https://doi.org/10.4081/aiua.2025.14277
Relugolix in treatment of prostate cancer: a review
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Published: 13 November 2025
Background: Androgen deprivation therapy (ADT) is a cornerstone treatment for advanced prostate cancer. While effective, traditional injectable luteinizing hormone-releasing hormone (LHRH) agonists are associated with an initial testosterone flare and potential cardiovascular risks. Relugolix is a novel, oral gonadotropin-releasing hormone (GnRH) antagonist developed to provide rapid suppression without a testosterone flare. This review synthesizes the latest evidence on the efficacy, safety, and clinical utility of relugolix.
Methods: This non-systematic review was conducted via a search of PubMed and MEDLINE databases up to July 2025 using the terms “relugolix” AND “ADT” OR “Androgen Deprivation Therapy” AND “Prostate Cancer.” Only original studies in English were included.
Results: The phase III HERO trial established the superiority of relugolix over leuprolide, demonstrating higher rates of sustained castration (96.7% vs 88.8%) and a significantly faster onset of action. Relugolix also showed a 54% reduction in major cardiovascular adverse events. Furthermore, it exhibited equivalent efficacy to injectable degarelix when combined with radiotherapy, but with more robust testosterone recovery after treatment cessation (52% vs 16%). Real-world data indicates high patient adherence to the oral regimen, and a cost-effectiveness analysis suggests it is a cost-effective option despite a higher drug cost.
Conclusions: Relugolix represents a significant advancement in ADT, offering a potent, oral alternative with a rapid onset of action, a superior cardiovascular safety profile, and improved testosterone recovery. It provides clinicians with a valuable option for treating advanced prostate cancer, particularly in patients with cardiovascular comorbidities.
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