Nilutamide (Nilandron, Anandron, RU 23908) is an androgen receptor (AR) blocker with an IC50 of 0.4 μM. The twofold stimulation of Shionogi cell proliferation caused by a 10-day exposure to 1 nM testosterone is competitively reversed by incubation with Nilutamide, at the IC50. Nilutamide at the IC50 values of 87 nM and in T-47D and ZR-75-1 cells blocks the marked increase in GCDFP-15 release induced by 1 nM testosterone.Nilutamide blocks the androgen induction of CYP27A1. Treatment of the HepG2 cells with dihydrotestosterone in presence of the AR antagonist Nilutamide almost completely abolishes the dihydrotestosterone-induced effect on the CYP27A1 promoter activity. Incubation with 100 µg/mL Nilutamide results in decreased movement of S. mansoni adults. Nilutamide inhibits hepatic cytochrome P-450 activity. Total worm burden reductions of 5.1%–35.6% are achieved with Nilutamide. The highest female worm burden reduction of 75.4% is observed with a 200 mg/kg dose of Nilutamide, while moderate female worm burden reductions of 22.5%–27.5% are observed following 50 mg/kg, 100 mg/kg and 400 mg/kg Nilutamide doses. At 400 mg/kg, Nilutamide reduced total and female worm burdens by 84.8% and 71.3%, respectively. Combinations of Nilutamide (100 mg/kg) and praziquantel (50 mg/kg or 100 mg/kg) reveals an increase in worm survival, above the level observed with praziquantel or Nilutamide monotherapy. However, a combination of Nilutamide (200 mg/kg) and praziquantel (100 mg/kg) produces statistically significant total and female worm burden reductions by 90.6% and 85.1%, respectively. Anandron (20 mg/kg/day) with even low doses of buserelin leads to an immediate decrease in prostate weight that is complete at 15 days. Nilutamide and Dasatinib has entered in a phase II clinical trial in the treatment of prostate cancer. Nilutamide plus bicalutamide, buserelin, cyproterone acetate, flutamide, goserelin or leuprolide acetate has entered in a phase III clinical trial in the treatmetn of prostate cancer.
Molecular Weight | 317.22 |
Formula | C12H10F3N3O4 |
CAS Number | 63612-50-0 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] No authors listed. Nilutamide
[2] Niraj S Trasi, et al. Nilutamide
[3] E J Dole, et al. Nilutamide: an antiandrogen for the treatment of prostate cancer
[5] P J Creaven, et al. Pharmacokinetics and metabolism of nilutamide
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