Indication
Prostate cancer, advanced
Dose
Prostate cancer, advanced
- Dose - Oral: Loading dose of 360 mg on day 1, followed by 120 mg once daily continuously until disease progression or unacceptable toxicity
- If treatment is interrupted for more than 7 days the loading dose must be repeated on day 1, followed by 120 mg once daily thereafter
Supplied
Available as 120 film-coated tablets. Tablets should NOT be crushed or broken. Store at room temperature in original bottle with desiccant and protect from light and moisture.
Pharmacological Category
Gonadotropin-Releasing Hormone Antagonist
Administration
Take with or without food
Missed Dose
If a dose is missed, patients should be instructed to take it as soon as they can if it is within 12 hours of the missed dose. If it is over 12 hours since the missed dose, patients should skip the missed dose and resume with the next scheduled dose.
Adverse Effects
Common: Hypersensitivity reactions, Glucose increase, Triglycerides increase, Hot flashes, Fatigue.
Less Common: Constipation, Diarrhea, Hemoglobin decrease, QT prolongation, Osteopenia/Osteoporosis, Decreased libido, Erectile dysfunction, Cardiac events (stroke, myocardial infarction).
The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.
Monitoring Parameters
Baseline before treatment: CBC & differential, platelets, PSA, creatinine, ALT, bilirubin, alkaline phosphatase, ECG, potassium, calcium, magnesium, glucose, triglycerides.
During treatment: ECG, potassium, calcium, magnesium, PSA.
If clinically indicated: ECG, potassium, calcium, magnesium, glucose, triglycerides.
Drug Interactions
This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
May increase the risk for QT interval prolongation. Avoid concurrent therapy with drugs associated with QTc prolongation and/or Torsades de pointes, if possible. If unavoidable, monitor for QT prolongation or cardiac arrhythmias.
Current drug interaction databases should be consulted for more information.
Clinical Pearls
Avoid in pregnancy and lactation.
Hot flashes are a common adverse event with relugolix, and may be controlled in some patients using non-pharmacological or pharmacological options to decrease the frequency and severity.
Patients with diabetes may be at an increased risk of insulin resistance while taking relugolix and may require increased glucose monitoring.
References
BC Cancer. BCCancer Drug Manual. Relugolix. Vancouver, British Columbia: BC Cancer Agency.Available at http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Relugolix_monograph.pdf:Developed December 1, 2024. Accessed February 19, 2025.
Sumitomo Pharma. Orgovyx Product Monograph. In: Health Canada, Drug Product Database. Available at: https://pdf.hres.ca/dpd_pm/00073150.PDF Updated October 30th,2023. Accessed February 19th, 2025.
