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Relugolix Combination Therapy
Relugolix is a gonadotropin-releasing hormone (GnRH) antagonist that suppresses luteinizing hormone and follicle-stimulating hormone, leading to rapid reduction of testosterone and estrogen levels.
Relugolix is a gonadotropin-releasing hormone (GnRH) antagonist that suppresses luteinizing hormone and follicle-stimulating hormone, leading to rapid reduction of testosterone and estrogen levels. Used for Advanced prostate cancer requiring androgen deprivation therapy, Hormone receptor-positive breast cancer (in combination with other therapies).
At a glance
| Generic name | Relugolix Combination Therapy |
|---|---|
| Also known as | Myfembree |
| Sponsor | Sumitomo Pharma Switzerland GmbH |
| Drug class | GnRH antagonist |
| Target | GnRH receptor |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Relugolix combination therapy pairs the GnRH antagonist relugolix with estradiol and norethisterone acetate to provide androgen deprivation while mitigating hypogonadism-related side effects. By blocking GnRH signaling, it rapidly lowers sex hormone production, which is therapeutically beneficial in hormone-sensitive cancers. The addition of hormone replacement helps manage adverse effects associated with severe hormone suppression.
Approved indications
- Advanced prostate cancer requiring androgen deprivation therapy
- Hormone receptor-positive breast cancer (in combination with other therapies)
Common side effects
- Hot flashes
- Fatigue
- Decreased libido
- Erectile dysfunction
- Headache
- Injection site reactions
Key clinical trials
- Supraphysiologic Testosterone Priming Induces Darolutamide Extended Response (PHASE2)
- Effects of Relugolix vs Leuprolide on Cardiac Function in Patients With Prostate Cancer (PHASE2)
- Relugolix for Endometriosis Associated Pain
- Estradiol-mediated Inflammation and Central Sensitization in the Pathophysiology of Endometriosis-associated Pelvic Pain (PHASE3)
- Neoadjuvant Darolutamide and Relugolix Combination Preceding Radical Prostatectomy for Prostate Cancer (PHASE1)
- Difluoromethylornithine and High Dose Testosterone With Enzalutamide in Metastatic Castration-Resistant Prostate Cancer (PHASE2)
- Two Studies for Patients With High Risk Prostate Cancer Testing Less Intense Treatment for Patients With a Low Gene Risk Score and Testing a More Intense Treatment for Patients With a High Gene Risk Score, The PREDICT-RT Trial (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)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Relugolix Combination Therapy CI brief — competitive landscape report
- Relugolix Combination Therapy updates RSS · CI watch RSS
- Sumitomo Pharma Switzerland GmbH portfolio CI