Orgovyx
Advanced prostate cancer.
Loading dose: 360 mg (three 120 mg tablets) orally on Day 1
Maintenance: 120 mg orally once daily
Take with or without food
Missed dose >24 hours: Testosterone may recover; consider re-loading
Tablets: 120 mg
None listed.
- QT/QTc Prolongation: Androgen deprivation therapy may prolong QTc. Consider risks vs benefits in patients with pre-existing QTc prolongation or risk factors.
- Cardiovascular Disease: ADT increases risk of MI, sudden cardiac death, and stroke. HERO trial showed lower major adverse cardiovascular events (MACE) vs leuprolide (2.9% vs 6.2%).
- Loss of Bone Mineral Density: Long-term ADT increases fracture risk. Consider DEXA scan.
- Hyperglycemia and Diabetes: Monitor blood glucose.
- Embryo-Fetal Toxicity
Hot flush (54%), musculoskeletal pain (30%), fatigue (26%), constipation (12%), diarrhea (12%), arthralgia (12%), decreased libido (5%), weight gain (3%)
Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.
Relugolix is a non-peptide, oral gonadotropin-releasing hormone (GnRH) receptor antagonist. It competitively binds to GnRH receptors in the anterior pituitary, directly blocking GnRH signaling without the initial stimulatory phase (testosterone surge/flare) seen with GnRH agonists (leuprolide, goserelin). This results in rapid suppression of LH, FSH, and consequently testosterone to castrate levels (typically within 4 days). Unlike injectable GnRH agonists, testosterone recovery upon discontinuation is faster (~90 days), and there is no flare phenomenon.
Tmax: 2-4 hours. Half-life: approximately 25 hours. Protein binding: 68-71%. Metabolized by CYP3A and P-gp (as substrate). Steady-state by Day 7. Excreted in feces (81%) and urine (4.1%). High-fat meals reduce Cmax by 28%.
Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.
- HERO — Relugolix vs. leuprolide in advanced prostate cancer. Phase III, n=930.