"目录号: HY-14281
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Trilostane(Win 24540; Modrastane)是3 β-羟化类固醇脱氢酶抑制剂，可作用于库兴氏综合征。
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生物活性
Description
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.IC50 value:Target: 3 β-HSDTrilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase (3-β-HSD or delta 5-delta 4-isomerase), an essential enzyme for the biosynthesis of all classes of hormonal steroids. It has been used in the treatment of Cushing′s syndrome for stopping the production of cortisol, and is currently approved for dogs in the US, but is still a human drug in the UK and other countries. It is being investigated as a possible treatment for both breast cancer and prostate cancer to prevent the synthesis of estrogens and androgens from endogenous precursors. It has also been used to inhibit endogenous production of progesterone in research studies.
Clinical Trial
NCT00181597
Genzyme, a Sanofi Company-Sanofi
Prostate Cancer-Prostate Adenocarcinoma
March 2004
Phase 2
NCT01615211
Kristina Gemzell Danielsson-Karolinska Institutet-The University of Hong Kong
Medical Abortion, Complete or Unspecified, Without Complication
May 2012
Phase 2
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References
[1].Helm JR, et al. A comparison of factors that influence survival in dogs with adrenal-dependent hyperadrenocorticism treated with mitotane or trilostane. J Vet Intern Med. 2011 Mar-Apr;25(2):251-60.
[2].Feldman EC, et al. Trilostane dose versus body weight in the treatment of naturally occurring pituitary-dependent hyperadrenocorticism in dogs. J Vet Intern Med. 2012 Jul-Aug;26(4):1078-80.