Drug intelligence / Profile preview

ethinyl estradiol + gestodene

Development stage
Phase 3
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Ethinyl estradiol + gestodene is a combined oral contraceptive containing two active ingredients: ethinyl estradiol (a synthetic estrogen) and gestodene (a third-generation synthetic progestogen/progestin). This combination is used primarily to prevent pregnancy. The mechanism of action involves suppression of ovulation through inhibition of gonadotropins (luteinizing hormone and follicle-stimulating hormone), thickening of cervical mucus to impede sperm penetration, and alteration of the endometrial lining to reduce the likelihood of implantation. Gestodene has high bioavailability and acts directly as a progestogen without requiring metabolic activation. The combination is available in monophasic or triphasic formulations with varying doses per tablet[6][5][7].

Brand names
FemodeneGyneraHarmonetLindynetteLogestMelianeMinesseMinuletMirelle
Other names
ethinylestradiol/gestodene
02

Targets

PR (Progesterone receptor)ESR2 (ERβ)GPER1 (G protein-coupled estrogen receptor 1)ESR1 (ERα)

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