DS-1001B is a potent and selective mutant IDH1 (Isocitrate Dehydrogenase-1) inhibitor with antitumor activity, ameliorating aberrant histone modifications and impairing tumor activity in chondrosarcoma.

Enasidenib mesylate (formerly known as AG-221; CC-90007; AG221; CC90007; trade name Idhifa), the mesylate salt of enasidenib, is a first-in-class, oral, potent and selective IDH2 (Isocitrate dehydrogenase 2) inhibitor approved in 2017 for the treatment of relapsed or refractory acute myeloid leukemia in people with specific mutations of the IDH2 gene, determined by an FDA-approved […]

Mutant IDH1-IN-1 is a novel, potent and mutant-selective IDH1 (isocitrate dehydrogenase 1) inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

Ivosidenib (formerly known as AG-120 or RG-120; trade name: Tibsovo®) is a novel, small molecule, orally bioavailable inhibitor of mutated cytosolic isocitrate dehydrogenase 1 (IDH1) developed by Agios Pharmaceuticals and has been approved for the treatment of cancer in patients with IDH1 mutations.

GSK864 is a novel, potent and selective isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.