Drug nameFlutamide
DescriptionAn antiandrogen with about the same potency as cyproterone in rodent and canine species.
DrugBankPrimary Accession Number: DB00499
DIN02239388
TypeApproved, Small Molecule
IndicationFor the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate
Mechanism of ActionFlutamide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Flutamide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.
AbsorptionRapidly and completely absorbed
ToxicityIn animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia.
Protein Binding94-96%
Interactions
RXListhttp://www.rxlist.com/cgi/generic2/flutam.htm
KEGGdrug: D00586 / compound: C07653
PubChemcompound: 3397 / substance: 9855
PharmGKBPA449685
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Cytochrome P450 1A2 (CYP1A2)CYP1A21544P05177rs740602 rs17853490
Target
NameGeneEntrezIDSwissprotSNP
Androgen receptorAR367ANDR_RABITrs55686369 rs35025615 rs9332972 rs9332971 rs9332970 rs9332969 rs9332968 rs5902610 rs3032358 rs1800053 rs6154 rs6153 rs6152
FilesDB00499.mol | DB00499_2003-04-01.pdf | DB00499_557.pdf | pdb_7643298824834-0.pdb | sdf_299011214996-0.sdf |
Smilesisomeric:
CC(C)C(=O)NC1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F
canonical:
CC(C)C(=O)NC1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F

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