Drug intelligence / Profile preview

estradiol cypionate

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intramuscular, Subcutaneous
01

Overview

Estradiol cypionate is a synthetic estrogen and prodrug of estradiol used primarily in hormone replacement therapy for menopausal symptoms such as hot flashes and vaginal dryness and for the treatment of hypoestrogenism due to hypogonadism. It is administered as an intramuscular or subcutaneous depot injection. After administration, the ester group is cleaved to release active endogenous estradiol (17β‑estradiol). Estradiol exerts its effects by binding to estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) in various tissues including breast, uterus, bone, brain and others. This leads to modulation of gene transcription with downstream effects such as relief of vasomotor symptoms and maintenance of bone density. Estradiol cypionate has a longer duration of action compared to other injectable esters due to its increased lipophilicity[1][2][6].

Brand names
Depo-Estradiol
Other names
estradiol 17-cyclopentanepropionateestradiol17-cyclopentanepropionateestradiol-17-cyclopentanepropionate(17β)-estra-1,3,5(10)-triene-3,17-diol 17β-cyclopentanepropanoatecyclopentanepropionic acid, 3-hydroxyestra-1,3,5(10)-trien-17β-yl esterestra-1,3,5(10)-triene-3,17-diol (17β), 17-cyclopentanepropanoate
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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