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 eciphera's kinase switch inhibitors target the mechanisms that render kinases oncogenic, retain potency against gatekeeper mutations, and afford selectivity profiles not easily attained by other approaches. |
Deciphera's KIT ProgramGastrointestinal Stromal Tumor (GIST) program DP-3407/DP-3429 preclinical development Treatment of primary and refractory GIST • inhibitor of primary mutant cKIT kinase • inhibitor of major secondary mutant forms: V654A/D816V/D816H/T670I • inhibitor of PDGFR-alpha and KDR kinases DP-3407 and DP-3429 inhibit the primary mutant form of cKIT kinase ( D JMD-KIT) causative of gastrointestinal stromal tumors (GIST) in 90% of newly diagnosed patients. Importantly, DP-3407 and DP-3429 also inhibit major secondary mutant forms of D JMD-KIT, wherein patients present with additional mutations: V654A, D816V, D816H, or the gatekeeper mutant T670I. Greater than 50% of patients on therapy for GIST develop resistance to currently marketed drugs due to the emergence of these secondary mutations. DP-3407 and DP-3429 are being developed to provide patients with superior coverage of all of these mutant forms of cKIT responsible for both primary and refractory GIST. DP-3407 and DP-3429 have demonstrated potent in vivo inhibition of KIT in animal models, and are being developed as oral treatments for GIST. |
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