Relugolix

DAE Class; Rx

Common Brand Names; Orgovyx

• Antineoplastics, GNRH Antagonists

Gonadotropin-releasing hormone (GnRH) receptor antagonist; binds to and blocks GnRH receptors in the anterior pituitary gland

Blocking GnRH receptors decreases the release of gonadotropins (ie, luteinizing hormone, follicle stimulating hormone), thereby decreasing the downstream production of testosterone by the testes in men

Indicated for advanced prostate cancer

None

>10%

All grades

• Hot flush (54%)
• Glucose increased (44%)
• Triglycerides increased (35%)
• Musculoskeletal pain (30%)
• Hemoglobin decreased (28%)
• ALT increased (27%)
• Fatigue (26%)
• AST increased (18%)
• Diarrhea (12%)
• Constipation (12%)

1-10%

All grades

• Increased weight (<10%)
• Insomnia (<10%)
• Gynecomastia (<10%)
• Hyperhidrosis (<10%)
• Depression (<10%)
• Decreased libido (<10%)

Grade 3-4

• Glucose increased (2.9%)
• Triglycerides increased (2%)
• Musculoskeletal pain (1.1%)

<1%

Grade 3-4

• Hot flush
• Fatigue
• Diarrhea
• ALT increased
• Hemoglobin increased

Based animal studies and mechanism of action, fetal harm may occur

Therapy suppresses pituitary gonadal system; results of diagnostic tests conducted during and after treatment may be affected; monitor therapeutic effect of relugolix by measuring serum concentrations of prostate specific antigen (PSA) periodically; if PSA increases, measure serum testosterone concentrations

Hypersensitivity reactions, including pharyngeal edema and other serious cases of angioedema, reported; advise patients who experience any symptoms of hypersensitivity to temporarily discontinue therapy and promptly seek medical care; discontinue therapy for severe hypersensitivity reactions and manage as clinically indicated

Pregnancy

Based on findings in animals and mechanism of action, can cause fetal harm and loss of pregnancy when administered to pregnant females

Human data are unavailable

Lactation

Data are unavailable on presence in human milk, effects on breastfed children, or effects on milk production

Relugolix and/or its metabolites were present in milk of lactating rats at concentrations up to 10-fold higher than in plasma at 2 hr post dose

Prostate Cancer

Indicated for advanced prostate cancer

Day 1 loading dose: 360 mg PO

Maintenance dose: 120 mg PO qDay

Dosing Considerations

Correct electrolyte abnormalities

Consider periodic ECG and electrolyte monitoring

Males with female partners of reproductive potential should use effective contraception

Relugolix