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A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
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Relugolix in treatment of prostate cancer: a review

Ioannis Kyriazis1, Themistoklis Bellos2, Stamatios Katsimperis1

  • 12nd Department of Urology, University of Athens, Sismanoglio General Hospital, Athens.

Archivio Italiano Di Urologia, Andrologia : Organo Ufficiale [Di] Societa Italiana Di Ecografia Urologica E Nefrologica
|November 17, 2025
PubMed
Abstract

Insights

Relugolix, an oral GnRH antagonist, offers rapid testosterone suppression for advanced prostate cancer without a flare. It demonstrates superior efficacy and cardiovascular safety compared to traditional therapies.

Area of Science:

  • Oncology
  • Endocrinology
  • Pharmacology

Background:

  • Androgen deprivation therapy (ADT) is a standard treatment for advanced prostate cancer.
  • Traditional injectable LHRH agonists carry risks like testosterone flare and cardiovascular events.
  • Relugolix is an oral GnRH antagonist designed for rapid testosterone suppression without a flare.

Purpose of the Study:

  • To review the efficacy, safety, and clinical utility of relugolix in advanced prostate cancer.
  • To synthesize current evidence on relugolix as an alternative ADT option.

Main Methods:

  • A non-systematic review of PubMed and MEDLINE databases up to July 2025.
  • Search terms included "relugolix," "ADT," "Androgen Deprivation Therapy," and "Prostate Cancer."
  • Inclusion of original studies published in English.

Main Results:

  • The HERO trial showed relugolix superior to leuprolide in sustained castration rates and onset speed.
  • Relugolix demonstrated a 54% reduction in major adverse cardiovascular events.
  • Equivalent efficacy to degarelix with improved testosterone recovery post-treatment was observed.

Conclusions:

  • Relugolix is a significant advancement in ADT, offering an oral, potent option.
  • It provides rapid action, a favorable cardiovascular safety profile, and better testosterone recovery.
  • Relugolix is a valuable choice for advanced prostate cancer, especially for patients with cardiovascular issues.
Keywords:
Androgenic, Deprivation, Prostate, Cancer, TreatmentBiochemical relapseCancer PatientsProstate Cancerandrogen deprivation therapy

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