Preferred Label : Palazestrant;
NCIt synonyms : CERAN OP-1250; Complete Estrogen Receptor Antagonist OP-1250;
NCIt definition : An orally available, small molecule antagonist of estrogen receptor alpha (ERalpha;
ERa; ESR1; nuclear receptor subfamily 3, group A, member 1; NR3A1) and a selective
ER degrader (SERD), with potential antineoplastic activity. Upon oral administration,
palazestrant competes with the endogenous activating estrogenic ligand 17-beta estradiol
for binding in the ligand binding pocket of ERalpha, thereby inhibiting the activity
of ERalpha. Palazestrant blocks estrogen-driven transcriptional activity and induces
degradation of ERalpha. This inhibits the growth and survival of ERalpha-expressing
cancer cells. ERalpha, a nuclear hormone receptor, is often overexpressed and/or mutated
in a variety of cancer cell types. It plays a key role in tumor cell proliferation
and survival.;
UNII : VU35KM56Q4;
CAS number : 2092925-89-6;
Molecule name : OP-1250; OP 1250;
NCI Metathesaurus CUI : CL1642919;
Origin ID : C176877;
UMLS CUI : C5854859;
Semantic type(s)
- concept_is_in_subset
- has_target
