Drug intelligence / Profile preview

tibolone

Development stage
Phase 4
Lead developer
Organon
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tibolone is a synthetic steroid hormone used primarily for menopausal hormone therapy, the prevention of postmenopausal osteoporosis, and the treatment of endometriosis. It is taken orally and acts as a tissue-selective estrogen activity regulator. Tibolone itself is pharmacologically inactive but is rapidly converted in the body to three active metabolites with estrogenic (3α-hydroxytibolone, 3β-hydroxytibolone), progestogenic, and androgenic (delta-4-tibolone) properties. These metabolites exert tissue-specific effects by acting as agonists at estrogen receptors (mainly in bone and vaginal tissues), progesterone receptors (preventing endometrial hyperplasia), and androgen receptors (affecting libido, mood, brain, and liver). Unlike traditional estrogens used in menopausal therapy, tibolone does not stimulate endometrial or breast tissue significantly. Its main indications are relief of vasomotor symptoms such as hot flashes and prevention of bone loss after menopause[1][2][3][4][5].

Brand names
Livial
02

Targets

PR (Progesterone receptor)AR (Adrenergic receptors)ESR1 (ERα)

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