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Add back therapy 1 (tibolone)

University of Cagliari · FDA-approved active Small molecule

Tibolone is a synthetic steroid that acts as a selective tissue estrogenic activity regulator (STEAR), providing estrogenic, progestagenic, and androgenic effects to alleviate menopausal symptoms.

Tibolone is a synthetic steroid that acts as a selective tissue estrogenic activity regulator (STEAR), providing estrogenic, progestagenic, and androgenic effects to alleviate menopausal symptoms. Used for Menopausal vasomotor symptoms (hot flushes, night sweats), Postmenopausal bone loss prevention, Postmenopausal vaginal atrophy.

At a glance

Generic nameAdd back therapy 1 (tibolone)
SponsorUniversity of Cagliari
Drug classSelective Tissue Estrogenic Activity Regulator (STEAR); Hormone Replacement Therapy
TargetEstrogen receptor, Progesterone receptor, Androgen receptor
ModalitySmall molecule
Therapeutic areaEndocrinology; Women's Health
PhaseFDA-approved

Mechanism of action

Tibolone is a prodrug that is metabolized in the body to three active metabolites with different tissue-selective activities. It binds to estrogen, progesterone, and androgen receptors with varying affinities depending on the tissue, providing symptom relief in menopause while minimizing some adverse effects associated with conventional hormone replacement therapy. This selective activity profile makes it particularly useful for managing vasomotor symptoms and bone loss in postmenopausal women.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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