Drug intelligence / Profile preview

estradiol acetate + levonorgestrel

Development stage
Phase 4
Modality
Small Molecules
Administration
Oral
01

Overview

**Estradiol acetate + levonorgestrel** is a combination hormone replacement therapy (HRT) consisting of estradiol acetate, a short-acting ester of the natural estrogen estradiol, and levonorgestrel, a synthetic progestin. It is primarily indicated for the treatment of moderate to severe vasomotor symptoms (hot flashes) associated with menopause and for the prevention of postmenopausal osteoporosis in women at significant risk who cannot use other osteoporosis therapies. The estrogen component alleviates menopausal symptoms by mimicking endogenous estradiol, while levonorgestrel opposes estrogen-induced endometrial proliferation to reduce the risk of endometrial hyperplasia and carcinoma. Available as low-dose oral tablets (e.g., 0.5 mg/0.25 mg or 1 mg/0.5 mg), it is typically dosed continuously or cyclically.

Brand names
FemhrtFemplusSklice
Other names
estradiol acetate/levonorgestrelestradiol 17-acetate + levonorgestrel
02

Targets

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

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