Nilutamide

Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate Y. 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 Y 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. (In Vitro) :Nilutamide (110 μM) inhibits hexobarbital hydroxylase, benzphetamine N-demethylase, benzo (a) pyrene hydroxylase and 7-ethoxycoumarin O-deethylase activities by 85, 40, 35 and 25%, respectively, in human liver microsomes.Nilutamide (550 μM) does not significantly increase the consumption of NADPH by aerobic microsomes, and does not modify the kinetics for the reduction of cytochrome P-450 by NADPH-cytochrome P-450 reductase in an anaerobic system.Nilutamide blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone in T-47D cells and ZR-75-1 cells with IC50s of 87 nM and 75 nM, respectively. (In Vivo) :Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adult Schistosoma mansoni cercariae worm burdens in infected mice.