Synthetic steroid with estrogenic, progestogenic and weak androgenic activity
ATC code: G03CX01 (Tibolone)
Tibolone is metabolized to three active forms: 3α-OH-tibolone and 3β-OH-tibolone act as estrogens on bone and the vulvovaginal mucosa, while the Δ4-isomer carries progestogenic and weak androgenic activity. Tissue-selective action delivers estrogenic effect on bone and vagina without significant stimulation of the endometrium and breast. Effect on hot flashes is comparable to low-dose combined MHT. Evidence rests on the LIBERATE and LIFT trials.
First line
Reduces frequency and severity of hot flashes and night sweats. NAMS 2022 and IMS 2024 meta-analyses show efficacy comparable to combined MHT (estradiol + progestogen). In women with an intact uterus it is taken continuously at 2.5 mg daily – no separate progestogen is required. In women over 60 it is not recommended due to increased stroke risk (LIFT trial).
Use only in women at least 12 months after their last menstrual period.
Second line
Reduces vertebral and non-vertebral fracture risk by 45% and 26% respectively (LIFT). Bone mineral density gains are smaller than with bisphosphonates and denosumab, so tibolone is an alternative in women with climacteric symptoms for whom osteoporosis is a secondary goal. Not the first choice once osteoporosis is the established diagnosis.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Tibolone is a synthetic steroid with estrogenic, progestogenic, and weak androgenic activity. It is prescribed for marked vasomotor symptoms of menopause and for postmenopausal osteoporosis prevention in women more than one year after menopause (NAMS 2022, NG23). In anti-aging practice, tibolone is positioned as a universal anti-aging drug for postmenopausal women to rejuvenate skin and libido. In women without marked menopausal symptoms, no clinical studies of prophylactic anti-aging use exist. The LIFT trial (2008) showed increased stroke risk in women over 60 on tibolone. Also: increased breast cancer recurrence (LIBERATE 2009), venous thromboembolism, and gallbladder disease. If tibolone was prescribed for anti-aging, consider seeking a second opinion.
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Pregnancy is an absolute contraindication. Stop the drug if pregnancy is suspected.
Breastfeeding is a contraindication. Active metabolites pass into milk and may affect the infant.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Tibolone is evaluated for the following indications with varying evidence strength: Menopausal vasomotor symptoms (evidence tier A), Postmenopausal osteoporosis (evidence tier B), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Tibolone (≥ 1 in 100): Breast tenderness, Light vaginal bleeding/spotting in early months, Weight gain, Vaginal discharge, Headache. See the Safety section for uncommon and serious reactions.
FDA category X. Pregnancy is an absolute contraindication. Stop the drug if pregnancy is suspected.
Breastfeeding is a contraindication. Active metabolites pass into milk and may affect the infant.
Tibolone is contraindicated in: History or suspicion of breast cancer; Estrogen-dependent malignancies (endometrial cancer); Undiagnosed vaginal bleeding; Active or prior venous thromboembolism; Prior arterial thromboembolism (stroke, MI). Full list in the Safety section.