Preferred Label : IDH1(R132) Inhibitor IDH305;
NCIt 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.;
Molecule name : IDH305;
Origin ID : C121457;
UMLS CUI : C4053635;
Semantic type(s)
- concept_is_in_subset
- has_target
