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Relugolix + Estradiol + Norethindrone Acetate
Relugolix suppresses luteinizing hormone and follicle-stimulating hormone by antagonizing GnRH receptors, while estradiol and norethindrone acetate provide hormone replacement to manage menopausal symptoms in women with endometriosis.
Relugolix suppresses luteinizing hormone and follicle-stimulating hormone by antagonizing GnRH receptors, while estradiol and norethindrone acetate provide hormone replacement to manage menopausal symptoms in women with endometriosis. Used for Moderate to severe pain associated with endometriosis in women of reproductive potential.
At a glance
| Generic name | Relugolix + Estradiol + Norethindrone Acetate |
|---|---|
| Also known as | MVT-601, MVT-601A, MYFEMBREE |
| Sponsor | Sumitomo Pharma Switzerland GmbH |
| Drug class | GnRH antagonist combination with hormone replacement therapy |
| Target | GnRH receptor (relugolix component) |
| Modality | Small molecule |
| Therapeutic area | Gynecology / Endometriosis |
| Phase | FDA-approved |
Mechanism of action
Relugolix is a non-peptide GnRH antagonist that rapidly suppresses gonadotropins, reducing estrogen production and providing pain relief in endometriosis. The combination with estradiol and norethindrone acetate (a progestin) replaces hormones to alleviate vasomotor and other menopausal symptoms that would otherwise occur from the GnRH antagonism, while maintaining the therapeutic benefit of low estrogen for endometriosis management.
Approved indications
- Moderate to severe pain associated with endometriosis in women of reproductive potential
Common side effects
- Hot flashes
- Headache
- Nausea
- Breast tenderness
- Vaginal bleeding/spotting
- Mood changes
Key clinical trials
- Estradiol-mediated Inflammation and Central Sensitization in the Pathophysiology of Endometriosis-associated Pelvic Pain (PHASE3)
- Study of the Safety and Contraceptive Efficacy of Relugolix Combination Therapy in Women With Uterine Fibroids or Endometriosis Who Are at Risk for Pregnancy (PHASE3)
- Surgical Myomectomy Followed by Oral Myfembree Versus Standard of Care Trial (SOUL) (PHASE4)
- Phenotyping of Idiopathic Pelvic Pain With Real-time Uterine Imaging and Relugolix-Combination Therapy Treatment (PHASE2)
- Ultrasound Transformation of Myomas During Relugolix-Estradiol-Norethisterone Treatment: The MySaturn Study
- A Phase 3B Study to Evaluate Bone Mineral Density With Long-Term Use of Relugolix Combination Tablet in Women With Uterine Fibroids or Endometriosis (PHASE3)
- MYFEMBREE®: A Retrospective Cohort Study Using an Administrative Healthcare Database to Assess Pregnancy Outcomes in Women Treated With Relugolix Combination Therapy
- The Effect of Medical Management Following Excisional Surgery for Endometriosis: A Randomized Controlled Trial (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
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