Relugolix

Indications

Relugolix is used for: Prostate Cancer

Adult Dose

Prostate Cancer Indicated for advanced prostate cancer Day 1 loading dose: 360 mg PO Maintenance dose: 120 mg PO once a Day Hepatic impairment Mild-to-moderate (Child-Pugh A or B): No dosage adjustment required Severe (Child-Pugh C): Not studied

Child Dose

Renal Dose

Renal impairment Mild-to-severe (CrCl 15-89 mL/min): No dosage adjustment required End-stage renal disease with or without hemodialysis: Not studied

Administration

Take at approximately the same time each day May take with or without food

Contra Indications

Precautions

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 QT/QTc interval prolongation Androgen deprivation therapy may prolong QT/QTc interval Consider benefits and risks in patients with congenital long QT syndrome, congestive heart failure, or frequent electrolyte abnormalities, and those taking drugs known to prolong QT interval Correct electrolyte abnormalities Consider periodic ECG and electrolyte monitoring

Pregnancy-Lactation

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 Animal studies Administration to pregnant rabbits during organogenesis caused embryofetal lethality at maternal exposures that were 0.3 times the human exposure at the recommended dose of 120 mg daily based on AUC Contraception Males with female partners of reproductive potential: Use effective contraception during treatment and for 2 weeks after last dose Infertility Based on findings in animals and mechanism of action, may impair fertility in males of reproductive potential 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

Interactions

Side Effects

Side effects of Relugolix : >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

Mode of Action

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