Drug intelligence / Profile preview

estradiol + levonorgestrel (Bayer, 66345b)

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

Overview

Nuvelle is a cyclical combined hormone replacement therapy (HRT) product containing two active ingredients: estradiol (2 mg) and levonorgestrel (75 mcg). It is administered on a cyclical basis, typically involving 16 days of estradiol alone followed by 16 days of combined estradiol and levonorgestrel. Estradiol, a natural estrogen, acts as an agonist at estrogen receptors to alleviate symptoms of estrogen deficiency and prevent bone loss. Levonorgestrel, a synthetic progestogen, acts as an agonist at progesterone receptors to protect the endometrium from estrogen-induced hyperplasia. Nuvelle has been specifically studied in women with premature ovarian failure (POF) to address bone mineral density loss and sexual dysfunction, demonstrating superior improvement in lumbar spine bone mineral density compared to combined oral contraceptive pills in clinical trials conducted at King's College London.

Brand names
Nuvelle
Other names
oestradiol + levonorgestrel
02

Targets

AR (Adrenergic receptors)ESR1 (ERα)ESR2 (ERβ)GR (Glucocorticoid receptor)MR (Mineralocorticoid receptor)PR-A (Progesterone Receptor A)RB1 (Retinoblastoma-associated Protein)PR (Progesterone receptor)

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