MLchartDataset catalogue

IDH1(R132) inhibitor IDH305

Term · Oncology and biomedicine · MLC-T-ONC-014309

An inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. Upon administration, IDH305 specifically inhibits IDH1(R132) mutant forms in the cytoplasm, which inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1(R132)-expressing tumor cells. 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.

Table 1. Record
IdentifierMLC-T-ONC-014309
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-014309",
  "term": "IDH1(R132) inhibitor IDH305",
  "field": "Oncology and biomedicine",
  "definition": "An inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity. Upon administration, IDH305 specifically inhibits IDH1(R132) mutant forms in the cytoplasm, which inhibits the formation of the oncometabolite 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1(R132)-expressing tumor cells. 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.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/idh1-r132-inhibitor-idh305/"
}

Record 8,925 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.