Suppression of Gonadotropins and Estradiol in Premenopausal Women by Oral Administration of the Nonpeptide GnRH Antagonist Elagolix

R. Scott Struthers, Andrew Nicholls, John S. Grundy, Takung Chen, Roland Jimenez, Haig Bozigian
2008 · W2189119026
article OA: closed CC0 Metadata only
View on OpenAlex
⚙ AI-generated summary by claude@2026-06, 2026-06-09 ⓘ

This study evaluated the safety, pharmacokinetics, and inhibitory effects of the oral nonpeptide GnRH antagonist elagolix on gonadotropins and estradiol in healthy premenopausal women.

One-sentence paraphrase of the abstract; not a substitute for reading it. No clinical advice. How this works

Abstract

ABSTRACT Context: Parenteral administration of peptide GnRH analogs is widely employed for treatment of endometriosis, fibroids and in assisted-reproductive therapy protocols. Elagolix is a novel, orally available nonpeptide GnRH antagonist. Objective: To evaluate the safety, pharmacokinetics and inhibitory effects on gonadotropins and estradiol of single dose and 7-day elagolix administration to healthy premenopausal women. Design: This was a first-in-human, double-blind, placebo-controlled, single- and multiple dose study with sequential dose-escalation. Participants: Fifty-five healthy, regularly cycling pre-menopausal women. Interventions: Subjects were administered a single oral dose of 25 to 400 mg or placebo. In a second arm of the study, subjects received placebo or 50, 100, or 200 mg q.d. or 100 mg b.i.d. for seven days. Treatment was initiated on Day 7 (±1) following onset of menses. Main Outcome Measures: Safety, tolerability, pharmacokinetics and serum LH, FSH and estradiol concentrations.

My notes (saved in your browser only)

Condition tags

endometriosis

Citation neighborhood

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. [ expand to 2 hops ] — adds papers reached through this work's immediate citers/citees. Heavier; up to 60 extra dots.

References (23)

Source provenance

openalex
last seen: 2026-06-10T17:14:06.276822+00:00
License: CC0 · commercial use OK