Drug intelligence / Profile preview

estradiol valerate

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

Overview

Estradiol valerate is a synthetic estrogen and prodrug of estradiol, the primary female sex hormone. It is an esterified form of estradiol that, once administered (typically by intramuscular injection), is rapidly hydrolyzed in the body to release active estradiol. Estradiol acts as an agonist at estrogen receptor (ERα and ERβ) in various tissues, mediating typical estrogenic effects such as regulation of reproductive function and secondary sexual characteristics. Estradiol valerate is used for hormone replacement therapy to treat moderate-to-severe vasomotor symptoms (hot flashes), vulvar and vaginal atrophy due to menopause, hypoestrogenism from hypogonadism or ovarian failure, palliative treatment of advanced androgen-dependent prostate cancer, and in combination with other agents for contraception or management of heavy menstrual bleeding[1][2][3][4][5][6][8].

Brand names
DelestrogenNatazia
Other names
estradiol 17-valerateestradiol17-valerateestradiol-17-valerateoestradiol valerate
02

Targets

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

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