K03861

AUZ454 is a potent and selective Type II FLT3 inhibitor. AUZ454 is able to override drug resistance that less potent "type I" inhibitors and "type II" first-generation FLT3 inhibitors cannot. Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage clinical trials. However, the identification of PKC412-resistant leukemic blast cells in the bone marrow of AML patients has propelled the development of novel and structurally distinct FLT3 inhibitors that have the potential to override drug resistance and more efficiently prevent disease progression or recurrence.