How tepotinib works

Tepotinib is a methionine-specific kinase inhibitor that includes exon 14-skipped variants—it inhibits methionine phosphorylation and subsequent downstream signaling pathways to inhibit tumor cell proliferation, anchorage-independent growth, and methionine-dependent tumor cell migration. Tepotinib was also observed to downregulate the expression of epithelial-to-mesenchymal transition (EMT) promoting genes (such as MMP7, COX-2, WNT1, MUC5B and c-MYC) and upregulate the expression of EMT suppressing genes (such as MUC5AC, MUC6) at clinically relevant concentrations.

Mesenchymal-Epithelial transition factor (MET) is a receptor tyrosine kinase that is found to be overexpressed and/or mutated in multiple tumor types, thus making it an ideal target in therapy. MET plays a crucial role in the proliferation, survival, invasion and mobilization of tumor cells, and abnormal activation of MET is believed to lead to the development of more aggressive cancers with worse prognosis. Suppression of melatonin1B and nisalin may also occur at clinically relevant concentrations, although the relevance of this activity to tepotinib's mechanism of action is unclear.

The original drug Tepotinib is a new type of drug that has not yet been marketed in China, so it has not been included in the medical insurance. Domestic patients cannot yet purchase this drug in pharmacies or hospitals. The price of Tepotinib's original drug specification 225mg*30 tablets per box is around RMB 80,000 per box (the price may fluctuate due to exchange rate effects). It has been on the market for a short time and is expensive. There are also generic Tepotinib drugs produced in other countries. The price of a box of 225mg*60 tablets produced by a Lao pharmaceutical factory is around RMB 8,600 (the price may fluctuate due to the exchange rate). The ingredients of generic drugs produced abroad are basically the same as those of the original drug. For specific prices and drug details, please consult Yaode’s medical consultant.