Drug intelligence / Profile preview

ethinyl estradiol

Development stage
Approved
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Ethinyl estradiol is a synthetic estrogen widely used as the estrogenic component in combined oral contraceptives and other hormonal therapies. It acts as an agonist of the estrogen receptor, mimicking the effects of natural estrogens like estradiol but with greater oral bioavailability and metabolic stability. Its primary mechanism is suppression of gonadotropins (luteinizing hormone and follicle-stimulating hormone), leading to inhibition of ovulation. Additional contraceptive effects include thickening cervical mucus to impede sperm penetration and altering endometrial lining to prevent implantation. Ethinyl estradiol has also been used in treating menopausal symptoms, gynecological disorders, certain hormone-sensitive cancers, acne, and moderate-to-severe vasomotor symptoms[1][7][9]. It was developed in the 1930s and introduced for medical use in 1943[1].

Brand names
Numerous
Other names
EthynylestradiolEthinyl oestradiol17α-Ethynylestradiol17α-Ethynylestra-1,3,5(10)-triene-3,17β-diol
02

Targets

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

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