Ripretinib’s mechanism of action

Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet-derived growth factor receptor A (PDGFRA) kinase, including wild-type, primary and secondary mutations. Repetinibalso inhibits other kinases in vitro, such asPDGFRB, TIE2, VEGFR2 and BRAF.

Ripetinib binds to KIT and PDGFRA receptors through mutations in exons 9, 11, 13, 14, 17, and 18 (for KIT mutations) and exons 12, 14, and 18 (for PDGFRA mutations). The "switch pocket" of protein kinases is often combined with the activation loop and acts as a "switch" for the kinase. Repetinib has a unique dual mechanism of action, binding to the kinase switch pocket and activation loop, thereby shutting down the kinase and its ability to cause dysregulation of cell growth.

The original drug of Ripetinib has been marketed in China and has been approved by the National Medical Insurance Bureau to enter the scope of Class B medical insurance, but it is limited to patients who meet the indications. The price of each box of 50mg*30 tablets may be around 30,000 yuan. The expensive price may increase the pressure on families with heavy financial burdens. The US version of Ripetinib Specifications50mg*90 tablets sold overseas may be priced around RMB 77,000 per box (the price may fluctuate due to exchange rates). The ingredients of foreign original drugs are basically the same as those of domestic original drugs. Currently, there is no generic drug of Ripetinib produced and marketed overseas. For specific prices and drug information, please consult Yaode’s medical consultant.