inlexisertib + ripretinib

This drug is a **combination therapy** consisting of inlexisertib (DCC-3116), a selective inhibitor of ULK1/2, and ripretinib, a tyrosine kinase inhibitor targeting KIT and PDGFRA. Inlexisertib inhibits autophagy initiation by blocking ULK1/2 and thereby decreases phosphorylation of autophagy-related proteins such as ATG13. Ripretinib broadly inhibits KIT and PDGFRA kinase activity, including primary and secondary drug-resistant mutants, blocking aberrant cell signaling that drives tumor proliferation and survival in gastrointestinal stromal tumors (GIST). The combination is being developed for the treatment of advanced gastrointestinal stromal tumor (GIST), particularly as a second-line therapy for patients who have progressed on or are intolerant to first-line imatinib. The rational for the combination is to address both mutant kinase signaling (via ripretinib) and cancer cell adaptive resistance via autophagy (via inlexisertib)[1][3][9]. Developer: Deciphera Pharmaceuticals (inlexisertib), with trials listing Ono Pharma, and ripretinib originally developed by Deciphera Pharmaceuticals.

Brand names

QINLOCK

Other names

DCC-3116 + ripretinib