cyproterone acetate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.00 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 10.28 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 100 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIM2,PRKDC,STK33,TEK,ZAP70 29
kinase-selectivity-class EIF2AK3,GRK2 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1974 YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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 1028.14 56.50 148 863 4923 90622513

FDA Adverse Event Reporting System (Male)

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 564.60 41.67 82 721 1645 42618887
Meningioma benign 46.46 41.67 6 797 45 42620487

FDA Adverse Event Reporting System (Geriatric)

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 1422.49 38.67 208 1498 5457 110582136
Meningioma benign 58.72 38.67 9 1697 307 110587286
Frontotemporal dementia 45.09 38.67 8 1698 675 110586918
Prosopagnosia 43.61 38.67 6 1700 94 110587499
Hepatitis fulminant 42.29 38.67 12 1694 8548 110579045
Aphasia 39.74 38.67 19 1687 58978 110528615

FDA Adverse Event Reporting System (Pediatric)

None

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 D006727 Hormone Antagonists
MeSH PA D000970 Antineoplastic Agents
MeSH PA D003272 Contraceptive Agents, Male
MeSH PA D012102 Reproductive Control Agents
CHEBI has role CHEBI:35497 androgen antagonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:59826 progestin
CHEBI has role CHEBI:176497 geroprotector

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

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
Mu-type opioid receptor GPCR Ki 6.05 DRUG MATRIX
Glucocorticoid receptor Nuclear hormone receptor IC50 7.80 WOMBAT-PK
Progesterone receptor Nuclear hormone receptor IC50 9.68 WOMBAT-PK
Androgen receptor Transcription factor IC50 4.74 CHEMBL
Progesterone receptor Transcription factor Ki 8.32 DRUG MATRIX
Adenosine receptor A1 GPCR IC50 8.30 CHEMBL

External reference:

IDSource
N0000167457 NUI
D01368 KEGG_DRUG
22054 RXNORM
C0056855 UMLSCUI
CHEBI:50743 CHEBI
CA4 PDB_CHEM_ID
CHEMBL139835 ChEMBL_ID
D017373 MESH_DESCRIPTOR_UI
DB04839 DRUGBANK_ID
9880 PUBCHEM_CID
2865 IUPHAR_LIGAND_ID
4KM2BN5JHF UNII
003475 NDDF
004825 NDDF
126119006 SNOMEDCT_US
126120000 SNOMEDCT_US
96370002 SNOMEDCT_US
C0010621 UMLSCUI
2098-66-0 SECONDARY_CAS_RN
5284537 PUBCHEM_CID
2050 INN_ID
D003534 MESH_DESCRIPTOR_UI
E61Q31EK2F UNII
CHEBI:50742 CHEBI
4KM2BN5JHF INXIGHT DRUGS
E61Q31EK2F INXIGHT DRUGS

Pharmaceutical products:

None