Drug intelligence / Profile preview

estriol

Development stage
Phase 4
Lead developer
Transo-Pharm Handels
Modality
Small Molecules
Administration
Oral, Vaginal, Topical
01

Overview

Estriol is a naturally occurring steroid hormone and one of the three major endogenous estrogens in humans (alongside estradiol and estrone). It is considered the weakest estrogen. Estriol is primarily produced in significant amounts during pregnancy by the placenta; its levels are otherwise low in non-pregnant women and men. As a medication, estriol is used mainly for hormone therapy to treat symptoms of estrogen deficiency such as vaginal dryness (atrophic vaginitis), vulvar itching or burning, urinary symptoms related to urogenital atrophy (e.g., frequency or mild incontinence), and menopausal symptoms. It can also be used preoperatively or postoperatively for vaginal surgery in postmenopausal women. Estriol acts as an agonist at estrogen receptors but has weaker activity compared to other estrogens due to its rapid metabolism and short retention time within target tissues[1][2][5][6]. In clinical use it may help restore normal vaginal flora and pH by promoting maturation of the vaginal epithelium[3]. Estriol can be administered orally or topically (vaginal cream/tablet)[4].

Brand names
OvestinHolinTheelolOrestin
Other names
oestriol16α-hydroxyestradiolestra-1,3,5(10)-triene-3,16α,17β-triol1,3,5(10)-Estratriene-3,16α,17β-triolTrihydroxyestrinÖstriol
02

Targets

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

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