Drug intelligence / Profile preview

ethinylestradiol + dienogest

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

Overview

Ethinylestradiol + dienogest is a combined oral contraceptive (COC) consisting of the synthetic estrogen ethinylestradiol and the fourth-generation progestin dienogest. Dienogest is unique among progestins for its potent progestogenic effect on the endometrium and its significant anti-androgenic activity, while lacking glucocorticoid or mineralocorticoid activity. In clinical practice, this combination is primarily used for contraception and the treatment of acne or heavy menstrual bleeding. In the context of infertility associated with endometriosis, it is utilized as a pre-treatment prior to Assisted Reproductive Technology (ART) to downregulate the hormonal environment and suppress endometriotic lesions, aiming to improve clinical pregnancy rates. The combination works by inhibiting the secretion of gonadotropins (FSH and LH), thereby suppressing ovulation and creating a stable endometrial environment.

Brand names
ValetteJeanineAristelleDienobelSibillaMaxim
Other names
ethinylestradiol/dienogestEE/DNG
02

Targets

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

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