Preferred Label : Safusidenib;
NCIt synonyms : Mutant Isocitrate Dehydrogenase Type 1 Inhibitor DS-1001;
NCIt definition : An orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1; IDH-1; IDH1
[NADP ] soluble) mutant forms, including substitution mutations at the arginine in
position 132, IDH1(R132) (IDH1-R132), with potential antineoplastic activity. Upon
oral administration, safusidenib specifically binds to and inhibits certain mutant
forms of IDH1, 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 mutations. 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. Safusidenib
minimally targets and affects wild-type IDH1, which is expressed in normal, healthy
cells.;
UNII : RCK8KK7SB9;
CAS number : 1898206-17-1;
Molecule name : DS 1001; DS-1001; DS-1001b; AB 218; AB-218;
NCI Metathesaurus CUI : CL550810;
Origin ID : C148134;
UMLS CUI : C5706633;
Semantic type(s)
- concept_is_in_subset
- has_target
