Ripretinib (DCC-2618) was designed to inhibit the full spectrum of mutant KIT 
and PDGFRA kinases found in cancers and myeloproliferative neoplasms, 
particularly in gastrointestinal stromal tumors (GISTs), in which the 
heterogeneity of drug-resistant KIT mutations is a major challenge. Ripretinib 
is a "switch-control" kinase inhibitor that forces the activation loop (or 
activation "switch") into an inactive conformation. Ripretinib inhibits all 
tested KIT and PDGFRA mutants, and notably is a type II kinase inhibitor 
demonstrated to broadly inhibit activation loop mutations in KIT and PDGFRA, 
previously thought only achievable with type I inhibitors. Ripretinib shows 
efficacy in preclinical cancer models, and preliminary clinical data provide 
proof-of-concept that ripretinib inhibits a wide range of KIT mutants in 
patients with drug-resistant GISTs.