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AttributesValues
rdf:type
rdfs:label
  • Telapristone Acetate
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
  • Steroid
Preferred_Name
  • Telapristone Acetate
PDQ_Open_Trial_Search_ID
  • 598776
PDQ_Closed_Trial_Search_ID
  • 598776
FULL_SYN
  • (8S,11R,13S,14S,17R)-11-(4-(Dimethylamino)phenyl)-17-(2-methoxyacetyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl AcetateSNNCI
  • CDB-4124CNNCI
  • ProgentaSYNCI
  • ProellexSYNCI
  • Telapristone AcetatePTNCI
DEFINITION
  • The acetate form of the 21-substituted-19-nor-progestin telapristone, an orally available selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Upon oral administration, CDB-4124 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
  • C104055
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