Drug intelligence / Profile preview

17beta-estradiol + progestin

Development stage
Unknown
Lead developer
Teva Pharmaceutical
Modality
Small Molecules
Administration
Oral, Vaginal
01

Overview

17beta-estradiol + progestin is a combination drug containing 17beta-estradiol (the naturally occurring estrogen in women) and a synthetic or natural progestin (such as dienogest, nomegestrol acetate, norethisterone, progesterone, cyproterone acetate, medroxyprogesterone, or others). - **Mechanism of Action:** The combination works primarily by supplementing deficient estrogen states and providing progestin to counteract the risk of endometrial hyperplasia from unopposed estrogen. Estradiol acts as an agonist of the estrogen receptor, reducing vasomotor symptoms (VMS) and menopausal symptoms, while the progestin acts as an agonist of the progesterone receptor, protecting against endometrial hyperplasia and allowing for use in women with an intact uterus. In contraceptive use, the combination suppresses ovulation and alters cervical mucus and the endometrium to prevent pregnancy[1][2][4]. - **Indications:** - Menopausal hormone therapy (treatment of moderate-to-severe vasomotor symptoms) - Hormonal contraception - Management of menstrual disorders - **Formulations:** Available in oral tablets (monophasic, biphasic, quadriphasic), capsules, and vaginal rings. Approved combinations include various progestins with 17beta-estradiol or its esters (e.g., estradiol valerate)[1][2][6][7].

Brand names
NataziaQlairaZoelyNaemisBijuvaFemilar
Other names
estradiol/progestin combinationE2 + progestin
02

Targets

GPER1 (G protein-coupled estrogen receptor 1)PR (Progesterone receptor)ESR2 (ERβ)ESR1 (ERα)

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