Drugs / Relugolix
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Relugolix

Small molecule targets GNRHR via inhibition

Developed for
prostate cancer · endometriosis · leiomyoma · prostate adenocarcinoma · prostate carcinoma · metastatic prostate carcinoma · pelvis syndrome · benign neoplasm of corpus uteri
+4 more · castration-resistant prostate carcinoma · menstrual disorder · uterine benign neoplasm · uterine corpus leiomyoma
Investigated by
Myovant Sciences GmbH · Takeda · Pfizer · National Cancer Institute (NCI) · Sumitomo Pharma America, Inc. · Millennium Pharmaceuticals, Inc.
+36 more · Sumitomo Pharma Switzerland GmbH · Bayer · Emory University · Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) · NYU Langone Health · National Comprehensive Cancer Network · Prostate Cancer Foundation · University of Chicago · ASKA Pharmaceutical Co., Ltd. · AdventHealth · Astellas Pharma Inc · Atish Choudhury, MD · Baptist Health South Florida · Blue Earth Diagnostics · Dana-Farber Cancer Institute · Debiopharm International SA · Endeavor Health · Insel Gruppe AG, University Hospital Bern · Janssen Research & Development, LLC · Mayo Clinic · NRG Oncology · National Cancer Institute, Naples · National Institutes of Health (NIH) · Ohio State University Comprehensive Cancer Center · Oregon Health and Science University · Qilu Pharmaceutical Co., Ltd. · Sean Sachdev · University Hospital, Geneva · University of Bern · University of Kansas Medical Center · University of Miami · University of Michigan · University of Oklahoma · University of Utah · Varian Medical Systems · Werner und Hedy Berger-Janser - Stiftung

Regulatory milestones approvals, filings & regulatory actions · 3 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansion US (FDA) ORGOVYX — 2024-10-18 fda.gov ↗
Approved EU (EMA) Ryeqo — 2021-07-16 europa.eu ↗
Approved US (FDA) ORGOVYX — 2020-12-18 fda.gov ↗

Trials 53

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 111 trials
Phase 1 NCT06130995 Dec 2024 → Jan 2029 expected — University of Oklahoma Recruiting No outcome recorded
Phase 1 NCT06631521 Oct 2024 → Jun 2026 overdue prostate adenocarcinoma AdventHealth Recruiting No outcome recorded
Phase 1 NCT05679388 Feb 2023 → Aug 2024 prostate adenocarcinoma University of Chicago Terminated No outcome recorded
Phase 1 NCT04666129 Feb 2021 → May 2024 castration-resistant prostate carcinoma, metastatic prostate carcinoma Sumitomo Pharma America, Inc. Completed No outcome recorded
Phase 1 NCT04714554 Jan → Mar 2021 — Myovant Sciences GmbH Completed No outcome recorded
Phase 1 NCT02792062 Jul → Aug 2016 — Takeda Completed No outcome recorded
Phase 1 NCT04978688 Jun → Sep 2016 — Myovant Sciences GmbH Completed No outcome recorded
Phase 1 NCT02396147 Mar → Apr 2015 — Takeda Completed No outcome recorded
Phase 1 NCT02252354 Sep → Oct 2014 — Takeda Completed No outcome recorded
Phase 1 NCT02141659 May 2014 → Apr 2017 prostate carcinoma Takeda Completed No outcome recorded
Phase 221 trials · 2 met primary
Phase 2 NCT07801664 Aug 2026 → Aug 2028 expected prostate cancer NYU Langone Health Recruiting No outcome recorded
Phase 2 NCT07455903 Apr 2026 → Oct 2029 expected prostate carcinoma Baptist Health South Florida Recruiting No outcome recorded
Phase 2 NCT07302451 Dec 2025 → May 2027 expected prostate adenocarcinoma National Cancer Institute, Naples Active not recruiting No outcome recorded
Phase 2 NCT07216248 Oct 2025 → Oct 2030 expected metastatic prostate carcinoma University of Utah Recruiting No outcome recorded
Phase 2 NCT07025369 Aug 2025 → Jan 2029 expected prostate adenocarcinoma Mayo Clinic Recruiting No outcome recorded
Phase 2 NCT06463457 Dec 2024 → Nov 2028 expected prostate cancer Atish Choudhury, MD Active not recruiting No outcome recorded
Phase 2 NCT06111313 Nov 2024 → Nov 2028 expected prostate cancer University of Miami Recruiting No outcome recorded
Phase 2 NCT06499870 Sep 2024 → Nov 2030 expected prostate adenocarcinoma Sean Sachdev Recruiting No outcome recorded
Phase 2 NCT06330805 Aug 2024 → Dec 2027 expected prostate adenocarcinoma Ohio State University Comprehensive Cancer Center Recruiting No outcome recorded
Phase 2 NCT06279195 Jun 2024 → Nov 2025 pelvis syndrome Endeavor Health Withdrawn No outcome recorded Stop: Business
Phase 317 trials · 9 met primary
Phase 3 NCT07100782 Dec 2025 → Aug 2028 expected endometriosis, pelvis syndrome University of Michigan Recruiting No outcome recorded
Phase 3 NCT06650579 Jan 2025 → Jul 2029 expected prostate carcinoma Emory University Recruiting No outcome recorded
Phase 3 NCT06671548 Jan 2024 → Nov 2026 expected leiomyoma Qilu Pharmaceutical Co., Ltd. Recruiting No outcome recorded
Phase 3 NCT05862272 Aug 2023 → Jul 2029 expected endometriosis, leiomyoma Sumitomo Pharma Switzerland GmbH Recruiting No outcome recorded
Phase 3 NCT05605964 Jan 2023 → Dec 2024 prostate cancer Sumitomo Pharma America, Inc. Completed No outcome recorded
Phase 3 NCT04756037 Mar 2021 → Feb 2025 — Sumitomo Pharma Switzerland GmbH Completed No outcome recorded
Phase 3 NCT03931915 May 2019 → Jun 2020 endometriosis ASKA Pharmaceutical Co., Ltd. Completed Met primary
Phase 3 NCT03751124 Oct 2018 → Feb 2021 uterine corpus leiomyoma Myovant Sciences GmbH Completed Met primary
Phase 3 NCT03654274 May 2018 → Dec 2021 endometriosis Myovant Sciences GmbH Completed No outcome recorded
Phase 3 NCT03204318 Dec 2017 → Jun 2020 endometriosis Myovant Sciences GmbH Completed Met primary
Phase 42 trials
Phase 4 NCT07111247 Jan 2026 → Aug 2027 expected — Oregon Health and Science University Recruiting No outcome recorded
Phase 4 NCT05538689 Nov 2022 → Oct 2024 leiomyoma, menstrual disorder University of Chicago Withdrawn No outcome recorded
Phase not applicable2 trials
— NCT07173127 Sep 2025 → Dec 2026 expected uterine benign neoplasm University Hospital, Geneva Recruiting No outcome recorded
— NCT05746806 Mar 2023 → Nov 2027 expected prostate carcinoma Insel Gruppe AG, University Hospital Bern Active not recruiting No outcome recorded
Comparator or background therapy19 trials
Phase 0 NCT07069465 Comparator Jun → Nov 2024 prostate cancer Urology Clinics of North Texas Completed No outcome recorded
Phase 1 NCT06531499 Background Nov 2024 → Nov 2028 expected prostate carcinoma Novartis Pharmaceuticals Recruiting No outcome recorded
Phase 1 NCT06379217 Background Jul 2024 → Sep 2026 overdue prostate neuroendocrine neoplasm Novartis Pharmaceuticals Active not recruiting No outcome recorded
Phase 1/2 NCT06312761 Background Jun 2024 → Dec 2025 hypogonadism, male University of Washington Unknown No outcome recorded
Phase 2 NCT07142551 Background Mar 2026 → Jun 2030 expected castration-resistant prostate carcinoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Recruiting No outcome recorded

News releases announcing trial results or a regulatory action · 13

DateIssuerRelease
2026-06-22 ASKA Pharmaceutical Co., Ltd. Results relugolix 配合剤(AKP-022)の子宮筋腫患者を対象とした 国内第 3 相臨床試験結果のお知らせ aska-pharma.co.jp ↗
2022-08-05 Pfizer Regulatory Myovant Sciences and Pfizer Receive U.S. FDA Approval of MYFEMBREE®, a Once-Daily Treatment for the Management of Moderate to Severe Pain Associated With Endometriosis pfizer.com ↗
MYFEMBREE (relugolix, estradiol, and norethindrone acetate) is a once-daily oral treatment approved by the U.S. Food and Drug Administration for the management of moderate to severe pain associated with endometriosis, with a treatment duration of up to 24 months.
2022-06-17 Pfizer Results Myovant Sciences and Pfizer Announce Publication in The Lancet of Phase 3 SPIRIT 1 and SPIRIT 2 Studies of Once-Daily Relugolix Combination Therapy in Women With Endometriosis-Associated Pain pfizer.com ↗
As previously reported, both studies achieved their co-primary endpoints by demonstrating clinically meaningful reductions in dysmenorrhea (menstrual pain) and non-menstrual pelvic pain in women with endometriosis.
2022-06-02 Pfizer Regulatory Myovant Sciences and Pfizer Announce FDA Acceptance of Supplemental New Drug Application for MYFEMBREE® pfizer.com ↗
2022-05-06 Pfizer Regulatory Myovant Sciences and Pfizer Provide Update on Supplemental New Drug Application (sNDA) for MYFEMBREE® for the Management of Moderate to Severe Pain Associated With Endometriosis pfizer.com ↗
2022-04-12 Pfizer Regulatory Myovant Sciences and Pfizer Provide Update on Supplemental New Drug Application for MYFEMBREE® for the Management of Moderate to Severe Pain Associated with Endometriosis pfizer.com ↗
The FDA noted that the letter does not reflect a final decision on the pending sNDA and that the application is still under review.
2021-09-09 Pfizer Regulatory Myovant Sciences and Pfizer Announce FDA Acceptance of Supplemental New Drug Application for MYFEMBREE® for the Management of Moderate to Severe Pain Associated With Endometriosis pfizer.com ↗
2021-05-26 Pfizer Regulatory Myovant Sciences and Pfizer Receive FDA Approval for MYFEMBREE®, the First Once-Daily Treatment for Heavy Menstrual Bleeding Associated With Uterine Fibroids pfizer.com ↗
The FDA approval of MYFEMBREE represents a significant milestone in expanding treatment options for uterine fibroids, a chronic and debilitating disease for many women in the U.S.
2021-03-24 Pfizer Results Myovant Sciences and Pfizer Announce Positive Data from Phase 3 LIBERTY Randomized Withdrawal Study of Once-Daily Relugolix Combination Therapy in Women with Uterine Fibroids pfizer.com ↗
78.4% of women who continued on relugolix combination therapy remained responders (menstrual blood loss < 80 mL) through Week 76 compared with 15.1% of women who discontinued treatment at Week 52 (p < 0.0001)
2021-02-17 Pfizer Results Myovant Sciences and Pfizer Announce Publication in the New England Journal of Medicine of Phase 3 LIBERTY Studies of Once-Daily Relugolix Combination Therapy in Women with Uterine Fibroids pfizer.com ↗
In the LIBERTY studies, relugolix combination therapy improved the most bothersome symptoms of uterine fibroids and had a well-tolerated safety profile including maintenance of bone mineral density comparable to placebo.
2021-01-26 Pfizer Results Myovant Sciences and Pfizer Announce Positive One-Year Data from Phase 3 SPIRIT Extension Study of Once-Daily Relugolix Combination Therapy in Women with Endometriosis pfizer.com ↗
84.8% and 73.3% of women reported clinically meaningful reductions in dysmenorrhea (menstrual pain) and non-menstrual pelvic pain at one year
2017-11-09 Takeda Results Takeda Announces Positive Results from its Phase 3 Clinical Trial in Japan Evaluating the Efficacy and Safety of Relugolix in the Treatment of Pain Symptoms Associated with Uterine Fibroids takeda.com ↗
Takeda Pharmaceutical Company Limited [ TSE: 4502 ] (“Takeda”) today announced that a Phase 3 clinical trial (“TAK-385-3008 Study”) evaluating the efficacy and safety of relugolix (generic name, development code: TAK-385), a gonadotropin-releasing hormone (GnRH) receptor antagonist, met the primary endpoint of statistical significance in improvement of pain symptoms associated with uterine fibroids compared to the control group.

All press releases naming this drug 18 releases

DateIssuerRelease

Evidence & citations 9 cited values

Every value below carries the sentence it was read from. 74 sources stand behind the page.

FieldValueCited text
Known as relugolix “Patients will continue on ADT with LHRH agonist (i.e. Zoladex, Trelstar, Eligard, or Lupron) or LHRH antagonist (Degarelix or Relugolix) if not surgically castrated throughout...” NCT06922318 ↗
61

“Ryeqo® consists of an oral treatment, available as a pill, which contains 40 mg of the GnRH antagonist Relugolix, combined with 1 mg of oestradiol and a progestin, such as...” NCT07173127 ↗

“The aim of this study was to evaluate the efficacy and safety of three dose levels of oral relugolix, a small molecule GnRH receptor antagonist, in Japanese women with uterine...” PMID 34711224 ↗ Oct 2021

“luteinizing hormone-releasing hormone (LHRH) agonist (i.e. Zoladex, Trelstar, Eligard, or Lupron) or LHRH antagonist (Degarelix or Relugolix)” NCT06059118 ↗

“ADT will be delivered with monthly Degarelix, or Leuprolide injections or daily Relugolix pills which are all standard ADT interventions.” NCT07801664 ↗

“Each tablet of Myfembree contains Relugolix 40mg, estradiol 1mg, and norethindrone acetate 0.5 mg.” NCT05538689 ↗

“ADT will be administered via Leuprolide or Degarelix monthly injections or daily Relugolix pills.” NCT07142967 ↗

“ADT is defined as a GnRH agonist/antagonist (leuprolide, goserelin, degarelix, or relugolix).” NCT05628363 ↗

“GNRH agonist (leuprolide, goserelin, triptorelin) or GNRH antagonist (relugolix, degarelix)” NCT06528210 ↗

“abarelix, degarelix, or relugolix” NCT06379217 ↗

“Degarelix, Relugolix” NCT06531499 ↗

Show 51 more sources

Known as [14C]-TAK-385 “[14C]-TAK-385 Oral Solution” NCT02252354 ↗
Known as Orgovyx “e.g. Orgovyx® Tablets 120mg; first day 360mg, after second day 120mg per day” NCT05746806 ↗
2

“LHRH agonist or antagonist (e.g. Eligard, Zoladex, Lupron, Orgovyx)” NCT07142551 ↗

“Relugolix 120 MG [Orgovyx]” NCT06111781 ↗

Known as Relugolix component of myfembree ChEMBL registry synonym — accepted as the source's own label CHEMBL1800159 ↗
Known as TAK-385 “The purpose of this study is to determine the efficacy and safety of TAK-385, once daily (QD), for 12 weeks in women with endometriosis.” NCT01458301 ↗
10

“The drug being tested in this study is called relugolix (TAK-385).” NCT02083185 ↗

“TAK-385 40 mg tablets + Leuprorelin acetate placebo injection” NCT03931915 ↗

NCT01452659 ↗

NCT01452685 ↗

NCT02792062 ↗

NCT02135445 ↗

NCT02141659 ↗

NCT02396147 ↗

NCT02252354 ↗

NCT02093390 ↗

Action Inhibit “Gonadotropin-releasing hormone receptor antagonist” CHEMBL1800159 ↗
1

“a small molecule GnRH receptor antagonist” PMID 34711224 ↗ Oct 2021

Modality Small molecule “a small molecule GnRH receptor antagonist” PMID 34711224 ↗ Oct 2021
1

CHEMBL1800159 ↗

Route Oral “Patients were randomized 1:1:1:1 to relugolix 10, 20, or 40 mg, or placebo, orally once daily for 12 weeks.” PMID 34711224 ↗ Oct 2021
Target GNRHR “Gonadotropin-releasing hormone receptor antagonist” CHEMBL1800159 ↗