Relugolix, an oral gonadotropin-releasing hormone receptor antagonist, reduces endometriosis-associated pain in a dose–response manner: a randomized, double-blind, placebo-controlled study

Osuga Y, Yutaka Osuga, Seki Y, Yoshifumi Seki, Tanimoto M, Masataka Tanimoto, Takeru Kusumoto, Kusumoto T, Kentarou Kudou, Naoki Terakawa, Terakawa N
Fertility and sterility · 2020 · vol. 115(2) , pp. 397–405 · doi:10.1016/j.fertnstert.2020.07.055 · PMID:32912633 · W3083548215
article OA: closed CC0 ⤵ 53 in-corpus citations
View on OpenAlex View on PubMed View at publisher
⚙ AI-generated summary by claude@2026-06, 2026-06-07 ⓘ

This randomized, double-blind, placebo-controlled study found that the oral GnRH receptor antagonist relugolix effectively reduced endometriosis-associated pain in a dose-dependent manner.

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

Abstract

ObjectiveTo evaluate the efficacy and safety of three dose levels of relugolix, a gonadotropin-releasing hormone receptor antagonist, compared with placebo and leuprorelin in women with endometriosis-associated pain.DesignPhase 2, multicenter, randomized, double-blind, placebo-controlled study.SettingHospitals and clinics.Patient(s)Adult premenopausal women with endometriosis who had dysmenorrhea and endometriosis-associated pelvic pain.Intervention(s)During a 12-week treatment period, patients received relugolix 10 mg (n = 103), 20 mg (n = 100), or 40 mg (n = 103) as a daily oral dose; placebo (n = 97) as a daily oral dose; or leuprorelin 3.75 mg (n = 80) as a monthly subcutaneous injection.Main outcome measure(s)Primary endpoint was the change from baseline in mean visual analog scale score for pelvic pain during 28 days before the end of treatment.Result(s)The mean changes in mean visual analog scale score for pelvic pain were -3.8 mm in the placebo group; -6.2, -8.1, and -10.4 mm in the relugolix 10-mg, 20-mg, and 40-mg groups; respectively; and -10.6 mm in the leuprorelin group. The major adverse events with relugolix were hot flush, metrorrhagia, menorrhagia, and irregular menstruation, and bone mineral density decrease in a dose-response manner, which were also observed in the leuprorelin group with a frequency comparable with that in the relugolix 40-mg group.Conclusion(s)Oral administration of relugolix alleviated endometriosis-associated pain in a dose-response manner and was generally well tolerated. Relugolix 40 mg demonstrated efficacy and safety comparable with those of leuprorelin.Clinical trial registration numberNCT01458301.

My notes (saved in your browser only)

Condition tags

endometriosischronic_pelvic_pain

MeSH descriptors

Androgen Antagonists Endometriosis Pain Measurement Pelvic Pain Phenylurea Compounds Pyrimidinones Receptors, LHRH Administration, Oral Adult Androgen Antagonists Dose-Response Relationship, Drug Double-Blind Method Endometriosis Endometriosis Female Humans Middle Aged Pain Measurement Pain Measurement Pelvic Pain

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 (19)

Cited by (50)

Source provenance

europepmc
last seen: 2026-07-26T06:08:39.051465+00:00
openalex
last seen: 2026-06-10T17:14:06.276822+00:00
pubmed
last seen: 2026-05-13T22:21:42.008780+00:00
License: CC0 · commercial use OK