Ripretinib is a kinase inhibitor primarily used to treat advanced gastrointestinal stromal tumor (GIST) that has not responded well to other kinase inhibitors like sunitinib and imatinib. Marketed under the name Qinlock, this medication is manufactured by Deciphera Pharmaceuticals and received FDA approval on May 15, 2020. It is notable for being the first drug approved as a fourth-line therapy, specifically for patients who have previously undergone treatment with at least three other kinase inhibitors, including imatinib. Ripretinib's mechanism of action involves inhibiting protein kinases, including both wild type and mutant forms of platelet-derived growth factor receptor A (PDGFRA) and KIT, which are implicated in the majority of gastrointestinal stromal tumors (GIST). This medication has been shown to inhibit other genes like PDGFRB, BRAF, VEGF, and TIE2 in laboratory studies. Its unique dual mechanism involves binding to the kinase switch pocket as well as the activation loop, effectively turning off the kinase and halting its ability to promote uncontrolled cell growth.

Ripretinib Pathway References