Tibolone is a progestin structurally related to norethynodrel. Its mechanism of action is tissue specific. Tibolone, after oral ingestion, is converted to three active metabolites which have different binding affinities to the various sexual steroid receptors. Tibolone has been used in the treatment of climacteric symptoms, improving mood and sexual response, and in the prevention and treatment of osteoporosis. It increases the risk of stroke, and its behavior in the breast is similar to estrogen plus progestin menopause therapy. Tissue-selective estrogen complex (TSEC) is the combination of a selective estrogen receptor modulator (SERM) with an estrogen. The unique TSEC that we have is the combination of Bazedoxifene (BZA), a SERM of the third generation that is used for osteoporosis management in postmenopausal women at fracture risk, having demonstrated a powerful antiestrogenic effect on the endometrium and conjugated estrogens (CE). This TSEC is designed to not only improve menopausal symptoms and vulvovaginal atrophy but also to prevent bone loss. So it maintains the benefits of estrogen therapy while antagonizes stimulation effects on the endometrium and mammary gland without the effects associated with progestins.

错误:搜索内容不能为空,请输入英文关键词
错误:关键词超出字数限制,请精简
高级检索

Hormone Therapy (II): Tibolone and the TSEC Concept

  • Santiago Palacios,
  • Mariella Lilue

摘要

Tibolone is a progestin structurally related to norethynodrel. Its mechanism of action is tissue specific. Tibolone, after oral ingestion, is converted to three active metabolites which have different binding affinities to the various sexual steroid receptors. Tibolone has been used in the treatment of climacteric symptoms, improving mood and sexual response, and in the prevention and treatment of osteoporosis. It increases the risk of stroke, and its behavior in the breast is similar to estrogen plus progestin menopause therapy. Tissue-selective estrogen complex (TSEC) is the combination of a selective estrogen receptor modulator (SERM) with an estrogen. The unique TSEC that we have is the combination of Bazedoxifene (BZA), a SERM of the third generation that is used for osteoporosis management in postmenopausal women at fracture risk, having demonstrated a powerful antiestrogenic effect on the endometrium and conjugated estrogens (CE). This TSEC is designed to not only improve menopausal symptoms and vulvovaginal atrophy but also to prevent bone loss. So it maintains the benefits of estrogen therapy while antagonizes stimulation effects on the endometrium and mammary gland without the effects associated with progestins.