Olutasidenib (FT-2102)

An inhibitor of mutant IDH1

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Background

Olutasidenib is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC₅₀s = 0.021 and 0.114 ?M for IDH1^R132H and IDH1^R132C, respectively).¹ It is selective for mutant IDH1 over wild-type IDH1 and mutant IDH2 (IC₅₀s = 22.4, 27.3, and >100 μM for wild-type IDH1, IDH2^R172K, and IDH2^R140Q, respectively). Olutasidenib inhibits production of ɑ-hydroxyglutaric acid in U87 cells expressing mutant IDH1^R132H, IDH1^R132C, IDH1^R132L, IDH1^R132G, and IDH1^R132S with IC₅₀ values of 0.009, 0.039, 0.042, 0.006, and 0.009 ?M, respectively. It reduces intratumor 2-HG levels in HCT116-IDH1^R132H and HCT116-IDH1^R132C mouse xenograft models when administered at doses of 12.5, 25, and 50 mg/kg.

1.Caravella, J.A., Lin, J., Diebold, R.B., et al.Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitorJ. Med. Chem.63(4)1612-1623(2020)