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Tibolone
[A synthetic anabolic steroid with potential menopausal symptoms suppressant activity. Tibolone exerts its effect mainly through its metabolites; its 3alpha- and 3beta-hydroxy metabolites selectively bind to and activate estrogenic receptors on bone and vaginal tissue leading to a decrease in bone turnover, improves bone density, and affects vaginal integrity and dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors in the brain and liver as well as progestogenic receptors in endometrial tissue, thereby affecting sexual function, lipid metabolism, and endometrial functions, respectively. In breast and endometrial tissue, tibolone inhibits sulfatase, thereby preventing the conversion of estrone sulfate to estrone and inhibit 17beta-hydroxysteroid dehydrogenase activity, thereby inhibiting estradiol formation from androgens and reducing estrogen-mediated effects in breast and uterus. ( NCI )]
UMLS (NCI) C0076660- Steroid
- Pharmacologic Substance
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