(R,S)-Ivosidenib (AG-120)

Description: 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) that is being developed by Agios Pharmaceuticals for the treatment of cancer in patients with IDH1 mutations. The mutated form of the IDH1 enzyme produces a metabolite, 2-hydroxyglutarate (2-HG), which is thought to play a role in the formation and progression of acute myeloid leukaemia (AML), gliomas and other cancers. Elevated 2-HG levels interfere with cellular metabolism and epigenetic regulation, thereby contributing to oncogenesis. Ivosidenib targets the IDH1 metabolic pathway to prevent a build-up of the oncometabolite 2-HG. On 7/20/2018, FDA approved Ivosidenib to treat patients with relapsed or refractory acute myeloid leukemia.

References: N Engl J Med. 2018 Sep 20; 379(12):1186; Drugs. 2018 Sep; 78(14):1509-1516; ACS Med Chem Lett. 2018 Jan 19; 9(4):300-305.

Related CAS#: 1448347-49-6 (Ivosidenib)