Pharmacological profile of RU 58642, a potent systemic antiandrogen for the treatment of androgen-dependent disorders

被引:21
作者
Battmann, T [1 ]
Branche, C [1 ]
Bouchoux, F [1 ]
Cerede, E [1 ]
Philibert, D [1 ]
Goubet, F [1 ]
Teutsch, G [1 ]
Gaillard-Kelly, M [1 ]
机构
[1] Roussel UCLAF, Ctr Rech, F-93235 Romainville, France
关键词
D O I
10.1016/S0960-0760(97)00151-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The pharmacological profile of RU 58642, a new non-steroidal antiandrogen was investigated both in vitro and in vivo. In vitro, the compound displays a strong and specific affinity for androgen receptor. In vivo, its antiandrogenic activity was evaluated in castrated rat supplemented with testosterone propionate and in intact animals on prostate, seminal vesicles weight and serum levels of testosterone by oral and subcutaneous route. In castrated rats RU 58642 induced a significant decrease in prostate weight at a dose as low as 0.3 mg/kg whatever the route of administration. In intact rats its activity was compared to that of other non-steroidal antiandrogens such as flutamide, nilutamide and bicalutamide. RU 58642 proved to be significantly more potent than the reference compounds in reducing prostate weight: 3-30 times orally and 3-100 times subcutaneously, and thus the most potent antiandrogen to date to our knowledge. These results suggest that this compound may be very useful in the treatment of systemic androgen-dependent diseases. (C) 1998 Elsevier Science Ltd. All rights reserved.
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收藏
页码:103 / 111
页数:9
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