Drug intelligence / Profile preview

gestodene

Development stage
Phase 4
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Transdermal
01

Overview

Gestodene is a potent, third-generation synthetic progestogen belonging to the 19-nortestosterone family. It is primarily used in combined oral contraceptive pills and menopausal hormone therapy to provide effective cycle control and ovulation suppression. Mechanistically, gestodene acts as a high-affinity agonist of the progesterone receptor, which inhibits the secretion of gonadotropins (luteinizing hormone and follicle-stimulating hormone) from the pituitary gland, thereby preventing ovulation and altering cervical mucus consistency. In addition to its progestogenic effects, gestodene exhibits significant antimineralocorticoid activity, which can mitigate estrogen-related water retention, and possesses weak androgenic properties. Developed by Schering AG (now Bayer), it is characterized by its high oral bioavailability and potency, allowing for lower therapeutic doses compared to first- and second-generation progestins.

Brand names
FemodeneMinuletMinesseGyneraMelianeTriadeneTri-Minulet
Other names
15-dehydronorgestrel17alpha-ethynyl-13-ethyl-17beta-hydroxy-4,15-gonadien-3-one13-ethyl-17-hydroxy-18,19-dinorpregna-4,15-dien-20-yn-3-one
02

Targets

AR (Adrenergic receptors)GR (Glucocorticoid receptor)MR (Mineralocorticoid receptor)PR (Progesterone receptor)SHBG (Sex hormone-binding globulin)

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