Preferred Label : Vorasidenib Citrate;
NCIt synonyms : Vorasidenib Hemicitric Acid Hemihydrate;
NCIt definition : The hemicitrate, hemihydrate form of vorasidenib, an orally available inhibitor of
wild-type (WT) and mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1
[NADP ] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP
], mitochondrial) in the mitochondria, with potential antineoplastic activity. Upon
administration, vorasidenib specifically targets and inhibits WT and mutant forms
of IDH1 and IDH2, 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 IDH1 or IDH2 mutations and/or overexpressing IDH1 or IDH2.
In addition, vorasidenib is able to penetrate the blood-brain barrier (BBB). IDH1
and 2, metabolic enzymes that catalyze the conversion of isocitrate into a-KG, play
key roles in energy production and are mutated in a variety of cancer cell types.
In addition, mutant forms of IDH1 and 2 catalyze the formation of 2HG and drive cancer
growth by blocking cellular differentiation and inducing cellular proliferation.;
UNII : X478M962XG;
InChIKey : YOUTVRFNJAAFNS-DLVAHKFUSA-N;
CAS number : 2316810-02-1;
Drug name : Voranigo;
NCI Metathesaurus CUI : CL1412486;
Origin ID : C174942;
UMLS CUI : C5421038;
Currated CISMeF NLP mapping
- Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- is_component_of_chemotherapy_regimen
- is_salt_form_of
