Drug nameNilutamide
DescriptionNilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration.
DrugBankPrimary Accession Number: DB00665
DIN02221861
TypeApproved, Small Molecule
IndicationFor use in combination with surgical castration for the treatment of metastatic prostate cancer (Stage D2)
Mechanism of ActionNilutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
AbsorptionRapidly and completely absorbed, yielding high and persistent plasma concentrations.
ToxicitySymptoms of overdose include dizziness, general discomfort, headache, nausea, and vomiting.
Protein BindingNot available
Interactions
RXListhttp://www.rxlist.com/cgi/generic2/nilutam.htm
KEGGdrug: D00965 / compound: C08164
PubChemcompound: 4493 / substance: 7848028
PharmGKBPA450632
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Cytochrome P450 2C19 (CYP2C19)CYP2C191557P33261rs58430367 rs17861152
NADPH-cytochrome P450 reductasePOR5447P16435rs11544669
Target
NameGeneEntrezIDSwissprotSNP
Alpha-1A adrenergic receptorADRA1A148ADA1A_HUMANrs56318220 rs56233953 rs59765666 rs1048101 rs56394436 rs7833704 rs3730287 rs3730247 rs2229126 rs2229125 rs2229124 rs1496121 rs1383914 rs1048102
Androgen receptorAR367ANDR_RABITrs55686369 rs35025615 rs9332972 rs9332971 rs9332970 rs9332969 rs9332968 rs5902610 rs3032358 rs1800053 rs6154 rs6153 rs6152
FilesDB00665.mol | pdb_153090981309-0.pdb | sdf_6573766914996-0.sdf |
Smilesisomeric:
CC1(C)NC(=O)N(C1=O)C1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F
canonical:
CC1(C)NC(=O)N(C1=O)C1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F

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