Structural formula of Tepotinib

Tepotinib is a kinase inhibitor provided as a film-coated tablet containing 225 mg of tepotinib (equivalent to 250 mg of tepotinib hydrochloride hydrate) and its chemical name is 3-{1-[(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}phenyl)methyl]-6-oxo-1,6-dihydropyridazin-3-yl}benzonitrile hydrochloride hydrate, common specifications are225mg*30 tablets.

Tepotinib is synthetically designed to targetc-MET, thereby inhibiting downstream signaling pathways. It binds to c-MET in a U-shaped geometry with hinge and activation loop residue Y1230 to prevent ATP binding. Therefore tepotinib is a new drug that targets and selectively binds MET, disrupting oncogenic signals and promoting tumor cell death. The U.S. Food and Drug Administration (FDA) has granted Breakthrough Therapy Designation to tepotinib for the treatment of patients with metastatic non-small cell lung cancer with METex14 skipping mutations who have progressed on platinum-based chemotherapy. Obtained accelerated approval for this indication in February 2021

The original drug Tepotinib is already on the market in China, but it is not yet eligible for medical insurance. Tepotinib Original drug currently marketed overseas is relatively expensive, and the price of each box of 225mg*30 tablets may be around RMB 80,000 (the price may fluctuate due to exchange rates). There are already generic Tepotinib drugs produced in other countries. The ingredients of these generic drugs are basically the same as those of the original drug, but the price is relatively cheap. For example, the price of 225mg*60 tablets produced by a Laos pharmaceutical factory may be more than 8,000 yuan per box (the price may fluctuate due to exchange rates).