"Casodex" (ICI 176,334)--a new, pure, peripherally-selective anti-androgen: preclinical studies

Horm Res. 1989;32 Suppl 1:69-76. doi: 10.1159/000181315.


The relative merits of the steroidal anti-androgen, cyproterone acetate, and the non-steroidal anti-androgens flutamide and nilutamide, are reviewed. It is concluded that pure anti-androgens offer some advantages over cyproterone acetate but that they each have some features which merit improvement. A new compound which was a pure anti-androgen, peripherally selective, well tolerated with a long half-life would have significant advantages. Preclinical studies in rats and dogs show that Casodex (ICI 176,334) is a potent pure anti-androgen which is well tolerated and has a long half-life. Casodex induces marked regression of the prostate yet fails to cause the substantial elevation in serum LH and testosterone seen with flutamide and nilutamide; it is thus peripherally selective. Casodex is as effective as surgical or medical castration with Zoladex in limiting the growth of the transplantable androgen-responsive Dunning rat prostate tumour. Such a profile makes Casodex a strong candidate as the future anti-androgen of choice for the treatment of prostate cancer and benign prostate hypertrophy.

MeSH terms

  • Androgen Antagonists / pharmacokinetics
  • Androgen Antagonists / pharmacology
  • Androgen Antagonists / therapeutic use*
  • Anilides / pharmacokinetics
  • Anilides / pharmacology
  • Anilides / therapeutic use*
  • Animals
  • Cyproterone / analogs & derivatives
  • Cyproterone / therapeutic use
  • Cyproterone Acetate
  • Dogs
  • Flutamide / therapeutic use
  • Imidazoles / therapeutic use
  • Imidazolidines*
  • Male
  • Nitriles
  • Prostatic Neoplasms / drug therapy*
  • Rats
  • Tosyl Compounds


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