5630-53-5

Description

Tibolone is a synthetic steroid with weak progestational and estrogenic properties, reportedly useful in controlling symptoms resulting from natural or surgical menopause. It has thus far shown no significant antithrombotic effect in post-menopausal patients.

Chemical Properties

White Solid

Originator

Akzo (Organon) (The Netherklands)

Uses

A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome

Definition

ChEBI: Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormon receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.

Brand name

Livial

Pharmacokinetics

Raloxifene is rapidly absorbed following oral administration, with an estimated 60% absorption, but it has a very low bioavailability (2%), associated with extensive phase II metabolism. The metabolites are excreted via the bile, with potential enterohepatic recycling that could account for the interaction with cholestyramine. Supportive of the enterohepatic recycling is the half-life of 28 hours. Metabolism of raloxifene occurs to a great extent in the intestine and consists of glucuronide conjugation catalyzed by uridine diphosphate glucuronosyltransferase (UGT).

Clinical Use

Tibolone is a synthetic steroid that has been shown to increase bone mineral density similar to alendronate. The U.S. FDA approval is pending; overseas, this agent is used for the treatment of menopausal symptoms as well as the prevention of osteoporosis. It is considered to be a viable alternative to conjugated equine estrogen plus micronized progesterone.

Side effects

The most common reason for patient withdrawal from clinical trials was vaginal bleeding (also a common side effect when estrogen therapy is used).