Drug intelligence / Profile preview

estradiol valerate + dienogest

Development stage
Phase 4
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

**Estradiol valerate + dienogest** is an oral fixed-dose estrogen-progestogen combination used in multiple product-specific regimens. Estradiol valerate is a prodrug of 17β-estradiol that activates estrogen receptors, while dienogest is a synthetic progestogen that activates the progesterone receptor and has antiandrogenic activity. Four-phasic 28-day products such as Natazia, Qlaira, and Klaira provide contraception through suppression of ovulation and endometrial effects and are also used for heavy menstrual bleeding in women choosing oral contraception. Continuous formulations such as Climodien, Klimodien, and Lafamme have been used as menopausal hormone therapy in postmenopausal women with an intact uterus. ([accessdata.fda.gov](https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/022252s009lbl.pdf))

Brand names
ClimodienKlairaKlimodienLafammeNataziaQlaira
Other names
dienogest + estradiol valeratedienogest/estradiol valerateE2V/DNGestradiol valerate + dienogestestradiol valerate and dienogestestradiol valerate/dienogestEV/DNG
02

Targets

PR (Progesterone receptor)AR (Adrenergic receptors)ER (Estrogen receptor)

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