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Estrone

Development stage
Phase 2
Modality
Small Molecules
Administration
Intramuscular, Vaginal, Oral
01

Overview

Estrone is a naturally occurring steroidal estrogen and one of the three main endogenous estrogens in humans. It is considered the weakest of the major estrogens and is primarily produced in the ovaries, placenta, and peripheral tissues such as adipose tissue through conversion from androstenedione. Estrone acts as an agonist at estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) but with much lower potency than estradiol—its estrogenic activity is about 4–10% that of estradiol. In clinical use, estrone serves mainly as hormone therapy for perimenopausal and postmenopausal symptoms such as vasomotor disturbances (hot flashes), atrophic vaginitis, vulvar atrophy, and prevention of osteoporosis due to estrogen deficiency. It can also be used to treat vaginal irritation or dryness caused by low estrogen levels[2][3][4][7]. Most or all of its biological effects are thought to result from its conversion into estradiol in vivo; thus it functions largely as a prodrug for estradiol[4].

Brand names
EstragynKestrinTheelin
Other names
E1E-1E 1
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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