Generic
Relugolix
4 brands available in the market
At a glance
Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used for the treatment of advanced prostate cancer. It competitively binds to pituitary GnRH receptors, reducing LH and FSH release, and consequently testosterone.
Description
Relugolix is a non-peptide small molecule GnRH receptor antagonist. It competitively binds to pituitary GnRH receptors, reducing LH and FSH release and decreasing testosterone. Plasma protein binding is 68-71% and effective half-life is 25 hours.
Indications
- Advanced prostate cancer
Therapeutic class
Gonadotropin-releasing hormone (GnRH) antagonist
Pharmacological class
GnRH Receptor Antagonist
Pharmacology
Relugolix is a non-peptide small molecule GnRH receptor antagonist that competitively binds to pituitary GnRH receptors. It reduces LH and FSH release, decreasing testosterone production, which slows prostate cancer growth.
Mechanism of action
Reduces testosterone production by blocking pituitary GnRH receptors.
Dosage
Adult Dose (Oral):
- Loading dose: 360 mg on the first day
- Maintenance dose: 120 mg once daily (at approximately the same time each day)
- Can be taken with or without food
- Missed dose: If >12 hours, skip and resume with next scheduled dose
- If treatment interrupted for >7 days, restart with loading dose
Administration
- Take at approximately the same time each day
- Swallow tablet whole; do not chew, crush, or break
Missed dose
If you miss a dose, take it as soon as you remember; if >12 hours, skip it; do not double the dose.
Side effects
Common Side Effects (≥10%):
- Hot flushes
- Increased glucose
- Increased triglycerides
- Musculoskeletal pain
- Decreased hemoglobin
- Increased ALT
- Fatigue
- Increased AST
- Constipation
- Diarrhea
Precautions & warnings
- QT/QTc interval may be prolonged (androgen deprivation therapy)
- Embryo-fetal toxicity: Can cause fetal harm; males with female partners of reproductive potential should use effective contraception
- Do not use during pregnancy
Contraindications
- Hypersensitivity to relugolix or any component
Drug interactions
- P-gp inhibitors: Avoid co-administration; if unavoidable, take relugolix first, separate by at least 6 hours
- P-gp + strong CYP3A inducers: Avoid; if unavoidable, increase dose to 240 mg/day
Food interactions
Food does not affect absorption; it is not known whether it is safe to consume alcohol.
Use in pregnancy
Use in Pregnancy: Safety not established; can cause fetal harm; do not use.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if excreted in human milk; do not use during breastfeeding.
Pediatric use
Safety and efficacy not established in pediatric patients.
Geriatric use
No overall differences in safety or effectiveness between older and younger subjects.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed; consult your doctor.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed; consult your doctor.
Overdose effects
No specific experience in management of overdose; consult your doctor if taken in excess.
Storage conditions
Store in a cool and dry place, protected from light and moisture; keep out of reach of children.
Chemical structure
Relugolix