Title: "Casodex" (ICI 176,334)--a new, pure, peripherally-selective anti-androgen: preclinical studies.
Title Abreviation: Horm Res Date of Pub: 1989
Author: Furr BJ;
Issue/Part/Supplement: -HEADING- Volume Issue: 32 Suppl 1 Pagination: 69-76
MESH Headings: Androgen Antagonists (PD/PK/*TU); Anilides (PD/PK/*TU); Animal; Cyproterone (AA/TU); Dogs; Flutamide (TU); Imidazoles (TU); Male; Prostatic Neoplasms (*DT); Rats; -RN-;
Journal Title Code: GBI Publication Type: JOURNAL ARTICLE
Date of Entry: 900315N Entry Month: 9005
Country: SWITZERLAND Index Priority: 2
Language: Eng Unique Identifier: 90128934
Unique Identifier: 90128934 ISSN: 0301-0163
Abstract: 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.
Abstract By: Author
Address: Bioscience I, ICI Pharmaceuticals, Macclesfield, Cheshire, UK.

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