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estradiol + levonorgestrel (Bayer, f5a2d0)
- Development stage
- Unknown
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Transdermal
01
Overview
Estradiol + levonorgestrel is a combination hormone replacement therapy (HRT) indicated for the treatment of moderate to severe vasomotor symptoms associated with menopause and the prevention of postmenopausal osteoporosis in women with an intact uterus. The product is typically formulated as a transdermal patch (e.g., Climara Pro) that provides continuous delivery of both hormones. Estradiol, a naturally occurring human estrogen, binds to and activates estrogen receptors to supplement declining endogenous estrogen levels, thereby alleviating menopausal symptoms and maintaining bone mineral density. Levonorgestrel, a synthetic progestin, acts as an agonist at progesterone receptors to protect the endometrium from the stimulatory effects of estrogen, significantly reducing the risk of endometrial hyperplasia and carcinoma that can occur with estrogen-only therapy in women with a uterus.
- Brand names
- Climara Pro
- Other names
- levonorgestrel + estradiolestradiol/levonorgestrelestradiol/levonorgestrel transdermal system
02
Targets
ESR1 (ERα)ESR2 (ERβ)PR-A (Progesterone Receptor A)RB1 (Retinoblastoma-associated Protein)PR (Progesterone receptor)
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