Nilutamide
نویسندگان
چکیده
THE CRYSTAL STRUCTURE OF NILUTAMIDE [SYSTEMATIC NAME: 5,5-dimethyl-3-[4-nitro-3-(trifluoro-meth-yl)phen-yl]imidazolidine-2,4-dione], C(12)H(10)F(3)N(3)O(4), was determined at 150 K. The dihedral angle between the mean planes through the imidazoline [maximum deviation = 0.0396 (14) Å] and benzene rings is 51.49 (5)°. The mol-ecule exhibits inter-molecular hydrogen bonding via N-H⋯O inter-actions, resulting in the formation of chains parallel to the c axis.
منابع مشابه
NILANDRON tablets contain nilutamide, a nonsteroidal, orally active antiandrogen having the chemical name 5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]-2,4-imidazolidinedione with the following structural formula: Nilutamide is a microcrystalline, white to practically white powder with a molecular weight of 317.25. Its molecular formula
CLINICAL PHARMACOLOGY Mechanism of Action Prostate cancer is known to be androgen sensitive and responds to androgen ablation. In animal studies, nilutamide has demonstrated antiandrogenic activity without other hormonal (estrogen, progesterone, mineralocorticoid, and glucocorticoid) effects. In vitro, nilutamide blocks the effects of testosterone at the androgen receptor level. In vivo, niluta...
متن کاملLong-term efficacy and safety of nilutamide plus castration in advanced prostate cancer, and the significance of early prostate specific antigen normalization. International Anandron Study Group.
PURPOSE We studied the long-term efficacy and tolerability of nilutamide, a nonsteroidal antiandrogen, combined with orchiectomy in patients with advanced prostate cancer. MATERIALS AND METHODS A large double-blind trial was done on 457 patients randomized to receive nilutamide or placebo after orchiectomy. RESULTS At 8.5 years of followup significant benefits were found for progression and...
متن کاملTolerability of Nonsteroidal Antiandrogens in the Treatment of Advanced Prostate Cancer.
This review compares the tolerability profiles of the three currently available nonsteroidal antiandrogens, flutamide, bicalutamide and nilutamide. Pharmacological effects associated with blockade of the androgen receptor are frequent with all three drugs. Gynecomastia and breast pain are seen more frequently during antiandrogen monotherapy than during combination with medical or surgical castr...
متن کاملProvocation test coupled with bronchoalveolar lavage in diagnosis of drug (nilutamide)-induced hypersensitivity pneumonitis.
A 79-year-old man was given a cumulative dose of 16.5 g of nilutamide for treatment of prostate cancer. He then presented with a respiratory illness having clinical, radiologic and functional characteristics of interstitial pneumonitis. No other cause of pneumonitis was found. Bronchoalveolar lavage showed a lymphocytic alveolitis with an inverted lymphocyte subset ratio. After an 11-week perio...
متن کاملActivity of antiandrogens against juvenile and adult Schistosoma mansoni in mice.
OBJECTIVES The antischistosomal properties of the marketed antiandrogens bicalutamide, flutamide, nilutamide and cyproterone acetate were studied both in vivo and in vitro. METHODS Schistosoma mansoni-infected mice were treated orally with 50-400 mg/kg of the antiandrogens 3 and 7 weeks post-infection. In addition, three drug combinations of nilutamide and praziquantel (200/100, 100/100 and 1...
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