1887014-12-1

Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1][2].

Olutasidenib specifically inhibits the mutant IDH1 enzyme, which reduces the accumulation of abnormal metabolites and promotes normal differentiation and maturation of cells. This targeted treatment approach aims to reduce tumor burden and improve patient outcomes.

IDH1

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[1] JM Watts, et al. A phase 1 dose escalation study of the IDH1m inhibitor, FT-2102, in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
[2] Justin A. Caravella, et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J Med Chem. 2020.