The mechanism of action of Ripretinib on stromal tumors

Ripretinib (Ripretinib) is a novel switch-controlled KIT that inhibits many of the most common primary and secondary activated KIT and platelet-derived growth factor receptor A (PDGFRA) kinase mutants involved in GIST progression through a dual mechanism of action, including wild-type, primary and secondary mutations. Ripetinib also inhibits other kinases such as PDGFRB, TIE2, VEGFR2 and BRAF in vitro. The "switch pocket" of protein kinases is often combined with the activation loop and acts as a "switch" for the kinase. Ripetinib has a unique dual mechanism of action by binding to the kinase switch pocket and activation loop, thereby shutting down the kinase and its ability to cause dysregulation of cell growth.