FF-10101

FF-10101 is a **first-in-class, irreversible, and covalent FMS-like tyrosine kinase 3 (FLT3) inhibitor** developed primarily for the treatment of **acute myeloid leukemia (AML)** with FLT3 mutations. Its design allows covalent binding to a cysteine residue at position 695 in the FLT3 protein, rendering potent and highly selective inhibition. Unlike earlier FLT3 inhibitors, FF-10101 is highly active against a spectrum of FLT3 mutations, including **FLT3-ITD, D835, F691**, and non-canonical activating mutations, even when resistant to other FLT3 inhibitors like quizartinib or gilteritinib[1][2][3][5]. It also demonstrates activity in relapsed/refractory AML settings with and without prior FLT3 inhibitor exposure. FF-10101 is administered orally and is currently in clinical development with phase 1 trials completed in relapsed/refractory AML. The recommended phase 2 dose is 75 mg twice daily[2][1].

Brand names

FF-10101FF10101FF 10101

Other names

FLT3-IN-1FLT-3-IN-1FLT 3-IN-1(S,E)-N-(1-((5-(2-((4-Cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide(E)-N-((2R)-1-(5-(2-(4-cyanoanilino)-4-(propylamino)pyrimidin-5-yl)pent-4-ynylamino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide