Drug intelligence / Profile preview

Gestrinone

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral, Intravaginal
01

Overview

Gestrinone is a synthetic steroidal hormone of the 19-norsteroid class, developed primarily for the treatment of endometriosis. It exhibits mixed progestogenic and antiprogestogenic (partial agonist) activity at the progesterone receptor, weak androgenic activity at the androgen receptor, and significant anti-estrogenic effects. Its mechanism involves suppression of pituitary gonadotropin release (LH and FSH), leading to inhibition of ovarian steroidogenesis and endometrial atrophy. Gestrinone also binds to estrogen receptors with functional antiestrogenic action in target tissues such as the endometrium. The drug has been approved for use in several countries outside the United States, including Latin America, Australia, and Europe[1][2][3][4][5][6]. It is used mainly for mild to moderate endometriosis with or without associated infertility[5].

Brand names
DimetroseNemestranDimetriose
Other names
EthylnorgestrienoneGestrinonaGestrinonum
02

Targets

ER (Estrogen receptor)AR (Adrenergic receptors)PR (Progesterone receptor)

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