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| 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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