FLX925

FLX925 is a rationally designed, orally administered small-molecule inhibitor that targets both FMS-like tyrosine kinase 3 (FLT3) and cyclin-dependent kinases 4 and 6 (CDK4/6). It was developed to overcome resistance mechanisms associated with earlier FLT3 inhibitors, particularly in acute myeloid leukemia (AML) patients with FLT3-ITD mutations. By inhibiting both FLT3—including clinically relevant secondary resistance mutations—and CDK4/6, which are central to cell cycle progression via retinoblastoma protein phosphorylation, FLX925 aims to reduce the emergence of resistant cancer clones. Its dual-inhibitor profile may also extend its therapeutic potential beyond AML to other malignancies dependent on these pathways. The drug has been evaluated in phase 1 clinical trials for relapsed or refractory AML[1][2][3][5][6].