oral MET kinase inhibitor
approved for clinical use in NSCLC
internal HTS and SBDD
Clinical Cancer Research
Merck KGaA
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…