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tepotinib

Development stage: Approved
Lead developer: Merck
Modality: Small Molecules
Administration: Oral

Overview

Tepotinib is an oral, highly selective type 1b mesenchymal–epithelial transition (MET) tyrosine kinase inhibitor developed for the treatment of metastatic non-small cell lung cancer (NSCLC) in patients whose tumors harbor MET exon 14 skipping alterations. By inhibiting MET phosphorylation, tepotinib blocks downstream signaling pathways involved in tumor cell proliferation, survival, angiogenesis, and metastasis. It is approved for use in several countries and was the first oral MET-targeted TKI to allow once-daily dosing. Tepotinib also exhibits off-target inhibition of melatonin receptor 2 and imidazoline receptor 1[4][5][7].

Brand names: Tepmetko
Other names: tepotinib hydrochloride hydrate

Targets

MET (Mesenchymal-epithelial transition factor receptor)

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