Tepotinib

Описание

Tepotinib is a highly selective inhibitor against MET. In xenograft models, acquired resistance to EGFR TKIs via secondary EGFR T790 M mutations can be overcome with tepotinib treatment.

Использование

EMD 1214063 is a novel ATP-comptetitive inhibitor of the MET hepatocyte growth factor receptor and a novel kinase inhibitor and a therapeutic agent for neuroblastoma. Potent c-MET inhibitor.

Имя бренда

Tepmetko

Механизм действия

Tepotinib is a Kinase Inhibitor. The mechanism of action of tepotinib is as a Mesenchymal Epithelial Transition Inhibitor, and P-Glycoprotein Inhibitor.

Клиническое использование

Tepotinib is currently being evaluated in combination with EGFR TKI gefitinib and also a separate trial in NSCLC patients with MET exon 14 skipping mutation and MET amplification.

взаимодействия лекарств

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.

Метаболизм

Tepotinib is metabolized primarily by CYP3A4 and CYP2C8, with some apparent contribution by unspecified UGT enzymes. The metabolite M506 is the major circulating metabolite, comprising approximately 40.4% of observed drug material in plasma, while the M668 glucuronide metabolite has been observed in plasma at much lower quantities (~4% of an orally administered dose). A total of 10 phase I and phase II metabolites have been detected following tepotinib administration, most of which are excreted in the feces.