Relugolix in treatment of prostate cancer: a review.
Kyriazis. Ioannis I; Bellos. Themistoklis T; Katsimperis. Stamatios S; Angelopoulos. Panagiotis P; Neofytoy. Panagiotis P; Varkarakis. Ioannis I; Skolarikos. Andreas A; Papatsoris. Athanasios A
Key Findings
- Relugolix achieved a higher rate of sustained castration (96.7%) compared with leuprolide (88.8%).
- It reduced major cardiovascular adverse events by 54% versus injectable hormone therapy.
- Testosterone recovery after stopping treatment was much better (52% vs 16%).
Practical Outcomes
- For men interested in hormone manipulation, relugolix shows that an oral GnRH antagonist can provide rapid testosterone suppression with a lower heart‑risk profile. It also suggests that stopping the drug may allow a quicker return of natural testosterone, which could be useful for managing long‑term hormone balance. The oral format improves adherence, making it a more convenient option than injections.
Summary
Relugolix is an oral drug that blocks the hormone signals that tell the testes to make testosterone. In advanced prostate cancer, it lowers testosterone faster and more reliably than the older injectable drugs, and it cuts the risk of serious heart problems by about half. It also lets testosterone bounce back more quickly after treatment stops, which could matter for men who care about hormone balance and heart health.
Abstract
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. 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. 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. 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.
Study Information
pubmed
2025
2025-11-13T00:00:00.000Z
10.4081/aiua.2025.14277
21