Drug intelligence / Profile preview

estradiol valerate + ethinylestradiol

Development stage
Preclinical
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Intramuscular Injection
01

Overview

Estradiol valerate + ethinylestradiol is a combination drug consisting of two synthetic estrogens. Estradiol valerate is an esterified form of estradiol, a natural estrogen, while ethinylestradiol is a potent synthetic estrogen commonly used in oral contraceptives. This combination may be formulated for hormonal therapy or contraception, though it is not a standard or widely marketed fixed-dose product; most commonly, estradiol valerate is combined with progestins (such as norethisterone enantate) for injectable contraception[1]. Both components act primarily by binding to and activating the estrogen receptor, leading to suppression of ovulation via negative feedback on the hypothalamic-pituitary-gonadal axis and modulation of endometrial growth and cervical mucus properties. Ethinylestradiol has higher oral bioavailability than natural estrogens due to its resistance to hepatic metabolism[8]. The primary indications for these agents individually include hormone replacement therapy (estradiol valerate) and contraception (ethinylestradiol), but their use together as a fixed combination appears rare.

Other names
戊酸雌二醇 + 炔雌醇
02

Targets

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

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