From the NCI Drug Dictionary: An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) with a mutation at arginine (R) 132, IDH1(R132), with potential antineoplastic activity. Upon administration, olutasidenib specifically inhibits IDH1(R132), thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH(R132).
Diseases for which it is established
History of changes in FDA indication
- 2022-12-01: Granted approval for adult patients with relapsed or refractory acute myeloid leukemia (AML) with a susceptible IDH1 mutation. (Based on 2102-HEM-101)
Also known as
- Code name: FT-2102
- Brand name: Rezlidhia