Olutasidenib CAS# 1887014-12-1 5-[1-(6-氯-2-氧-1H-喹啉-3-基)乙基胺]-1-甲基-6-氧硫苷-2-碳腈

Olutasidenib (FT-2102) is a potent, selective oral inhibitor of mutant isocitrate dehydrogenase 1 (IDH1). In preclinical studies, it inhibited mutant IDH1 (R132H/C) enzyme activity with an IC50 of ~10 nM, blocking the abnormal production of the oncometabolite 2-hydroxyglutarate (2-HG) in cancer cells. Treatment of IDH1-mutant leukemia and glioma cell lines reduced 2-HG levels by >90%, promoted cellular differentiation, and inhibited proliferation. In IDH1-mutant xenograft mouse models, olutasidenib reduced intratumoral 2-HG concentrations and induced tumor growth inhibition. Pharmacokinetic studies demonstrated good oral bioavailability and sustained target engagement, supporting its advancement into clinical trials for IDH1-mutant malignancies.