Related Experiment Video
Updated: Oct 10, 2025

Reproductive Techniques for Ovarian Monitoring and Control in Amphibians
Published on: May 12, 2019
Relugolix: A new kid on the block among gonadotrophin-releasing hormone antagonists
Charalampos Fragkoulis1, Ioannis Glykas1, Athanasios Dellis2
1Department of Urology, General Hospital of Athens 'G. Gennimatas', Mesogeion Avenue 154, Athens, P.C, 115 27, Greece.
Abstract:
Androgen-deprivation therapy (ADT) is the cornerstone of metastatic prostate cancer treatment. ADT can be achieved through surgical castration, or it may be induced either by gonadotrophin-releasing hormone (GnRH) agonists or GnRH antagonists. GnRH antagonists provide a more rapid castration alongside with a safer profile regarding adverse events. Degarelix is the sole GnRH antagonist used in clinical practice. Injection site reactions are the commonest adverse events related to the use of degarelix. Relugolix, a novel molecule, represents the first orally administered United States Food and Drug Administration approved GnRH antagonist, with clinical efficacy equal to that of the established ADT regimens. The main advantages of relugolix are the avoidance of the injection site reactions of GnRH antagonists such as degarelix alongside its patient-friendly oral administration. The aim of the present review article is to present novel data regarding the role of relugolix as ADT for the treatment of prostate cancer. Abbreviations: ADT: androgen-deprivation therapy; FDA: United States Food and Drug Administration.
Insights
Androgen-deprivation therapy (ADT) for metastatic prostate cancer now includes relugolix, an oral gonadotrophin-releasing hormone (GnRH) antagonist. This novel treatment offers efficacy comparable to existing methods while avoiding injection site reactions associated with other GnRH antagonists.
Area of Science:
- Oncology
- Endocrinology
Background:
- Androgen-deprivation therapy (ADT) is crucial for metastatic prostate cancer.
- Gonadotrophin-releasing hormone (GnRH) antagonists offer rapid castration with fewer adverse events than agonists.
- Degarelix is the only currently used GnRH antagonist, with injection site reactions being common.
Purpose of the Study:
- To review novel data on relugolix as an ADT for prostate cancer.
- To highlight the advantages of oral administration and reduced adverse events.
- To present relugolix as a new therapeutic option in prostate cancer management.
Main Methods:
- Review of clinical data and studies on relugolix.
- Comparison of relugolix efficacy and safety profile with existing ADT regimens.
- Analysis of patient-reported outcomes and administration convenience.
Main Results:
- Relugolix is the first orally administered GnRH antagonist approved by the FDA.
- Clinical efficacy of relugolix is equivalent to established ADT regimens.
- Relugolix avoids injection site reactions common with GnRH antagonists like degarelix.
Conclusions:
- Relugolix offers a patient-friendly oral alternative for ADT in prostate cancer.
- It provides comparable efficacy to injectable GnRH antagonists and agonists.
- The avoidance of injection site reactions represents a significant advantage for patient compliance and quality of life.
Related Concept Videos
Gonadal and Placental Hormones
In males, testosterone is the primary gonadal androgen. It plays a central role in the maturation of male reproductive organs — the penis and testes. Additionally, testosterone is instrumental in the development of secondary sexual characteristics — a deep voice as well as facial and pubic hair...
Hormonal Regulation of the Menstrual Cycle
At puberty, GnRH begins a pulsatile release pattern, which triggers the anterior pituitary gland to secrete follicle-stimulating hormone (FSH) and luteinizing hormone (LH). The frequency and amplitude of GnRH pulses vary across the menstrual cycle, with faster pulses favoring LH release and slower pulses favoring FSH...
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
Hormonal Control of the Ovarian Cycle
Before puberty, the hypothalamus releases GnRH in a low frequency, low amplitude pulsatile manner. This along with the immature hypothalamic-pituitary-gonadal axis activity, results in low estrogen levels and the absence of a fully functional ovarian cycle. At puberty, GnRH secretion increases in both frequency and...
Ovarian Cycle
Testosterone: Functions and Regulation

