promegestone

Promegestone is a synthetic progestin (progestogen) medication used primarily in menopausal hormone therapy and for the treatment of gynecological disorders. It is administered orally. Promegestone acts as an agonist of the progesterone receptor with high affinity and is not metabolized by 20α-hydroxysteroid dehydrogenase, which allows it to sustain progesterone receptor signaling. It has weak antiandrogenic, glucocorticoid, and antimineralocorticoid activity but no significant other hormonal effects. The drug functions largely as a prodrug for trimegestone. In addition to its clinical use in several countries (notably France), it has been widely utilized in scientific research as a radioligand for the progesterone receptor[1][6]. Mechanistically, it can also act as a noncompetitive antagonist at nicotinic acetylcholine receptors at higher concentrations[5].

Brand names

Surgestone

Other names

17α,21-Dimethyl-δ9-19-norprogesterone17α,21-Dimethyl-19-norpregna-4,9-diene-3,20-dionepromegestona