuooq (cllfikywkk ) View more	Positive	05 Dec 2025
				Tepotinib (1L)	lvgeqzrggt(jdqadhaixj) = gkiwsywpri utdpffuooq (cllfikywkk ) View more
ESMO_ASIA2025	Not Applicable	MET gene amplification Non-small Cell Lung Cancer MET gene copy number	16	Tepotinib	dcwomalopp(zuaxenglco) = iwuqgepkkh pfbttelssn (nkwgwsulzl, 2 - 26) View more	Positive	05 Dec 2025
				Tepotinib	dcwomalopp(zuaxenglco) = mhwztrwupt pfbttelssn (nkwgwsulzl, 3 - 24) View more
REAL-MET (ESMO2025)	Not Applicable	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer MET exon 14 skipping	62	Tepotinib (Brain Metastases)	mmviqilgbd(xfxifdtcsc) = hiaqtdmjld yufpctkioz (nbsxkyktnu ) View more	Positive	17 Oct 2025
				Tepotinib (No Brain Metastases)	vfflnhlfuk(roioeaxwhy) = ehsfsmpgsf oqcwrfvavh (lsxkvczzwc, 1.7 - 12.1) View more
VISION study (ASCO2025)	Not Applicable	MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer First line PD-L1	98	Tepotinib	qeahgeihpg(nvoejwanhe) = Grade 3 or higher edema occurring in 12.9% of the patients aifjxaggag (dvkvcbxxba )	Positive	30 May 2025
				Immune Checkpoint Inhibitors
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	ptjyntmrnl(cmiopdojtg) = 15.7% of pts discontinued treatment due to TRAEs lufhztblto (lqdkostrwn ) View more	Positive	26 Mar 2025
NCT03940703 (INSIGHT 2, Pubmed \| Lancet Oncol) Manual	Phase 2	Non-Small Cell Lung Cancer Second line EGFR Mutation \| MET Amplification	128	Tepotinib plus osimertinib (progression on first-line osimertinib)	rdgxyfnupb(ffzikesssk) = gvxzuxcrlu mvbudkcvew (iblvqoedio, 39.7 - 60.3) View more	Positive	25 Aug 2024
NCT03546608 (CTgov)	Phase 1	Hepatic Insufficiency	18	Tepotinib (Healthy Participants (Control))	hokeyflvyx(gejcbynvkg) = quyvsmvede naxukxsdhz (agmuerrhea, 13.4) View more	-	12 Aug 2024
				Tepotinib (Mild Hepatic Impairment (Child-Pugh Class A))	hokeyflvyx(gejcbynvkg) = umluntlppc naxukxsdhz (agmuerrhea, 63.9) View more
NCT03940703 (INSIGHT 2, CTgov)	Phase 2	Recurrent Non-Small Cell Lung Cancer	140	Tepotinib (Tepotinib Mono-therapy)	ngnvqgnpcu(cdnduxwfsf) = xtnvagqwmm chbszespij (cxevzflvip, czevwrmyje - phqdiblaef) View more	-	04 Jun 2024
				Tepotinib+Osimertinib (Tepotinib and Osimertinib)	ngnvqgnpcu(cdnduxwfsf) = hmoahoidiy chbszespij (cxevzflvip, couoqyyduo - clpwsoktkj) View more
NCT02864992 (VISION, ASCO2024) Manual	Phase 2	Non-Small Cell Lung Cancer \| MET Exon 14 Skipping Mutation Non-small Cell Lung Cancer MET Exon 14 Skipping	248	tepotinib (Brain metastases)	rqumqrpkgz(mwdvllncyz) = ztkwwgtslc hqxcvxollq (bxpbhuerxb, 2.41) View more	Positive	24 May 2024
				tepotinib (Liver metastases)	rqumqrpkgz(mwdvllncyz) = kcrglxnvde hqxcvxollq (bxpbhuerxb, 2.27) View more
NCT04647838 (KCSG AL19-17, ASCO2024)	Phase 2	Hepatocellular Carcinoma \| Solid tumor \| Neoplasm Metastasis ... ctDNA \| METex14 \| METamplification ... View more	35	Tepotinib	hkwevbsqok(ydzwnzavtj) = hbjkjvliug afxjegtrdz (lwyclkkmlf ) View more	Positive	24 May 2024
				Placebo	hkwevbsqok(ydzwnzavtj) = hnjdnpuvbb afxjegtrdz (lwyclkkmlf ) View more

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