MLchartDataset catalogue

Enasidenib mesylate

Term · Oncology and biomedicine · MLC-T-ONC-002786

  1. A drug used to treat adults with acute myeloid leukemia that has come back or has not gotten better with other treatment. It is used in patients whose cancer has a mutation (change) in the IDH2 gene. It is also being studied in the treatment of other types of cancer. Enasidenib mesylate blocks the protein made by the mutated IDH2 gene. Blocking this protein may help keep cancer cells from growing. Enasidenib mesylate is a type of enzyme inhibitor. Also called Idhifa.

  2. The mesylate salt form of enasidenib, 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.

Table 1. Record
IdentifierMLC-T-ONC-002786
FieldOncology and biomedicine
SynonymsIdhifa; enasidenib methanesulfonate; AG-221 mesylate
ReferencesNCI Dictionary of Cancer Terms; National Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-002786",
  "term": "Enasidenib mesylate",
  "field": "Oncology and biomedicine",
  "definitions": [
    "A drug used to treat adults with acute myeloid leukemia that has come back or has not gotten better with other treatment. It is used in patients whose cancer has a mutation (change) in the IDH2 gene. It is also being studied in the treatment of other types of cancer. Enasidenib mesylate blocks the protein made by the mutated IDH2 gene. Blocking this protein may help keep cancer cells from growing. Enasidenib mesylate is a type of enzyme inhibitor. Also called Idhifa.",
    "The mesylate salt form of enasidenib, 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."
  ],
  "synonyms": [
    "Idhifa",
    "enasidenib methanesulfonate",
    "AG-221 mesylate"
  ],
  "references": [
    "NCI Dictionary of Cancer Terms",
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/enasidenib-mesylate/"
}

Record 6,609 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.