Tibolone is a Selective Tissue Estrogen Activity Regulator (STEARs), which is a synthetic steroid hormone.
Basic Information
CAS Number: 5630-53-5
Molecular Formula: C21H28O2
Molecular Weight: 312.45
English Name: Tibolone
Pharmacological Effects
Tibolone has weak hormonal activity itself and exerts its pharmacological effects primarily through tissue-specific enzymatic activity and tissue-specific metabolic mechanisms, exhibiting different effects in different tissues. After oral administration, Tibolone is rapidly metabolized into three compounds that play their roles:
3α-OH-Tibolone and 3β-OH-Tibolone, both metabolites exhibit estrogenic activity.
The third metabolite, the Δ4-isomer of Tibolone, possesses progestogenic and androgenic activity.
Clinical Applications
Tibolone is primarily used in the treatment of climacteric syndrome in women, including alleviating vasomotor symptoms, improving genitourinary atrophy symptoms, preventing bone loss, and reducing the incidence of fractures. Additionally, it enhances quality of life. Specifically, Tibolone can be used for:
Treatment of uterine fibroids, recommended for patients with fibroids <3cm, with regular monitoring.
Treatment of endometriosis, reducing the incidence of pelvic pain.
Add-back therapy with hypothalamic gonadotropin-releasing hormone to alleviate climacteric symptoms and prevent osteoporosis.
