Preferred Label : Vorasidenib;
NCIt definition : An orally available inhibitor of 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 inhibits 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 IDH mutations. 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 : 789Q85GA8P;
InChIKey : QCZAWDGAVJMPTA-RNFRBKRXSA-N;
CAS number : 1644545-52-7;
Molecule name : AG-881; AG 881;
Codes from synonyms : 120883;
Origin ID : C152914;
UMLS CUI : C4726974;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_salt_form
- has_target
- is_free_acid_or_base_form_of
