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molecules of the month

tepotinib

oral MET kinase inhibitor

approved for clinical use in NSCLC

internal HTS and SBDD

Clinical Cancer Research

Merck KGaA

Chemical structure of molecule Tepotinib (Merck KGaA MET kinase inhibitor)
1 min read

9.      The Merck KGaA MET kinase inhibitor, tepotinib, was approved earlier this year for METex14 positive NSCLC patients, and is administered once-daily in contrast to capmatinib, which was approved in 2020. Both molecules were approved based on small numbers of patients (tepotinib pivotal trial: NCT02864992) due to the significance of the response in trials. MET is a great case study for small molecules being approved before large molecules for a surface receptor – anti-MET antibodies were expected to lead in this area and were initially thought to be more clinically advanced. MET antibodies surprisingly failed to demonstrate efficacy in later trials, which may be due to a number of factors including the fact that antibodies can in certain cases be agonists for their…


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