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Updated: Sep 12, 2025

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
GnRH Antagonists: Current Evidence and Role in Prostate Cancer
Antonio Lazo1, Manuel Blanco2, Abrahams Ocanto3
1Department of Radiation Oncology, Hospital Universitario Virgen de la Victoria, 29010 Malaga, Spain.
Gonadotropin-releasing hormone (GnRH) antagonists offer rapid testosterone suppression for prostate cancer (PCa) without flare. However, their long-term efficacy and safety, especially cardiovascular risks, require further investigation.
Area of Science:
- Oncology
- Endocrinology
- Pharmacology
Background:
- Androgen deprivation therapy (ADT) is a cornerstone in prostate cancer (PCa) management.
- Gonadotropin-releasing hormone (GnRH) agonists are the most common ADT, but GnRH antagonists offer an alternative.
- Antagonists provide rapid testosterone suppression without the initial flare effect seen with agonists.
Purpose of the Study:
- To provide a comprehensive literature review on the role of GnRH antagonists in PCa management.
- To highlight the potential benefits and limitations of GnRH antagonists.
- To address existing controversies regarding their efficacy and safety.
Main Methods:
- Narrative literature review.
- Analysis of existing clinical evidence and studies on GnRH antagonists (degarelix, relugolix).
- Evaluation of testosterone suppression, recovery, and cardiovascular risk profiles.
Main Results:
- GnRH antagonists achieve rapid testosterone suppression without flare.
- Relugolix (oral antagonist) shows rapid testosterone recovery post-treatment and potential for lower cardiovascular risk.
- Evidence on superiority over agonists in clinical outcomes and side effects is limited and sometimes contradictory.
Conclusions:
- GnRH antagonists represent a valuable option for personalized PCa treatment.
- Further long-term prospective studies are essential to confirm efficacy, safety, and cardiovascular risks.
- The definitive role of antagonists in various PCa stages and combination therapies needs further validation.
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