Drug intelligence / Profile preview

17-beta-estradiol + medroxyprogesterone acetate

Development stage
Unknown
Lead developer
Orion
Modality
Small Molecules
Administration
Oral, Transdermal
01

Overview

This drug is a fixed-dose combination of 17-beta-estradiol, a natural estrogen, and medroxyprogesterone acetate, a synthetic progestin. It is primarily used as part of menopausal hormone therapy (MHT) in postmenopausal women with an intact uterus to treat moderate to severe vasomotor symptoms (such as hot flashes), vulvar and vaginal atrophy, and to prevent postmenopausal osteoporosis. The addition of the progestin component (medroxyprogesterone acetate) counteracts the risk of endometrial hyperplasia and cancer associated with unopposed estrogen therapy. Mechanistically, 17-beta-estradiol acts as an agonist at estrogen receptors throughout the body, while medroxyprogesterone acetate acts as an agonist at progesterone receptors. This combination may be administered orally or transdermally depending on formulation[1][10]. The combination is not typically used for contraception; other related combinations are used for that purpose.

Brand names
LunelleCyclofemPremproPremphase
Other names
17β-estradiol + medroxyprogesterone acetateestradiol + medroxyprogesterone acetate
02

Targets

PR (Progesterone receptor)ESR2 (ERβ)GR (Glucocorticoid receptor)ESR1 (ERα)

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