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Orgovyx (relugolix)
Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors.
Orgovyx, developed by Pfizer Inc., is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors. This reduces the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone. Orgovyx is used in the treatment of prostate cancer, uterine fibroids, and endometriosis. It is taken by mouth and has shown significant clinical differentiation in its mechanism of action. Orgovyx has achieved commercial significance with revenue of $21.2B and has a strong presence in the market. Pfizer Inc. continues to develop its pipeline, with Orgovyx being a key player in the company's portfolio.
At a glance
| Generic name | relugolix |
|---|---|
| Sponsor | MYOVANT SCIENCES |
| Drug class | Gonadotropin Releasing Hormone Receptor Antagonist [EPC] |
| Target | Gonadotropin-releasing hormone receptor |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2020 |
| Annual revenue | 421 |
Mechanism of action
Relugolix works by binding to the gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland. This binding action reduces the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn decreases the production of testosterone. This mechanism of action is unique and provides a new approach to treating conditions such as prostate cancer, uterine fibroids, and endometriosis.
Approved indications
- Abnormal uterine bleeding due to uterine fibroid
- Lower abdominal pain
- Malignant tumor of prostate
- Menorrhagia
- Pain associated with endometriosis
- Uterine fibroids
Common side effects
- Hot flush
- Glucose increased
- Triglycerides increased
- Musculoskeletal pain
- Hemoglobin decreased
- Alanine aminotransferase increased (ALT)
- Fatigue
- Aspartate aminotransferase increased (AST)
- Constipation
- Diarrhea
- Myocardial infarction
- Acute kidney injury
Drug interactions
- P-gp Inhibitors
- P-gp Inhibitors
- P-gp Inhibitors
- Combined P-gp and Strong CYP3A Inducers
- Combined P-gp and Strong CYP3A Inducers
- P-gp Inhibitors
- Combined P-gp and Strong CYP3A Inducers
Key clinical trials
- Androgen Deprivation Therapy (Relugolix) for the Improvement of Diagnostic Imaging (PSMA PET/CT Scan) in Patients With High Risk or Very High Risk Prostate Cancer, The EnrichPSMA Trial (PHASE2)
- Supraphysiologic Testosterone Priming Induces Darolutamide Extended Response (PHASE2)
- NEPC Study: An Exploratory Safety and Efficacy Study With PSMA, SSTR2 and GRPR Targeted Radioligand Therapy in Metastatic Neuroendocrine Prostate Cancer. (PHASE1)
- Neoadjuvant High Dose Rate Brachytherapy Prior to Radical Prostatectomy in Patients With Prostate Cancer (PHASE1, PHASE2)
- Effects of Relugolix vs Leuprolide on Cardiac Function in Patients With Prostate Cancer (PHASE2)
- Comeback From Long coursE Androgen Deprivation Therapy (ADT) With RElugolix and Darolutamide (CLEARED) (PHASE2)
- Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT (PHASE2)
- Relugolix + Enzalutamide Study in High-Risk Prostate Cancer (PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
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 |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Orgovyx CI brief — competitive landscape report
- Orgovyx updates RSS · CI watch RSS
- MYOVANT SCIENCES portfolio CI