Overview

Tepotinib is a MET tyrosine kinase inhibitor intended to treat a variety of MET-overexpressing solid tumors. It was originally developed in partnership between EMD Serono and the University of Texas M.D. Anderson Cancer Center in 2009 and has since been investigated in the treatment of neuroblastoma, gastric cancers, non-small cell lung cancer, and hepatocellular carcinoma. MET is a desirable target in the treatment of certain solid tumors as it appears to play a critical role, both directly and indirectly, in the growth and proliferation of tumors in which it is overexpressed and/or mutated. Tepotinib was first approved in Japan in March 2020 for the treatment of non-small cell lung cancers (NSCLC) with MET alterations, and was subsequently granted accelerated approval by the US FDA in February 2021, under the brand name Tepmetko, for the treatment of adult patients with metastatic NSCLC and MET exon 14 skipping alterations. It is the first oral MET-targeted tyrosine kinase inhibitor to allow for once-daily dosing, an advantage that may aid in easing the pill burden often associated with chemotherapeutic regimens. In February 2022, tepotinib was approved for use in Europe.

Indication

Tepotinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) who have mesenchymal-epithelial transition (MET) exon 14 skipping alterations.

Associated Conditions

Metastatic Non-Small Cell Lung Cancer

Research Report

Published: Aug 25, 2025

A Comprehensive Monograph on Tepotinib (TEPMETKO®): A Selective MET Tyrosine Kinase Inhibitor for METex14 Skipping Non-Small Cell Lung Cancer

I. Executive Summary

Tepotinib, marketed under the brand name TEPMETKO®, is an orally administered, highly selective, and potent small molecule inhibitor of the Mesenchymal-Epithelial Transition (MET) receptor tyrosine kinase.[1] It represents a significant advancement in precision oncology, specifically developed for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors harbor

MET gene alterations leading to exon 14 (METex14) skipping.[3] This genetic alteration, found in approximately 3-4% of NSCLC cases, is a key oncogenic driver associated with an aggressive disease course and poor prognosis, particularly in the typically older patient population it affects.[5]

The clinical development of tepotinib was anchored by the pivotal Phase II VISION trial (NCT02864992), a large, single-arm, biomarker-driven study that prospectively enrolled patients based on the presence of METex14 skipping alterations.[7] The trial demonstrated robust, consistent, and remarkably durable clinical efficacy. In treatment-naïve patients, tepotinib achieved an overall response rate (ORR) of 57% with a median duration of response (DOR) of 46.4 months. In previously treated patients, the ORR was 45% with a median DOR of 12.6 months.[7] This profound and lasting activity has fundamentally altered the treatment paradigm for this molecular subtype of NSCLC, shifting the goal from short-term palliation to long-term disease management.

Continue reading the full research report

Clinical Trials

Title	Posted	Study ID	Phase	Status	Sponsor
Tepotinib vs Standard Treatment in Patients With Advanced MET Exon 14 Mutated Non-Small Cell Lung Cancer Previously Treated	2025/04/03	NCT06908993	Phase 3	Not yet recruiting	Intergroupe Francophone de Cancerologie Thoracique
Lazertinib & Tepotinib for EGFR Mutant NSCLC in MET Overexpressed or Amplified Who Progressed After Lazertinib Treatment	2023/10/30	NCT06106802	Phase 2	Not yet recruiting	Samsung Medical Center
PhI/II Study of Amivantamab and Tepotinib Combo in MET-altered Non-small Cell Lung Cancer	2023/10/16	NCT06083857	Phase 1	Active, not recruiting	M.D. Anderson Cancer Center
Targeted Treatment for Advanced Non-Small Cell Lung Cancer That Has a MET Exon 14 Skipping Gene Change (An Expanded Lung-MAP Treatment Trial)	2023/09/11	NCT06031688	Phase 2	Recruiting	SWOG Cancer Research Network
POTENT - Tepotinib in Combination With Pembrolizumab in NSCLC	2023/03/23	NCT05782361	Phase 1	Recruiting	Institute of Cancer Research, United Kingdom
Tepotinib Plus Paclitaxel in MET Amplified or MET Exon 14 Alterated Gastric and GEJ Carcinoma	2022/06/30	NCT05439993	Phase 1	Recruiting	Hallym University Medical Center
Tepotinib Drug-Drug Interaction Study With Carbamazepine in Healthy Participants	2022/01/28	NCT05213481	Phase 1	Completed	Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany
Tepotinib Drug-Drug Interaction Study With Itraconazole in Healthy Participants	2022/01/24	NCT05203822	Phase 1	Completed	Merck Healthcare KGaA, Darmstadt, Germany, an affiliate of Merck KGaA, Darmstadt, Germany
The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs	2021/12/16	NCT05159245	Phase 2	Recruiting	Helsinki University Central Hospital
A Phase 1a/1b Study to Determine the Recommended Phase 2 Dose, of Tepotinib in Participants With MET Alterations and Brain Tumors	2021/11/16	NCT05120960	Phase 1	Withdrawn	M.D. Anderson Cancer Center

FDA Drug Approvals

Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
TEPMETKO	EMD Serono, Inc.	44087-5000	ORAL	225 mg in 1 1	2/23/2024

EMA Drug Approvals

Approved Product	Authorization Holder	Status	Issued Date
Tepmetko	Merck Europe B.V.,Gustav Mahlerplein 102,1082 MA Amsterdam,The Netherlands	Authorised	2/16/2022

HSA Drug Approvals

Approved Product	Manufacturer	Approval Number	Dosage Form	Strength	Approval Date
TEPMETKO FILM-COATED TABLET 225MG	Merck Healthcare KGaA	SIN16386P	TABLET, FILM COATED	225mg	11/25/2021

NMPA Drug Approvals

Approved Product	Company	Approval Number	Drug Type	Dosage Form	Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product	Registration No.	Company	Licence No.	Strength	Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product	ARTG ID	Sponsor	Registration Type	Status	Registration Date
TEPMETKO tepotinib 225 mg (as hydrochloride monohydrate) tablet blister pack	370977	Merck Healthcare Pty Ltd	Medicine	A	1/17/2022

Health Canada Drug Approvals

Approved Product	Company	DIN	Dosage Form	Strength	Market Date
No Health Canada approvals found for this drug.

CIMA AEMPS Drug Approvals

Approved Product	Company	Registration Number	Pharmaceutical Form	Prescription Type	Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product	Company	License Number	Dosage Form	Strength	Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product	Company	Registration Number	Dosage Form	Strength	Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.

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FDA Approves FoundationOne Liquid CDx as Companion Diagnostic for Tepotinib in METex14-Skipping NSCLC