PAD Refills

What is tibolone (Tibella)? The basis of Health Canada’s approval of tibolone for vasomotor symptoms associated with menopause.

Download as a PDF

Read previous PAD Refills newsletters

The BC Provincial Academic Detailing (PAD) service's topic Medications for menopause-associated vasomotor and genitourinary symptoms delivers evidence and practical drug information for the most commonly prescribed estrogen and progestogen products (oral, transdermal, vaginal).¹ Visit www.bcpad.ca to book a session with an academic detailing pharmacist in your area. We received this question during PAD sessions: What is tibolone (Tibella)?  

Basics^2-5

Tibolone (Tibella) is a prohormone with three active metabolites: two metabolites have estrogenic activity, one has progestogenic and androgenic activity. Due to its progestogenic activity, a separate progestogen is not added for endometrial protection. Tibolone was approved by Health Canada in 2019 for the short-term treatment of vasomotor symptoms in postmenopausal women.

Tibolone carries the same contraindications and precautions as other estrogen hormone therapies. A Cochrane systematic review found that tibolone was more effective than placebo for reducing vasomotor symptoms but less effective than estrogen plus a progestogen. There was a lower rate of unscheduled bleeding with tibolone compared to estrogen plus a progestogen.

The dosage of tibolone is 2.5 mg orally once per day. Current annual cost is approximately $1,300 (excluding markup and professional fees) and it is not a BC PharmaCare benefit.

Effects on other health outcomes^6-9

Safety concerns identified by Health Canada during their review of tibolone include increased risks of endometrial cancer, breast cancer and stroke when compared to placebo. In addition to examining tibolone’s efficacy for vasomotor symptoms, Health Canada’s review refers to two long term clinical trials.

Both trials were stopped early (Table).

• LIFT due to an increased risk of stroke
• LIBERATE due to futility

This means there was little chance of the trial achieving its objectives. Tibolone has not been compared to estrogen plus progestogen in a long-term clinical trial.

Trial	Participants	Trial objective	Trial outcome
LIFT 2008	4,538 postmenopausal women ages 60-85 with osteoporosis (mean age 68)	To assess whether tibolone reduces the risk of radiographic vertebral fractures compared to placebo	Tibolone reduced the risk of radiographic fractures (HR 0.55, 95%CI 0.41 to 0.74) but increased the risk of stroke (HR 2.19, 95%CI 1.14 to 4.23) The trial was stopped early after a median follow up of 2.8 years due to the increased stroke risk
LIBERATE 2009	3,148 postmenopausal women aged < 75 with vasomotor symptoms and a history of breast cancer (mean age 53)	To assess wither tibolone reduces the risk of breast cancer recurrence compared to placebo	Tibolone increased the risk of breast cancer recurrence (HR 1.40, 95%CI 1.14 to 1.70) The trial was stopped early after a median follow up of 3.1 years due to futility

Publicly accessible drug reviews by the US Food and Drug Administration (US FDA) have historically been more comprehensive than those provided by Health Canada but in 2006 tibolone was considered “not approvable” by the US FDA, so a detailed review is not available.

Health Canada reports weighing their decision to approve tibolone on the clinical experience and observational evidence from its use in other countries. They do advise that the “decision to use Tibella should be based on assessment of the patient’s overall risks, including risk of stroke, particularly in patients over 60 years of age”. The short-term use indication is not strictly defined but Health Canada recommends reviewing the need for continued treatment after 6 months.

---

¹BC PAD Service Medications for Menopause-Associated Vasomotor and Genitourinary Symptoms (May 2025); ²Health Canada Drug Product Database Tibella (tibolone); ³McKesson Canada (accessed January 30, 2026); ⁴BC PharmaCare Formulary Search; ⁵Formoso Cochrane Database Syst Rev 2016 (PMID:27733017); ⁶Health Canada Summary Basis of Decision for Tibella; ⁷LIFT NEJM 2008 (PMID:18703472); ⁸LIBERATE 2009 Lancet Oncol (PMID:19167925); ⁹Akzo Nobel Press Release 2006 FDA says tibolone not approvable as menopause treatment in the US