Drug nameCyproterone
DescriptionAn anti-androgen that, in the form of its acetate (cyproterone acetate), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. [Pubchem]
DrugBankPrimary Accession Number: DB04839
DIN00704423
TypeApproved, Investigational, Small Molecule
IndicationFor the palliative treatment of patients with advanced prostatic carcinoma.
Mechanism of ActionThe direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. In addition, cyproterone exerts a negative feed-back on the hypothalamo-pituitary axis, by inhibiting the secretion of luteinizing hormone resulting in diminished production of testicular testosterone.
AbsorptionCompletely absorbed following oral administration.
ToxicityNot available
Protein BindingNot available
Interactions
RXListNot available
KEGGdrug: Not available / compound: Not Available
PubChemcompound: 5284537 / substance: 11039334
PharmGKBPA10049
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Cytochrome P450 3A4 (CYP3A4)CYP3A41576P08684rs13306281
Target
NameGeneEntrezIDSwissprotSNP
Androgen receptorAR367ANDR_RABITrs55686369 rs35025615 rs9332972 rs9332971 rs9332970 rs9332969 rs9332968 rs5902610 rs3032358 rs1800053 rs6154 rs6153 rs6152
FilesDB04839.mol | pdb_9665226024834-0.pdb | sdf_8180392114996-0.sdf |
Smilesisomeric:
CC(=O)[C@@]1(O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)[C@@H]5C[C@@H]5[C@]4(C)[
C@H]3CC[C@]12C
canonical:
CC(=O)C1(O)CCC2C3C=C(Cl)C4=CC(=O)C5CC5C4(C)C3CCC12C

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