Drug intelligence / Profile preview

Estradiol dienanthate

Development stage
Discontinued
Modality
Small Molecules
Administration
Intramuscular Injection
01

Overview

Estradiol dienanthate is a long-acting synthetic ester of estradiol, functioning as a prodrug that is hydrolyzed in the body to release active estradiol. It acts as an agonist of the estrogen receptor, exerting estrogenic effects. Historically, it was used in menopausal hormone therapy to alleviate symptoms such as hot flashes, vaginal dryness, and mood changes, and also for contraception (as a component of combination drugs) and lactation suppression. It was typically administered via intramuscular injection. First described in 1959, it was available in Canada and Germany but was discontinued by 2005 and is no longer available in any form.

Brand names
ClimacteronAmenoseLactimexLactostat
Other names
Estradiol diheptanoateEstra-1,3,5(10)-triene-3,17β-diol diheptanoate
02

Targets

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

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