Chemical formula: C₁₉H₁₇F₆N₇O Molecular mass: 473.383 g/mol PubChem compound: 89683805
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.
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 | |
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 |
Enasidenib is an active ingredient of these brands:
United States (US)
Canada (CA)
Note the following: The list of brand names is continuously updated, and thus does not include the total of products circulating worldwide. |
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