Drug intelligence / Profile preview

estradiol + norgestimate

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

Overview

estradiol + norgestimate is a fixed-dose combination of two hormones: **estradiol** (a naturally occurring estrogen) and **norgestimate** (a synthetic progestin), used primarily in menopausal hormone therapy. This combination is marketed under the brand name Prefest and is used to treat symptoms associated with menopause, such as hot flashes and vaginal dryness. - **Mechanism of action:** Estradiol acts as an agonist at estrogen receptors, exerting estrogenic effects on tissues, while norgestimate acts as an agonist at the progesterone receptor, counterbalancing the effects of estrogen on the endometrium and thus reducing the risk of endometrial hyperplasia associated with estrogen therapy. The combination provides both estrogenic and progestogenic activity for hormone replacement in postmenopausal women[1][9]. - **Primary indication:** Management of moderate to severe vasomotor symptoms associated with menopause and prevention of postmenopausal osteoporosis where other treatments are unsuitable[1][9]. - **Other indications:** Not indicated for birth control (that combination uses ethinyl estradiol, not estradiol)[1][9]. - **Developer/manufacturer:** Marketed by companies such as Pfizer and Teva, among others.

Brand names
PrefestOrtho-Prefest
Other names
estradiol/norgestimate systemic
02

Targets

PR (Progesterone receptor)ESR2 (ERβ)AR (Adrenergic receptors)ESR1 (ERα)

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