Nilutamide: an antiandrogen for the treatment of prostate cancer

Ann Pharmacother. 1997 Jan;31(1):65-75. doi: 10.1177/106002809703100112.


Objective: To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of nilutamide and to compare this agent with the currently marketed nonsteroidal antiandrogens (i.e., bicalutamide, flutamide) by critically analyzing the published literature.

Data sources: MEDLINE (1980-1995) and CANCERLIT (1991-1995) were searched for English-language publications using the terms nilutamide, bicalutamide, and flutamide alone, and either nilutamide or androgen antagonists in combination with prostatic neoplasms.

Study selection and data extraction: All articles with subject matter on nilutamide, bicalutamide, and flutamide were considered for inclusion. For studies published in more than one journal, the first publication was used unless a subsequent publication included additional or follow-up data, in which case the latter publication was cited instead.

Data synthesis: Nilutamide was effective in combination with orchiectomy in improving responses in patients with advanced prostate cancer. However, patient survival was not improved in these trials, and improvements in bone pain did not usually result in improved performance status in these patients. The few trials of nilutamide monotherapy or nilutamide in combination with a luteinizing hormone-releasing hormone analog are too small to draw meaningful conclusions regarding its efficacy or its role in the treatment of advanced prostate cancer. No comparative trials of nilutamide with other antiandrogens and no analysis of the impact of nilutamide on patient quality of life are currently available. Nilutamide appears to produce a higher frequency of adverse effects than the other currently marketed nonsteroidal antiandrogens, bicalutamide and flutamide.

Conclusions: Nilutamide does not appear to represent a major advance in the treatment of advanced prostate cancer and appears to be somewhat inferior to both flutamide and bicalutamide with regard to adverse effects. Nilutamide should not be considered the antiandrogen of choice in the treatment of advanced prostate cancer.

Publication types

  • Review

MeSH terms

  • Androgen Antagonists / adverse effects
  • Androgen Antagonists / pharmacokinetics
  • Androgen Antagonists / therapeutic use*
  • Anilides / therapeutic use
  • Flutamide / therapeutic use
  • Half-Life
  • Humans
  • Imidazoles / adverse effects
  • Imidazoles / pharmacokinetics
  • Imidazoles / therapeutic use*
  • Imidazolidines*
  • Male
  • Nitriles
  • Orchiectomy
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / mortality
  • Prostatic Neoplasms / surgery
  • Structure-Activity Relationship
  • Tosyl Compounds


  • Androgen Antagonists
  • Anilides
  • Imidazoles
  • Imidazolidines
  • Nitriles
  • Tosyl Compounds
  • nilutamide
  • Flutamide
  • bicalutamide