Enasidenib

Chemical formula: C₁₉H₁₇F₆N₇O  Molecular mass: 473.383 g/mol  PubChem compound: 89683805

Active ingredient description

Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC code Group title Classification
L01XX59 L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01X Other antineoplastic agents → L01XX Other antineoplastic agents
Discover more medicines within L01XX59

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Title Information Source Document Type  
IDHIFA Film-coated tablet FDA, National Drug Code (US) MPI, US: SPL/PLR

Structural formula

Graphic representation of the active ingredient's molecular structure

External identifiers

CAS Substance: 1446502-11-9
DrugBank Drug: DB13874
PubChem Compound: 89683805
RxNorm Ingredient: 1940332
SNOMED-CT Concept: 763038001
Enasidenib (substance)
UNII Identifier: 3T1SS4E7AG
ENASIDENIB

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