Relugolix

Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone.

• ORGOVYX is indicated for the treatment of adult patients with advanced prostate cancer. ORGOVYX is a gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the treatment of adult patients with advanced prostate cancer ( 1 ).ICD-10: C61

• ORGOVYX is contraindicated in patients with severe hypersensitivity to relugolix or to any of the product components. Known severe hypersensitivity to relugolix or to any of the product components ( 4 ).contraindicated

Recommended Dosage: A loading dose of 360 mg on the first day of treatment followed by 120 mg taken orally once daily, at approximately the same time each day ( 2.1 ). ORGOVYX can be taken with or without food ( 2.1 , 12.3 ). Instruct patients to swallow tablets whole and not to crush or chew tablets ( 2.1 ). 2.1 Recommended Dosage Initiate treatment of ORGOVYX with a loading dose of 360 mg on the first day and continue treatment with a 120 mg dose taken orally once daily at approximately the same time each day. ORGOVYX can be taken with or without food [see Clinical Pharmacology ( 12.3 )] . Instruct patients to swallow tablets whole and not to crush or chew tablets. Advise patients to take a missed dose of ORGOVYX as soon as they remember. If the dose was missed by more than 12 hours, patients should not take the missed dose and resume with the next scheduled dose. If treatment with ORGOVYX is interrupted for greater than 7 days, restart ORGOVYX with a loading dose of 360 mg on the first day, and continue with a dose of 120 mg once daily. In patients treated with GnRH receptor agonists and antagonists for prostate cancer, treatment is usually continued upon development of nonmetastatic or metastatic castration-resistant prostate cancer. 2.2 Dosage Modifications for P-gp Inhibitors Avoid co-administration of ORGOVYX with oral P-gp inhibitors. If co-administration is unavoidable, take ORGOVYX first and separate dosing by at least 6 hours [ see Drug Interactions ( 7.1 ) and Clinical Pharmacology ( 12.3 ) ] . Monitor patients for increased adverse reactions.

QT/QTc Interval Prolongation: Androgen deprivation therapy may prolong the QT interval ( 5.1 ). Hypersensitivity: ORGOVYX can cause hypersensitivity reactions, including angioedema. Withhold ORGOVYX in patients who experience symptoms of hypersensitivity. Discontinue ORGOVYX for severe hypersensitivity reactions and manage as clinically indicated ( 5.2 ). Embryo-Fetal Toxicity: ORGOVYX can cause fetal harm. Advise males with female partners of reproductive potential to use effective contraception ( 5.3 , 8.1 , 8.3 ). 5.1 QT/QTc Interval Prolongation Androgen deprivation therapy, such as ORGOVYX, may prolong the QT/QTc interval. Providers should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, or frequent electrolyte abnormalities and in patients taking drugs known to prolong the QT interval. Electrolyte abnormalities should be corrected. Consider periodic monitoring of electrocardiograms and electrolytes [see Clinical Pharmacology ( 12.2 )]. 5.2 Hypersensitivity Reactions ORGOVYX is contraindicated in patients with severe hypersensitivity to relugolix or any of the product components [see Contraindications ( 4 )] . Hypersensitivity reactions, including pharyngeal edema and other serious cases of angioedema, have been reported postmarketing in patients treated with ORGOVYX. In HERO, patients treated with relugolix reported angioedema (0.2%) [see Clinical Trials Experience ( 6.1 )] .

The following clinically significant adverse reactions are described elsewhere in the labeling: QT/QTc Interval Prolongation [see Warnings and Precautions ( 5.1 )] . The most common adverse reactions (≥ 10%) and laboratory abnormalities (≥ 15%) were hot flush, glucose increased, triglycerides increased, musculoskeletal pain, hemoglobin decreased, alanine aminotransferase (ALT) increased, fatigue, aspartate aminotransferase (AST) increased, constipation, and diarrhea ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Sumitomo Pharma America, at 1-833-696-8268 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of ORGOVYX was evaluated in HERO, a randomized (2:1), open-label, clinical study in patients with advanced prostate cancer [see Clinical Studies ( 14 )] . Patients received orally administered ORGOVYX as a loading dose of 360 mg on the first day followed by 120 mg taken orally once daily (n = 622) or received leuprolide acetate administered by depot injection at doses of 22.5 mg (n = 264) or 11.25 mg (n = 44) per local guidelines every 12 weeks (n = 308). Leuprolide acetate 11.25 mg is a dosing regimen that is not recommended for this indication in the US. Among patients who received ORGOVYX, 91% were exposed for at least 48 weeks.

8.1 Pregnancy Risk Summary The safety and efficacy of ORGOVYX have not been established in females. Based on findings in animals and mechanism of action, ORGOVYX can cause fetal harm and loss of pregnancy when administered to a pregnant female [see Clinical Pharmacology ( 12.1 )] . There are no human data on the use of ORGOVYX in pregnant females to inform the drug-associated risk. In an animal reproduction study, oral administration of relugolix to pregnant rabbits during organogenesis caused embryo-fetal lethality at maternal exposures that were 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC ( see Data ). Advise patients of the potential risk to the fetus. Data Animal Data In an embryo-fetal development study, oral administration of relugolix to pregnant rabbits during the period of organogenesis resulted in abortion, total litter loss, or decreased number of live fetuses at a dose of 9 mg/kg/day (approximately 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC). 8.2 Lactation Risk Summary The safety and efficacy of ORGOVYX have not been established in females. Relugolix was detected in human breast milk ( see Data ). There are no data on the effects of relugolix or its metabolites on the breastfed child, or the effects on milk production.

Metabolism

After administration of single doses ranging from 60 mg to 360 mg (0.17 to 1 times the recommended loading dose), total systemic exposure (AUC) and the maximum concentration (C max ) of relugolix increases in an approximately dose proportional manner. After administration of multiple doses of relugolix once daily, the AUC of relugolix increases in an approximately dose proportional manner while the C max increase is greater than dose proportional for doses from 20 mg to 180 mg (0.17 to 1.5 times the recommended daily dose).

• Dec 18, 2020NDANDA214621Sumitomo Pharma Am
• May 26, 2021NDANDA214846Sumitomo Pharma Am

1. 1Hot Flush7,29630%
2. 2Fatigue5,59923%
3. 3Therapy Interrupted3,76716%
4. 4Incorrect Dose Administered2,0098.4%
5. 5Asthenia1,8697.8%
6. 6Arthralgia1,5176.3%
7. 7Diarrhoea1,4766.1%
8. 8Product Dose Omission Issue1,3045.4%
9. 9Dizziness1,2715.3%
10. 10Constipation9924.1%
11. 11Death9253.9%
12. 12Weight Increased8753.6%
13. 13Pain8503.5%
14. 14Insomnia8263.4%
15. 15Myalgia7763.2%

The 10 most recently updated of 77 ClinicalTrials.gov registrations naming Relugolix as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• The Effect of Medical Management Following Excisional Surgery for Endometriosis: A Randomized Controlled Trial
  Recruiting · Phase 3 · Interventional · 110 enrolled · Main Line Health
  NCT06439524updated 2026-06-12
• NEPC Study: An Exploratory Safety and Efficacy Study With PSMA, SSTR2 and GRPR Targeted Radioligand Therapy in Metastatic Neuroendocrine Prostate Cancer.
  Active not recruiting · Phase 1 · Interventional · 31 enrolled · Novartis Pharmaceuticals
  NCT06379217updated 2026-06-10
• Surgical Myomectomy Followed by Oral Myfembree Versus Standard of Care Trial (SOUL)
  Withdrawn · Phase 4 · Interventional · 0 enrolled · University of Chicago
  NCT05538689updated 2026-06-05
• Relugolix and Enzalutamide in Combination With Radiation Therapy for the Treatment of Very High Risk Prostate Cancer, OPTIMAL Trial
  Recruiting · Phase 2 · Interventional · 50 enrolled · Sean Sachdev
  NCT06499870updated 2026-06-05
• Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
  Recruiting · Phase 3 · Interventional · 804 enrolled · ECOG-ACRIN Cancer Research Group
  NCT04423211updated 2026-05-15
• Assessing Efficacy of Neoadjuvant ADT in Localized High-Risk Prostate Cancer Patients Utilizing 18F-Flotufolastat PSMA PET/CT
  Recruiting · Phase 2 · Interventional · 50 enrolled · Baptist Health South Florida
  NCT07455903updated 2026-05-13
• Study of the Safety and Contraceptive Efficacy of Relugolix Combination Therapy in Women With Uterine Fibroids or Endometriosis Who Are at Risk for Pregnancy
  Completed · Phase 3 · Interventional · 1,164 enrolled · Sumitomo Pharma Switzerland GmbH
  NCT04756037updated 2026-05-13
• The SUGAR Study; SBRT and Relugolix) for Prostate Cancer
  Recruiting · Phase 2 · Interventional · 60 enrolled · Yale University
  NCT06111781updated 2026-05-11
• Testing the Addition of the Drug Relugolix to the Usual Radiation Therapy for Advanced-Stage Prostate Cancer, The NRG Promethean Study
  Active not recruiting · Phase 2 · Interventional · 194 enrolled · NRG Oncology
  NCT05053152updated 2026-05-04
• Two Studies for Patients With Unfavorable Intermediate 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 Higher Gene Risk Score, The Guidance Trial
  Active not recruiting · Phase 3 · Interventional · 2,050 enrolled · NRG Oncology
  NCT05050084updated 2026-05-04

Frequently asked questions

How does Relugolix work?

Relugolix is a nonpeptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and consequently testosterone.

What is Relugolix used for?

According to FDA labeling, Relugolix carries indications including: ORGOVYX is indicated for the treatment of adult patients with advanced prostate cancer. ORGOVYX is a gonadotropin-releasing hormone (GnRH) receptor antagonist indicated for the treatment of adult patients with advanced prostate cancer ( 1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Relugolix?

Relugolix is classified as Other hormone antagonists and related agents, Gonadotropin Releasing Hormone Receptor Antagonist, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 2B6 Inducers, Cytochrome P450 3A Inducers, Gonadotropin Releasing Hormone Receptor Antagonists, P-Glycoprotein Inhibitors, Decreased GnRH Activity, Decreased GnRH Secretion.

What are the brand names for Relugolix?

Relugolix is marketed under brand names including Myfembree, Orgovyx.

What are the contraindications for Relugolix?

Relugolix labeling lists contraindications including: ORGOVYX is contraindicated in patients with severe hypersensitivity to relugolix or to any of the product components. Known severe hypersensitivity to relugolix or to any of the product components ( 4 ).. Always consult the full prescribing information and a clinician.