Elagolix (Orilissa)
Overview
Elagolix is a small molecule non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist administered orally. While not a peptide itself, it mimics the antagonist action of peptide GnRH blockers by competitively inhibiting endogenous GnRH at pituitary receptors, resulting in dose-dependent suppression of luteinizing hormone, follicle-stimulating hormone, and ovarian sex steroids. It is indicated for management of moderate to severe endometriosis pain and heavy menstrual bleeding associated with uterine fibroids. The oral bioavailability distinguishes it from injectable peptide GnRH antagonists.
Key Research Findings
Elagolix received FDA approval in 2018 for endometriosis and in 2020 (as part of a combination product) for uterine fibroids. The Elaris endometriosis trials (published in NEJG 2017) demonstrated significant reductions in dysmenorrhea and non-menstrual pelvic pain compared to placebo across two dose regimens. Phase 3 trials in uterine fibroids showed meaningful reductions in menstrual blood loss when combined with estradiol and norethindrone add-back therapy.
Oral
FDA Approved
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