Drug intelligence / Profile preview

estradiol + drospirenone

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

Overview

**Estradiol + drospirenone** is a continuous oral fixed-dose menopausal hormone-therapy combination comprising 17β-estradiol, an estrogen, and drospirenone, a synthetic progestin with antimineralocorticoid and antiandrogenic pharmacology. Estradiol replaces diminished estrogen activity after menopause, while drospirenone provides progestogenic endometrial protection in women with an intact uterus and has antialdosterone activity. The Bayer product **Angeliq** is approved in the United States for moderate-to-severe menopausal vasomotor symptoms and moderate-to-severe vulvar and vaginal atrophy symptoms in women with a uterus; marketed strengths include drospirenone 0.25 mg plus estradiol 0.5 mg and drospirenone 0.5 mg plus estradiol 1 mg tablets. ([dailymed.nlm.nih.gov](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=761834c2-6b61-4583-84c2-f1ca4a97c4f2))\n\nOutside the United States, products containing estradiol 1 mg plus drospirenone 2 mg have also been marketed for climacteric symptoms, atrophic urogenital conditions, and reduction of postmenopausal osteoporosis risk in women with an intact uterus. ([bayer.com](https://www.bayer.com/sites/default/files/angeliq-en-pi.pdf))

Brand names
AltesseAllureneAngeliqAngeliq MicroAngeminClinomatClobotil
Other names
17β-estradiol + drospirenonedrospirenone + estradioldrospirenone and estradioldrospirenone/estradiolE2/DRSPestradiol + drospirenoneestradiol/drospirenone
02

Targets

PR (Progesterone receptor)AR (Adrenergic receptors)ESR1 (ERα)MR (Mineralocorticoid receptor)

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