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
RCT OA: closed CC0 ⤵ 53 in-corpus citations
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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.

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Abstract

OBJECTIVE: To 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. DESIGN: Phase 2, multicenter, randomized, double-blind, placebo-controlled study. SETTING: Hospitals 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 NUMBER: NCT01458301.

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Condition tags

endometriosischronic_pelvic_pain

MeSH descriptors

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

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