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AttributesValues
rdf:type
rdfs:label
  • Telapristone
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
  • Steroid
Preferred_Name
  • Telapristone
CAS_Registry
  • 198414-30-1
FULL_SYN
  • TelapristonePTNCI
  • 11Beta-(4-(dimethylamino)phenyl)-17-hydroxy-21-methoxy-19- norpregna-4,9-diene-3,20-dioneSNNCI
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.NCI
code
  • C104057
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