Drug intelligence / Profile preview

linzagolix + estradiol + norethisterone acetate

Development stage
Unknown
Lead developer
ObsEva
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of **linzagolix** (an oral, non-peptide GnRH antagonist), **estradiol** (an estrogen), and **norethisterone acetate** (a progestin), used as a fixed-dose oral medication for managing moderate to severe symptoms of **endometriosis** and **uterine fibroids** in adult women of reproductive age. Linzagolix acts by competitively binding to GnRH receptors in the pituitary, suppressing luteinising hormone and follicle-stimulating hormone, which leads to dose-dependent reductions in serum estradiol. The addition of estradiol and norethisterone acetate as hormonal add-back therapy (ABT) mitigates hypoestrogenic side effects (e.g., bone density loss, vasomotor symptoms) and maintains estradiol in the optimal range. Efficacy for the combination (linzagolix 200 mg + ABT: 1.0 mg estradiol and 0.5 mg norethisterone acetate) is demonstrated in reducing endometriosis-related dysmenorrhea and non-menstrual pelvic pain, and reducing heavy menstrual bleeding associated with uterine fibroids[1][2][6].

Other names
OBE2109 + estradiol + norethindrone acetate
02

Targets

ESR2 (ERβ)PR (Progesterone receptor)ESR1 (ERα)GnRHR (Gonadotropin-releasing hormone receptor)

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