Preferred Label : Telapristone;
NCIt synonyms : 11Beta-(4-(dimethylamino)phenyl)-17-hydroxy-21-methoxy-19- norpregna-4,9-diene-3,20-dione;
NCIt definition : An orally available 21-substituted-19-nor-progestin and selective progesterone receptor
modulator (SPRM), with potential anti-progesterone and antineoplastic activities.
Upon oral administration, telapristone competitively binds to the progesterone receptor
(PR) in progesterone-responsive tissue and inhibits PR-mediated gene expression. This
interferes with progesterone activity in the reproductive system. As a result, this
agent may suppress ovulation and inhibit proliferation of endometrial tissue. Also,
this agent may prevent cell growth and induce apoptosis in estrogen receptor (ER)
and PR-positive breast cancer cells through a reduction in progesterone levels, ER
downregulation and a suppression of the expression of cyclin-dependent kinases (CDK)
2 and 4, ultimately leading to G1/S cell cycle arrest. Unlike some other SPRMs, this
agent does not exert any estrogenic, androgenic, anti-estrogenic, and anti-androgenic
activities.;
UNII : 65703MV349;
InChIKey : BHERMCLNVOVDPU-DQFOBABISA-N;
CAS number : 198414-30-1; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 198414-30-1
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G-SRS /a ;
Origin ID : C104057;
UMLS CUI : C3641719;
Semantic type(s)
- concept_is_in_subset
