ITRI-260

ITRI-260 is a small molecule kinase inhibitor belonging to the azaazulenone class, developed by the Industrial Technology Research Institute (ITRI) in Taiwan. It acts as a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3), particularly targeting the internal tandem duplication (FLT3-ITD) mutation, as well as the c-Kit receptor tyrosine kinase. Preclinical studies demonstrated that ITRI-260 effectively inhibits the growth and phosphorylation of FLT3-ITD-mutated acute myeloid leukemia (AML) cells. In animal models, the compound showed favorable oral bioavailability and induced complete tumor regression in AML xenografts, including those resistant to other kinase inhibitors like sunitinib and sorafenib. Its safety profile is characterized by a lower potential for cardiotoxicity compared to earlier FLT3 inhibitors, as indicated by reduced hERG channel inhibition in patch-clamp assays.