86-MM1076.00-0250 - tibolone | 5630-53-5

Applications A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome.
References de Visser, J., et al.: Arzneim.-Forsch., 34, 1010 (1984), Geusens, P., et al.: Maturitas Suppl, 1, 1 (1987)

Tibolone is a synthetic steroidal estrogen with both estrogenic and progestogenic activity. It has been shown to be effective in the treatment of postmenopausal symptoms, especially those related to the breast. Tibolone is also used for prevention of osteoporosis and to prevent recurrence of hormone-dependent cancers such as breast cancer or endometrial cancer. Tibolone binds to both estrogen receptor subtypes (ERα and ERβ) and progesterone receptor (PR), but with higher affinity for ERβ. This leads to increased levels of circulating estradiol and progesterone when compared to other estrogens such as nomegestrol acetate or conjugated equine estrogen. The drug also decreases expression of genes that are regulated by the response element (RE) in ERβ-positive cells, which may contribute to its anti-cancer effects. Tibolone has been shown to be statistically more effective than nomegestrol acetate in reducing hot flashes