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Tepotinib

Generic Name
Tepotinib
Brand Names
Tepmetko
Drug Type
Small Molecule
Chemical Formula
C29H28N6O2
CAS Number
1100598-32-0
Unique Ingredient Identifier
1IJV77EI07
Background

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
Clinical Trials
Related News

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

• The FDA has approved FoundationOne Liquid CDx as a companion diagnostic to identify metastatic non-small cell lung cancer (mNSCLC) patients with _MET_ exon 14 skipping alterations. • This approval expands access to precision medicine, enabling clinicians to identify patients who may benefit from treatment with tepotinib (Tepmetko), a targeted MET inhibitor. • The approval is based on data from the phase 2 VISION trial, which demonstrated improved responses with tepotinib in patients with _MET_ exon 14 skipping NSCLC. • FoundationOne Liquid CDx analyzes over 300 cancer-related genes using blood samples, offering a non-invasive option for biomarker testing in advanced NSCLC.

FDA Approves Companion Diagnostic for Tepotinib in mNSCLC with MET Exon 14 Skipping Alterations

• The FDA approved FoundationOne Liquid CDx as a companion diagnostic for tepotinib, aiding in identifying mNSCLC patients with MET exon 14 skipping alterations. • Tepotinib received regular approval in February 2024 for mNSCLC patients with MET exon 14 skipping alterations, following an earlier accelerated approval in 2021. • Phase 2 VISION trial data supported tepotinib's approval, demonstrating overall response rates of 57% in treatment-naive and 45% in previously treated patients.

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