Drug intelligence / Profile preview

estrone-3-sulfate

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Transdermal, Vaginal, Injection
01

Overview

**Estrone-3-sulfate** is a naturally occurring estrogenic steroid and the sulfate ester of estrone. It is both a metabolite and circulating reservoir form of estrogens in humans, acting mainly as a prodrug that is converted via steroid sulfatase into active estrone and, subsequently, to estradiol. Pharmacodynamically, estrone-3-sulfate acts as a **prodrug of estradiol and estrone**, which are potent agonists of the estrogen receptor. The drug is mainly used in menopausal hormone therapy and can be administered alone (as estropipate) or as a component of conjugated or esterified estrogens for indications such as menopausal symptom management, treatment of some forms of infertility, underdeveloped female sexual characteristics, atrophic vaginitis, certain breast cancers (in men and postmenopausal women), prostate cancer, and osteoporosis prevention. It can be administered orally, and in some combination products via transdermal, vaginal, and injectable routes[1][3].

Brand names
estropipateOgen
Other names
sodium estrone sulfateestrone 3-sulfateestrone3-sulfateestrone-3-sulfateestrone, hydrogen sulfate
02

Targets

ESR2 (ERβ)KCNH2 (Voltage-gated potassium channel subfamily H member 2)ESR1 (ERα)

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