NCIt definition : An orally available inhibitor of specific mutant forms of the mitochondrial enzyme
isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon
administration, enasidenib specifically inhibits various mutant forms of IDH2, including
the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate
(2HG). This may lead to both an induction of cellular differentiation and an inhibition
of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric
acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth
by blocking differentiation and the production of the oncometabolite 2HG.;