Drug intelligence / Profile preview

ethinylestradiol + desogestrel

Development stage
Phase 4
Lead developer
Organon
Modality
Small Molecules
Administration
Oral
01

Overview

Ethinylestradiol + desogestrel is a combined oral contraceptive (COC) consisting of a synthetic estrogen and a third-generation progestin. Ethinylestradiol acts as an agonist at estrogen receptors, suppressing the release of follicle-stimulating hormone (FSH), while desogestrel (via its active metabolite etonogestrel) acts on progesterone receptors to inhibit the luteinizing hormone (LH) surge, thereby preventing ovulation. In clinical research sponsored by Bayer (such as trial NCT00413062), this combination was utilized in a traditional 21/7 regimen (21 days of active hormones followed by a 7-day hormone-free interval) as an active comparator to evaluate the efficacy of a 24/4 ethinylestradiol/drospirenone regimen (YAZ) in mitigating hormone withdrawal-associated symptoms. These symptoms, which include headaches, pelvic pain, and breast tenderness, frequently occur during the pill-free interval of standard contraceptive cycles due to the abrupt decline in exogenous hormone levels.

Brand names
MercilonKimidess
Other names
Ethinylestradiol/Desogestrel (21/7 regimen)
02

Targets

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

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