TAK-901

TAK-901 is an investigational, multitargeted Aurora B kinase inhibitor with potential antineoplastic activity. TAK-901 potently inhibited only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2. TAK-901 inhibited cell proliferation with effective concentration values from 40 to 500 nmol/L in various human cancer cell lines. TAK-901 suppressed cellular histone H3 phosphorylation and induced polyploidy. TAK-901 displayed potent activity against several leukemia models. In rodent xenografts, TAK-901 exhibited potent activity against multiple human solid tumor types, and complete regression was observed in the ovarian cancer A2780 model. In vivo studies showed that TAK-901 induced pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue. TAK-901 is currently in a phase I clinical trials in patients within a diverse range of cancers.