Drug intelligence / Profile preview

norethisterone acetate + estrogen

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

Overview

Norethisterone acetate + estrogen is a combination drug containing a progestogen (norethisterone/norethindrone acetate) and an estrogen (commonly estradiol or ethinyl estradiol). It is used primarily for hormone replacement therapy in postmenopausal women to treat moderate to severe vasomotor symptoms of menopause such as hot flashes and vaginal atrophy, as well as for the prevention of postmenopausal osteoporosis[1][4][5]. In some formulations with ethinyl estradiol it is also used as an oral contraceptive[3][8]. The addition of the progestogen protects the endometrium from hyperplasia associated with unopposed estrogen therapy[2]. The mechanism involves binding to nuclear hormone receptors: estrogens act via the estrogen receptor to regulate gene transcription involved in reproductive tissues; progestins act via the progesterone receptor to oppose endometrial proliferation induced by estrogens.

Brand names
ActivellaLopreezaMimveyCombipatchEstalisEstalis-SequiAmabelzFemHRTFyavolvJinteliLarin 1/20Larin 1.5/30Loestrin 1/20Loestrin 1.5/30Microgestin 1/20Microgestin 1.5/30Estrostep
Other names
estradiol and norethindrone acetate (USAN)norethindrone acetate and ethinyl estradiol
02

Targets

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

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