-5%
Religox is indicated for the management of adult patients with advanced prostate cancer.
Relugolix is a non-peptide, small-molecule GnRH receptor antagonist. It binds competitively to pituitary GnRH receptors, thereby reducing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This results in suppression of testosterone production, which is essential in controlling prostate cancer progression.
- Absorption: Oral bioavailability ~12%; Tmax ~2.25 hours.
- Food effect: High-fat meals do not significantly alter pharmacokinetics.
- Distribution: Plasma protein binding 68–71% (mainly to albumin).
- Metabolism: Primarily via CYP3A, minor by CYP2C8.
- Elimination: Effective half-life ~25 hours; terminal half-life ~61 hours.
- Excretion: ~81% via feces (4.2% unchanged), ~4.1% via urine (2.2% unchanged).
