Will there be resistance to Ripretinib?

Ripretinib is the first and only switch-controlled kinase inhibitor that provides broad-spectrum inhibition of KIT and PDGFRα kinase signaling in vitro through a novel dual mechanism of action. Advanced gastrointestinal stromal tumor (GIST) is a highly complex disease with numerous mutations that contribute to drug resistance and progression. Gastrointestinal stromal tumors are often driven by primary activating mutations in kinase genes that maintain the kinase in an active state, leading to uncontrolled cell proliferation and/or cell survival.

Advanced gastrointestinal stromal tumors are marked by the development of secondary drug-resistant mutations, which play a key role in disease progression, and a single patient with gastrointestinal stromal tumors may have multiple mutations within or between tumors. With the emergence of secondary resistance mutations, some TKIs may lose their ability to prevent kinase activation, leading to cancer cell proliferation. Study data showed that compared with placebo, progression-free survival (PFS) was significantly improved in patients treated with repetitinib (6.3 months vs. 1.0 months; P<0.0001), and 66% of treated patients had stable disease, compared with 20% of patients in the placebo group.

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.