Drug intelligence / Profile preview

estradiol + norethisterone acetate (Novo Nordisk)

Development stage
Phase 3
Lead developer
Novo Nordisk
Modality
Small Molecules
Administration
Oral
01

Overview

ABT(E2 1 mg / NETA 0.5 mg) is a continuous combined oral hormone replacement therapy consisting of a fixed low-dose combination of estradiol (1 mg) and norethisterone acetate (0.5 mg). Estradiol acts as an agonist at estrogen receptors to alleviate hypoestrogenic symptoms, while norethisterone acetate acts as a progesterone receptor agonist to protect the endometrium from estrogen-induced hyperplasia. In clinical trials, this combination is widely used as a hormonal add-back therapy (ABT) in conjunction with gonadotropin-releasing hormone (GnRH) receptor antagonists (such as linzagolix, relugolix, and elagolix) to counteract the bone mineral density loss and vasomotor symptoms associated with profound estrogen suppression. In China, Bio Genuine is co-developing this combination as an adjunct to linzagolix (BG2109) in Phase III trials for the management of moderate to severe endometriosis-associated pain and heavy menstrual bleeding associated with uterine fibroids.

Brand names
ActivellaAmabelzKliovanceLopreezaMimvey
Other names
ABT (E2 1 mg / NETA 0.5 mg)ABT(E2 1 mg / NETA 0.5 mg)E2/NETAestradiol + norethindrone acetateestradiol/norethindrone acetateestradiol/norethisterone acetate
02

Targets

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

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