Drug intelligence / Profile preview

dienogest + estradiol valerate

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Dienogest + estradiol valerate is a continuous combined hormone replacement therapy (HRT) indicated for the treatment of estrogen deficiency symptoms in postmenopausal women and the prevention of osteoporosis. It combines estradiol valerate, a synthetic ester of the natural estrogen 17β-estradiol, with dienogest, a fourth-generation progestin. Estradiol valerate acts as an estrogen receptor agonist to replace declining endogenous estrogen levels, alleviating vasomotor symptoms and vaginal atrophy. Dienogest acts as a selective progesterone receptor agonist to provide endometrial protection against estrogen-induced hyperplasia. Notably, dienogest is characterized by potent endometrial effects and significant anti-androgenic activity, while lacking significant androgenic, mineralocorticoid, or glucocorticoid properties. This specific combination has been the subject of extensive clinical research at the Karolinska Institutet, particularly regarding its impact on mammographic breast density and breast cell proliferation compared to other HRT regimens.

Brand names
LafammeClimodienQlairaNatazia
Other names
estradiol valerate + dienogest
02

Targets

PR (Progesterone receptor)ESR2 (ERβ)AR (Adrenergic receptors)ESR1 (ERα)

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