Drug intelligence / Profile preview

dienestrol

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Rectal, Vaginal
01

Overview

Dienestrol is a synthetic nonsteroidal estrogen of the stilbestrol group. It acts as an estrogen receptor agonist and is used primarily to treat atrophic vaginitis and kraurosis vulvae in women. Mechanistically similar to other estrogens such as diethylstilbestrol (DES), dienestrol binds to estrogen receptors in target tissues—including the female reproductive tract—leading to increased gene transcription and protein synthesis associated with estrogenic effects. It was introduced in the United States by Schering as Synestrol in 1947 and has been marketed under various brand names worldwide. In addition to its primary indications for menopausal symptoms (such as vaginal dryness or inflammation), it has also been studied for use by rectal administration in prostate cancer treatment for men[1][7].

Brand names
Ortho DienestrolDienoestrolDienoestrol OrthoSexadienCycladieneDenestrolinDienolDinovexFollormonOestrodieneSynestrol
Other names
dienoestrolp-[(E,E)-1-Ethylidene-2-(p-hydroxyphenyl)-2-butenyl]phenol3,4-Di(para-hydroxyphenyl)-2,4-hexadiene
02

Targets

ESR1 (ERα)ESR2 (ERβ)

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