4838
T3D4783
Nilutamide
Nilutamide 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 that 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.
63612-50-0
4493
C12H10F3N3O4
White powder.
4.19e-03 g/L
Rapidly and completely absorbed, yielding high and persistent plasma concentrations.
Nilutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin that stimulate the growth of normal and malignant prostatic tissue. This blockade of androgen receptors may result in growth arrest or transient tumor regression through inhibition of androgen-dependent DNA and protein synthesis.
The results of a human metabolism study using 14C-radiolabelled tablets show that nilutamide is extensively metabolized and less than 2% of the drug is excreted unchanged in urine after 5 days.
Route of Elimination: Nilutamide is extensively metabolized andless than 2% of the drug is excreted unchanged in urine after 5 days. Fecal elimination is negligible, ranging from 1.4% to 7% of the dose after 4 to 5 days.
Half Life: 38.0-59.1 hours
No indication of carcinogenicity to humans (not listed by IARC).
For use in combination with surgical castration for the treatment of metastatic prostate cancer involving distant lymph nodes, bone, or visceral organs (Stage D2).
Symptoms of overdose include dizziness, general discomfort, headache, nausea, and vomiting.
2014-09-11T05:16:24Z
2014-12-24T20:26:57Z
Nilutamide
C08164
7573
DB00665
true
CC1(C)N=C(O)N(C1=O)C1=CC(=C(C=C1)N(=O)=O)C(F)(F)F
C12H10F3N3O4
InChI=1S/C12H10F3N3O4/c1-11(2)9(19)17(10(20)16-11)6-3-4-8(18(21)22)7(5-6)12(13,14)15/h3-5H,1-2H3,(H,16,20)
InChIKey=XWXYUMMDTVBTOU-UHFFFAOYSA-N
317.2207
317.062340438
Exogenous
Solid
1.8
HMDB14803
CHEMBL1274
4337