A Systematic Review on Analytical Method Development and Validation for Relugolix

Relugolix is an orally active, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of advanced prostate cancer. It produces rapid suppression of testosterone levels by directly blocking pituitary GnRH receptors, without causing an initial hormonal flare. The oral administration of relugolix offers improved convenience compared to injectable androgen-deprivation therapies. This review article summarizes the pharmacological profile of relugolix, including its mechanism of action, pharmacokinetics, pharmacodynamics, adverse effects, and drug interactions. In addition, various reported analytical methods such as UV spectrophotometry, HPLC, UPLC, LC-MS/MS, and GC-MS for the estimation and quality control of relugolix in bulk drug and pharmaceutical dosage forms are reviewed.