Drug intelligence / Profile preview

estradiol acetate

Development stage
Approved
Lead developer
Warner Chilcott
Modality
Small Molecules
Administration
Oral, Vaginal
01

Overview

Estradiol acetate is a synthetic estrogen and pro-drug ester of estradiol, the primary endogenous female sex hormone. It is used primarily in hormone therapy for women to treat symptoms associated with menopause, such as vasomotor symptoms (hot flashes) and moderate to severe vulvar and vaginal atrophy. After administration, estradiol acetate is rapidly hydrolyzed in vivo to active estradiol. Estradiol acts by binding to estrogen receptors (ERα and ERβ) located throughout various tissues including the breasts, uterus, ovaries, skin, bone, fat tissue, brain, prostate gland (in men), hypothalamus and pituitary gland. Upon receptor binding and activation in target cells, it regulates gene transcription leading to increased synthesis of specific proteins that mediate its physiological effects. These include maintenance of the female reproductive system and secondary sexual characteristics as well as modulation of hepatic protein synthesis (e.g., sex hormone-binding globulin). Estradiol suppresses follicle-stimulating hormone from the anterior pituitary via negative feedback[1][2][3][6].

Brand names
FemtraceFemringMenoring
Other names
EA
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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