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relugolix

nonpeptide GnRH antagonist · Antineoplastic agent

nonpeptide GnRH antagonistAntineoplastic agentATC null
CDSCO approved
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
X
FDA category + note
Top interactionssee all 12
  • AzithromycinSevereDatabaseDDInter
  • BedaquilineSevereDatabaseDDInter
  • CabozantinibSevereDatabaseDDInter
  • CapmatinibSevereDatabaseDDInter

Mechanism

Relugolix is an orally available, nonpeptide GnRH antagonist that antagonizes the GnRH receptor by reversible competition with GnRH. This results in rapid reduction in LH and FSH secretion from the pituitary and concomitant loss of testosterone production to castrate levels from the testes. It avoids the initial testosterone surge seen with GnRH agonists and is more effective at suppressing FSH.

Indications

Treatment of prostate cancer (FDA-approved)

Dosing

Adult
Initial oral loading dose (360 mg), followed by one tablet (120 mg) daily.

Pharmacokinetics

Onset
Steady-state levels are achieved after 7 days.
Bioavailability
Food can diminish oral bioavailability by 50%.
Metabolism
Predominant metabolizer is CYP3A4. Absorption and distribution are influenced by the efflux transporter P-glycoprotein (Pgp).
Excretion
Metabolites are excreted mainly in feces.

Contraindications

  • Women of childbearing potential (male patients with female partners of reproductive potential should use contraception during and for 2 weeks following the last dose due to reproductive and fetal harm in animal toxicity tests)

Side effects

Common
Hot flushesIncreased blood glucose levelsIncreased triglyceride levelsMusculoskeletal painAnemiaIncreased liver enzymesTirednessConstipationDiarrhea
Serious
  • Prolongation of the cardiac QT/QTc interval
  • Reproductive and fetal harm (in animal toxicity tests)

Pregnancy & lactation

Pregnancy

X

Drug interactions

Azithromycin
Severe
Database

Drug interaction classified as: synergy, absorption

Source: DDInter

Bedaquiline
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cabozantinib
Severe
Database

Drug interaction classified as: synergy, absorption

Source: DDInter

Capmatinib
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Carvedilol
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Citalopram
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clarithromycin
Severe
Database

Drug interaction classified as: synergy, absorption

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: absorption

Source: DDInter

Crizotinib
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team