Literature DB >> 32912633

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

Yutaka Osuga1, Yoshifumi Seki2, Masataka Tanimoto2, Takeru Kusumoto2, Kentarou Kudou2, Naoki Terakawa3.   

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.
Copyright © 2020 The Authors. Published by Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Endometriosis-associated pain; GnRH; gonadotropin-releasing hormone receptor antagonist; relugolix

Mesh:

Substances:

Year:  2020        PMID: 32912633     DOI: 10.1016/j.fertnstert.2020.07.055

Source DB:  PubMed          Journal:  Fertil Steril        ISSN: 0015-0282            Impact factor:   7.329


  6 in total

1.  An Efficient UPLC-MS/MS Method Established to Detect Relugolix Concentration in Rat Plasma.

Authors:  Liying Xing; Ya-Nan Liu; Hongye Yao; Tingting Wang; Fuchen Xie; Shunbin Luo; Pingping Luo; Shengling Tang
Journal:  Front Pharmacol       Date:  2022-06-16       Impact factor: 5.988

2.  Therapeutic effects of an oral gonadotropin-releasing hormone receptor antagonist, relugolix, on preventing premature ovulation in mild ovarian stimulation for IVF.

Authors:  Kazuki Nakao; Keiji Kuroda; Takashi Horikawa; Azusa Moriyama; Hiroyasu Juen; Akiko Itakura; Hideaki Watanabe; Satoru Takamizawa; Yuko Ojiro; Koji Nakagawa; Rikikazu Sugiyama
Journal:  Reprod Med Biol       Date:  2021-10-19

3.  A novel orally active gonadotropin-releasing hormone antagonist, relugolix, is a potential substitute for injectable GnRH antagonists in controlled ovarian stimulation in assisted reproductive technology.

Authors:  Michiko Hamada; Michiharu Horikawa; Chie Ensaka; Megumi Enomoto; Rena Ishii; Rena Toriumi; Naoyuki Tachibana; Yuji Taketani
Journal:  Reprod Med Biol       Date:  2021-11-12

Review 4.  GnRH Antagonists with or without Add-Back Therapy: A New Alternative in the Management of Endometriosis?

Authors:  Jacques Donnez; Marie-Madeleine Dolmans
Journal:  Int J Mol Sci       Date:  2021-10-20       Impact factor: 5.923

5.  Relugolix, an oral gonadotropin-releasing hormone (GnRH) receptor antagonist, in women with endometriosis-associated pain: phase 2 safety and efficacy 24-week results.

Authors:  Yutaka Osuga; Yoshifumi Seki; Masataka Tanimoto; Takeru Kusumoto; Kentarou Kudou; Naoki Terakawa
Journal:  BMC Womens Health       Date:  2021-06-21       Impact factor: 2.809

6.  Uterine Adenomyosis Treated by Linzagolix, an Oral Gonadotropin-Releasing Hormone Receptor Antagonist: A Pilot Study with a New 'Hit Hard First and then Maintain' Regimen of Administration.

Authors:  Jacques Donnez; Olivier Donnez; Jean Tourniaire; Michel Brethous; Elke Bestel; Elizabeth Garner; Sébastien Charpentier; Andrew Humberstone; Ernest Loumaye
Journal:  J Clin Med       Date:  2021-12-10       Impact factor: 4.241

  6 in total

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