Drug intelligence / Profile preview

oestradiol

Development stage
Approved
Lead developer
Viatris
Modality
Small Molecules
Administration
Oral, Transdermal, Topical, Vaginal, Intramuscular
01

Overview

Oestradiol is a naturally occurring steroid hormone and the primary, most potent form of estrogen in humans. It is used as a pharmaceutical agent to treat symptoms associated with menopause (such as hot flashes, night sweats, vaginal dryness), prevent postmenopausal osteoporosis, manage hypoestrogenism due to hypogonadism or ovarian failure, and for palliative treatment of certain breast and prostate cancers. Oestradiol acts primarily by binding to and activating estrogen receptors throughout the body—most notably in reproductive tissues, bone, brain, liver, and cardiovascular system—modulating gene expression that regulates growth and function of these tissues. In cancer therapy (breast/prostate), it exerts anti-androgenic effects by suppressing gonadotropin secretion[1][2][5][7].

Brand names
EstraceVivelle-DotVivelleDelestrogenDepo-EstradiolClimaraDivigelElestrinEsclimEstradermEstrasorbEstringEstroGelEvamistFemringFemtraceMenostarMinivelleVagifem
Other names
estradiol (USAN, INN)oestradiolum (Ph. Helv.)beta-Estradioldihydrofollicular hormonedihydrofolliculindihydrotheelindihydroxyestrinprofoliol
02

Targets

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

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