Relugolix for the treatment of prostate cancer

Androgen deprivation therapy consists of the cornerstone of prostate cancer medical treatment. Until recently, castration of hypothalamus-hypophysis-gonadal axial was based on injectable medical agents. A few years ago, a novel per os administered GnRH antagonist was approved leading testosterone to castration level. Relugolix was approved by FDA in 2020, and it is the first per os administered GnRH antagonist. The present study is a literature review of the efficacy, safety and clinical perspectives of relugolix.

A literature narrative review was conducted using PubMed/MEDLINE, Scopus, and the Cochrane library. Studies written in English language, considering efficacy, safety and cost-effectiveness of relugolix compared with other androgen deprivation therapies were included in the review.

Recent studies have examined efficacy of relugolix revealing a testosterone suppression percentage of 78.4% after 48 weeks from treatment initiation. Moreover, relugolix has been associated with less major cardiovascular events as well as better rate of testosterone recovery after treatment completion compared with the GnRH agonists. However, there is no head-to-head trial comparing relugolix with injectable GnRH antagonists, so far. As a result, a trial comparing the methods of antagonists' administration should be performed in the future.