Drug intelligence / Profile preview

ethynodiol diacetate

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Ethynodiol diacetate is a synthetic progestin used primarily as an active ingredient in oral contraceptives. It acts as a prodrug, rapidly converted in the body to norethisterone, which exerts its contraceptive effects by binding to progesterone and estrogen receptors in target tissues such as the female reproductive tract, mammary gland, hypothalamus, and pituitary. This action suppresses ovulation by inhibiting gonadotropin-releasing hormone (GnRH) release from the hypothalamus and blunting the preovulatory luteinizing hormone (LH) surge. Ethynodiol diacetate also has weak androgenic and some estrogenic activity. It was first synthesized in 1954 and introduced for medical use in 1965[2][5]. The drug's primary indication is contraception. Ethynodiol diacetate is most commonly used in combination with ethinyl estradiol for oral contraception; it is marketed under various brand names worldwide but only available in a few countries today[5].

Brand names
ConovaContinuinDemulenFemulenKelnorLo-MalmoredeLuteonormLuto-MetrodiolMalmoredeMetrodiolOvulenSolunaZovia
Other names
etynodiol diacetate
02

Targets

PR (Progesterone receptor)ER (Estrogen receptor)

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