olutasidenib

Olutasidenib is a small-molecule, orally administered, highly selective inhibitor of mutated isocitrate dehydrogenase 1 (IDH1), specifically targeting IDH1-R132 variants found in acute myeloid leukemia (AML). It acts as an allosteric inhibitor by binding to a hydrophobic pocket near the IDH1 heterodimer interface, stabilizing the mutant enzyme in its inactive conformation and preventing the production of the oncometabolite 2-hydroxyglutarate (2-HG). This reduction in 2-HG levels reverses epigenetic dysregulation and promotes differentiation of leukemic cells. Olutasidenib is indicated for adult patients with relapsed or refractory AML harboring susceptible IDH1 mutations. The drug was developed by Forma Therapeutics and is marketed under the brand name Rezlidhia[4][5][8].

Brand names

Rezlidhia

Other names

olutasidenib