cyproterone acetate Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
antiandrogens 766 427-51-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cyproterone acetate
  • cyproviron
An agent with anti-androgen and progestational properties. It shows competitive binding with dihydrotestosterone at androgen receptor sites.
  • Molecular weight: 416.94
  • Formula: C24H29ClO4
  • CLOGP: 3.96
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 60.44
  • ALOGS: -5.44
  • ROTB: 3

Drug dosage:

DoseUnitRoute
0.10 g O
0.10 g P

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1974 YEAR INTRODUCED

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Meningioma 143.15 61.81 18 64 931 4637979
Rhabdomyolysis 100.98 61.81 20 62 19538 4619372

Pharmacologic Action:

SourceCodeDescription
ATC G03HA01 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
ANTIANDROGENS
Antiandrogens, plain
ATC G03HB01 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
ANTIANDROGENS
Antiandrogens and estrogens
MeSH PA D000726 Androgen Antagonists
MeSH PA D000970 Antineoplastic Agents
MeSH PA D003270 Contraceptive Agents
MeSH PA D003272 Contraceptive Agents, Male
MeSH PA D006727 Hormone Antagonists
MeSH PA D012102 Reproductive Control Agents
CHEBI has role CHEBI:35497 androgen antagonist

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Androgen receptor Nuclear hormone receptor ANTAGONIST IC50 7.43 WOMBAT-PK IUPHAR
Progesterone receptor Nuclear hormone receptor IC50 9.68 WOMBAT-PK
Mu-type opioid receptor GPCR Ki 6.05 DRUG MATRIX
Glucocorticoid receptor Nuclear hormone receptor IC50 7.80 WOMBAT-PK
Progesterone receptor Transcription factor Ki 8.32 DRUG MATRIX
Androgen receptor Transcription factor IC50 4.74 CHEMBL
Adenosine receptor A1 GPCR IC50 8.30 CHEMBL

External reference:

IDSource
D003534 MESH_DESCRIPTOR_UI
N0000167457 NUI
C0056855 UMLSCUI
D01368 KEGG_DRUG
4KM2BN5JHF UNII
003475 NDDF
22054 RXNORM
126120000 SNOMEDCT_US
CHEMBL142130 ChEMBL_ID
CHEMBL139835 ChEMBL_ID
2050 INN_ID
2098-66-0 SECONDARY_CAS_RN
CA4 PDB_CHEM_ID
DB04839 DRUGBANK_ID
CHEBI:50743 CHEBI
2865 IUPHAR_LIGAND_ID
D017373 MESH_DESCRIPTOR_UI
9880 PUBCHEM_CID

Pharmaceutical products:

None