Nilutamide

Nilutamide (Nilandron) is an orally active nonsteroidal androgen receptor antagonist with affinity for androgen receptors but not for progestogen, estrogen or glucocorticoid receptors. Nilutamide can be used to research prostate cancer. Nilutamide also has antischistosomal properties^[1][4]. IC50 & Target:Androgen receptor, Parasite^[1][4] 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^[2].
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^[2].
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^[3]. In Vivo:Nilutamide (50-400 mg/kg; p.o.; single dosage) reduces juvenile and adult Schistosoma mansoni cercariae worm burdens in infected mice^[4].