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

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Authors:

Yutaka Osuga, M.D., Ph.D., Yoshifumi Seki, M.Sc., Masataka Tanimoto, B.Pharm.,
Takeru Kusumoto, M.Sc., Kentarou Kudou, M.Sc., and Naoki Terakawa, M.D., Ph.D.

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.

Fertility and Sterility

Editorial Office, American Society for Reproductive Medicine

Fertility and Sterility® is an international journal for obstetricians, gynecologists, reproductive endocrinologists, urologists, basic scientists and others who treat and investigate problems of infertility and human reproductive disorders. The journal publishes juried original scientific articles in clinical and laboratory research relevant to reproductive endocrinology, urology, andrology, physiology, immunology, genetics, contraception, and menopause. Fertility and Sterility® encourages and supports meaningful basic and clinical research, and facilitates and promotes excellence in professional education, in the field of reproductive medicine.

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