Olutasidenib

{
  "id": "MLC-T-ONC-006056",
  "term": "Olutasidenib",
  "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 and has a mutation (change) in the IDH1 gene. It is also being studied in the treatment of other types of cancer. Olutasidenib blocks the protein made by the mutated IDH1 gene. Blocking this protein may help keep cancer cells from growing. Olutasidenib is a type of enzyme inhibitor. Also called Rezlidhia.",
    "An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1 [NADP+] soluble) with a mutation at arginine (R) 132, IDH1(R132), with potential antineoplastic activity. Upon administration, olutasidenib specifically inhibits IDH1(R132), thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH(R132). IDH1(R132) mutations are highly expressed in certain malignancies, including gliomas; they initiate and drive cancer growth by both blocking cell differentiation and catalyzing the formation of 2HG."
  ],
  "synonyms": [
    "Rezlidhia",
    "IDH1-R132 inhibitor FT-2102"
  ],
  "references": [
    "NCI Dictionary of Cancer Terms",
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/olutasidenib/"
}