Drug intelligence / Profile preview

estrogens + diethylstilbestrol

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral, Vaginal, Topical, Injection
01

Overview

A combination drug consisting of **estrogens** (natural or synthetic) and **diethylstilbestrol** (DES), a synthetic nonsteroidal estrogen. Diethylstilbestrol acts as a potent agonist of estrogen receptors (notably ERα and ERβ), and the combination with other estrogens produces pronounced estrogenic effects. Both components act through estrogen receptors to modulate gene expression and hormonal feedback mechanisms. Historically, combinations of estrogens and diethylstilstilbestrol were used for menopausal hormone therapy, treatment of estrogen deficiency, and other gynecological indications. However, DES is no longer used in clinical practice due to significant safety concerns, including increased carcinogenic risk and adverse reproductive outcomes[1][2][3][6]. The combination amplifies the hormonal actions and risks associated with estrogen therapy.

02

Targets

ESRRG (Estrogen-related receptor gamma)ESRRB (Estrogen-related receptor beta)ESR2 (ERβ)ESR1 (ERα)ESRRA (Estrogen-related receptor alpha)

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