Drug intelligence / Profile preview

estradienolone

Development stage
Preclinical
Lead developer
McGill University
Modality
Small Molecules
Administration
Parenteral
01

Overview

Estradienolone (also referred to as estradiol dienolone) is a novel endogenous 19-nor steroid hormone identified in pregnant women. It is an isomer of estradiol that acts as a natural inverse agonist of the estrogen-related receptors alpha (ERRα) and gamma (ERRγ), directly interacting with these receptors to inhibit their transcriptional activity. Estradienolone has demonstrated strong anti-mitogenic properties, inhibiting the growth of both estrogen receptor-positive and estrogen receptor-negative breast cancer cells in a dose-dependent manner while showing minimal effect on normal epithelial breast cells. It also binds with high affinity to the progesterone receptor and sex hormone-binding globulin (SHBG). The compound is being investigated by researchers at McGill University and the University of Montreal as a potential therapeutic strategy for breast cancer.

Other names
17β-hydroxy-1,5-estradiene-3-one17β-hydroxy-19-nor-androsta-1,5-dien-3-oneestradiol dienoloneestradienolone
02

Targets

SHBG (Sex hormone-binding globulin)PR (Progesterone receptor)ESRRA (Estrogen-related receptor alpha)ESRRG (Estrogen-related receptor gamma)

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