Nilutamide

Abstract

Nilutamide is a nonsteroidal antiandrogen 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 which stimulate the growth of normal and cancerous prostatic tissue. Nilutamide has a long half-life which permits once-daily administration. Nilutamide is usually given in combination with surgical or chemical castration using gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH)] agonists. In castrated patients the addition of nilutamide improves objective response rates, bone pain, urinary symptoms, tumour markers and time to disease progression. The tolerance of nilutamide is generally acceptable. Adverse effects are usually mild and reversible and consistent with androgen depletion. Unexpected but reversible adverse effects of nilutamide include delayed adaption to dark after exposure to bright light, transient increases in transaminases, and more severe but rare interstitial pneumonitis. Thus, nilutamide is a welcome treatment option that may be particularly useful in patients to whom the convenience of once-daily administration is seen as a worthwhile benefit.

Inhibitors of the PI3K/Akt/mTOR Pathway in Prostate Cancer Chemoprevention and Intervention

“…Abiraterone inhibits androgenic steroid synthesis [ 29 ], while enzalutamide and darolutamide are AR antagonists [ 30 ]. Apalutamide, flutamide, and nilutamide are other common AR inhibitors [ 29 , 31 ]. Gonadotropin-releasing hormone (GnRH) agonists or antagonist therapy is a specific type of ADT.…”

Square wave adsorptive stripping voltammetric determination of anticancer drug nilutamide in biological fluids using cationic surfactant cetyltrimethylammonium bromide

“…1 Reports on the lung toxicity of drugs containing nitro aromatic groups explain their toxicity as resulting from ring oxidation and nitro reductive biotransformation pathways. It blocks the action of androgens of adrenal and testicular origin, which stimulate the growth of normal and cancerous prostatic tissue.…”

“…It blocks the action of androgens of adrenal and testicular origin, which stimulate the growth of normal and cancerous prostatic tissue. 1 Reports on the lung toxicity of drugs containing nitro aromatic groups explain their toxicity as resulting from ring oxidation and nitro reductive biotransformation pathways. 2 Acute liver failure, interstitial pneumonitis and mild elevations in serum enzymes have been reported during NLM therapy.…”

Delayed Antiandrogen Withdrawal Syndrome After Discontinuation of Bicalutamide

“…The half-lives of flutamide, nilutamide, and bicalutamide are 7.8 hours, 56 hours, and 1 week, respectively 17-19 . Therefore, the time required to endure 4 half-lives for washout from the serum would be 31.2 hours, 9.3 days, and 4 weeks, respectively.…”