enasidenib

Enasidenib is a small molecule inhibitor of the mitochondrial enzyme isocitrate dehydrogenase 2 (IDH2). It selectively targets mutant forms of IDH2 (notably R140Q, R172S, and R172K), which are found in a subset of patients with acute myeloid leukemia (AML). Mutant IDH2 catalyzes the reduction of α-ketoglutarate to the oncometabolite 2-hydroxyglutarate (2-HG), leading to DNA and histone hypermethylation, altered gene expression, and impaired differentiation of hematopoietic cells. By inhibiting mutant IDH2, enasidenib reduces 2-HG levels and promotes differentiation and maturation of myeloid cells. It is FDA-approved for adults with relapsed or refractory AML harboring an IDH2 mutation as detected by an FDA-approved test[1][4][6][10].

Brand names

Idhifa

Other names

enasidenib mesylate