Relugolix for Uterine Fibroids
Recruiting in Palo Alto (17 mi)
+85 other locations
Age: 18 - 65
Sex: Female
Travel: May be covered
Time Reimbursement: Varies
Trial Phase: Phase 3
Recruiting
Sponsor: Myovant Sciences GmbH
No Placebo Group
Pivotal Trial (Near Approval)
Prior Safety Data
Approved in 2 jurisdictions
Trial Summary
What is the purpose of this trial?The purpose of this clinical trial to characterize changes in bone mineral density during continuous treatment with relugolix combination tablet for up to 48 months (4 years) and 1 year of post-treatment follow-up in premenopausal women with heavy menstrual bleeding associated with uterine leiomyomas (fibroids) or with moderate-to-severe pain associated with endometriosis.
What data supports the effectiveness of the drug Relugolix Combination Tablet for treating uterine fibroids?
Research shows that the Relugolix Combination Tablet significantly reduces heavy menstrual bleeding and other symptoms associated with uterine fibroids. In clinical trials, it was well tolerated and helped maintain bone health over long-term use.
23456How is the drug Relugolix Combination Tablet unique for treating uterine fibroids?
Relugolix Combination Tablet is unique because it is the first and only once-daily oral therapy that combines a GnRH receptor antagonist with estradiol and norethindrone acetate to manage heavy menstrual bleeding and other symptoms of uterine fibroids, while also preventing bone loss and hot flashes.
23457Is Relugolix safe for treating uterine fibroids?
Relugolix combination therapy, used for uterine fibroids, is generally well tolerated with the most common side effects being hot flashes and other vasomotor symptoms (like sweating and flushing). Long-term use did not lead to significant bone loss in most women, making it a safe option for many.
12345Will I have to stop taking my current medications?
The trial requires participants to stop using hormonal contraceptives or other prohibited medications. If you are currently using these, you will need to discontinue them to join the study.
Eligibility Criteria
This trial is for premenopausal women aged 18-50 with uterine fibroids or endometriosis causing heavy menstrual bleeding or pain. Participants must not be at risk of pregnancy or agree to nonhormonal contraception for 4 years, have a BMI ≥ 18 kg/m^2, and cannot have certain bone density issues, vitamin D deficiencies without supplementation, history of specific cancers, organ transplants, psychiatric disorders affecting study participation, or use prohibited medications.Participant Groups
The trial studies the long-term effects (up to 48 months) of Relugolix Combination Tablet on bone mineral density in women with uterine fibroids or endometriosis. It includes continuous treatment and a follow-up year to monitor changes in bone health.
1Treatment groups
Experimental Treatment
Group I: Relugolix Combination TabletExperimental Treatment1 Intervention
Participants will receive relugolix combination therapy orally once daily for 48 months.
Relugolix Combination Tablet is already approved in United States, European Union for the following indications:
🇺🇸 Approved in United States as Myfembree for:
- Heavy menstrual bleeding associated with uterine fibroids
- Moderate to severe pain associated with endometriosis
🇪🇺 Approved in European Union as Ryeqo for:
- Moderate to severe symptoms of uterine fibroids
Find A Clinic Near You
Research locations nearbySelect from list below to view details:
DelandDeLand, FL
NorcrossNorcross, GA
WebsterWebster, TX
LakewoodLakewood, CO
More Trial Locations
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Who is running the clinical trial?
Myovant Sciences GmbHLead Sponsor
Sumitomo Pharma Switzerland GmbHLead Sponsor
References
Relugolix, a novel oral gonadotropin-releasing hormone antagonist, in the treatment of pain symptoms associated with uterine fibroids: a randomized, placebo-controlled, phase 3 study in Japanese women. [2020]To investigate the efficacy and safety of the oral gonadotropin-releasing hormone receptor antagonist, relugolix, in patients experiencing uterine fibroid-associated pain.
Relugolix/Estradiol/Norethisterone (Norethindrone) Acetate: A Review in Symptomatic Uterine Fibroids. [2022]An oral fixed-dose combination of relugolix/estradiol/norethisterone (also known as norethindrone) acetate (Ryeqo®; Myfembree®) has been approved for the management of heavy menstrual bleeding associated with uterine fibroids in the USA and management of moderate to severe symptoms of uterine fibroids in the EU. Relugolix is a gonadotropin releasing hormone (GnRH) receptor antagonist that decreases serum estradiol and progesterone concentrations to postmenopausal levels. The addition of estradiol/norethisterone acetate to relugolix ameliorates relugolix-induced bone loss and hot flush. In the two phase 3 LIBERTY trials, relugolix + estradiol/norethisterone substantially decreased menstrual bleeding and improved a range of other uterine fibroid symptoms in women with uterine fibroids-associated heavy menstrual bleeding. The combination was generally well tolerated, with vasomotor symptoms being the most common adverse reaction. Treatment with this combination for over up to 2 years did not induce a clinically meaningful bone loss in the majority of women. Relugolix/estradiol/norethisterone acetate, with its convenient once-daily administration, is a useful addition to current pharmacological treatment options for premenopausal women with symptomatic uterine fibroids.
Development of relugolix combination therapy as a medical treatment option for women with uterine fibroids or endometriosis. [2023]Treatment of uterine fibroids (UF) and endometriosis (EM) has relied on the surgical skills of gynecologists to improve symptoms and potentially alter the course of these debilitating diseases. Medical management of symptoms for both diseases leverages combined hormonal contraceptives used off label as a first-line treatment, with nonsteroid anti-inflammatory drugs and opioids to manage pain as needed. Gonadotropin-releasing hormone (GnRH) receptor agonists (peptide analogs) have been used as short-term therapy to manage severe symptoms of UF or EM, treat anemia, and reduce fibroid size before surgery. The introduction of oral GnRH receptor antagonists opened the door for the development of new treatment options for UF, EM, and other estrogen-driven diseases. Relugolix is an orally active, nonpeptide, GnRH receptor antagonist that competitively binds to GnRH receptors, preventing the release of follicle-stimulating hormone and luteinizing hormone (LH) into the systemic circulation. In women, the reduction in follicle-stimulating hormone concentrations prevents natural follicular development, suppressing ovarian production of estrogen, and together with reductions in LH concentrations, prevent ovulation, corpus luteum formation, and, thereby, the production of progesterone (P). By reducing circulating concentrations of estradiol (E2) and P, relugolix improves heavy menstrual bleeding and other symptoms associated with UF and moderate to severe pain associated with EM, including dysmenorrhea, nonmenstrual pelvic pain (NMPP) and dyspareunia. However, as monotherapy, the use of relugolix is associated with signs and symptoms of a hypoestrogenic state, including bone mineral density loss and vasomotor symptoms. The clinical development of relugolix incorporated the addition of a 1 mg dose of E2 and a 0.5-mg dose of norethindrone acetate (NETA) to achieve systemic E2 concentrations that remain in a therapeutic range while mitigating the risk for bone mineral density loss and vasomotor symptoms, enabling the longer-term treatment and reducing the impact of symptoms on quality of life, and potentially delaying or preventing the need for surgery. Relugolix 40 mg in combination with estradiol (E2) 1 mg and NETA 0.5 mg as a single fixed-dose combination tablet (relugolix combination therapy [relugolix-CT]) approved in the United States as MYFEMBREE is the first and only once daily oral GnRH antagonist combination therapy indicated for the management of heavy menstrual bleeding associated with UF and moderate to severe pain associated with EM. In the European Union (EU) and the United Kingdom (UK), relugolix-CT is approved as RYEQO for the management of symptoms associated with UF. In Japan, relugolix 40 mg, as monotherapy, was the first GnRH receptor antagonist approved to improve symptoms associated with UF or pain associated with EM under the brand name RELUMINA. In men, relugolix suppresses testosterone production. Relugolix 120 mg (ORGOVYX) was developed by Myovant Sciences and is approved in the United States, EU, and UK as the first and only oral androgen-deprivation therapy for the treatment of advanced prostate cancer. This review is focused on the development of relugolix and relugolix-CT in women's health indications.
Relugolix combination therapy in European women with symptomatic uterine fibroids: a subgroup analysis from the randomized phase 3 LIBERTY pivotal trials. [2023]Label="OBJECTIVE" NlmCategory="UNASSIGNED">In the 24-week, phase 3 LIBERTY 1 (L1) and LIBERTY 2 (L2) trials, relugolix combination therapy (relugolix-CT (relugolix 40 mg, estradiol 1 mg, norethisterone acetate 0.5 mg)) reduced uterine fibroid (UF)-associated symptoms. This post hoc analysis assessed safety and efficacy of relugolix-CT in European women from L1/L2.
LIBERTY randomized withdrawal study: relugolix combination therapy for heavy menstrual bleeding associated with uterine fibroids. [2023]In the pivotal LIBERTY 1 and 2 trials and long-term extension study, once-daily relugolix combination therapy (40 mg relugolix, 1 mg estradiol, 0.5 mg norethindrone acetate) reduced menstrual blood loss volume and pain among women with uterine fibroids. Relugolix combination therapy was well tolerated with preservation of bone mineral density through 52 weeks.
Relugolix combination therapy in Black/African American women with symptomatic uterine fibroids: LIBERTY Long-Term Extension study. [2023]In the LIBERTY Long-Term Extension study, once-daily relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) substantially improved uterine fibroid-associated heavy menstrual bleeding throughout the 52-week treatment period in the overall study population.
Relugolix combination therapy and symptoms of uterine myomatosis - selected case reports of indication spectrum and treatment outcomes. [2023]An illustrative review of the indications for relugolix combination therapy (RCT) in the management of symptoms associated with uterine myomatosis.