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Review
. 2023 Mar;18(2):295-302.
doi: 10.1007/s11523-022-00944-4. Epub 2023 Jan 18.

Relugolix: A Review in Advanced Prostate Cancer

Matt Shirley  1
Affiliations
Review

Relugolix: A Review in Advanced Prostate Cancer

Matt Shirley. Target Oncol. 2023 Mar.

Erratum in

Abstract

Relugolix (Orgovyx®), an orally active nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist that provides rapid testosterone suppression, is indicated in the USA for the treatment of advanced prostate cancer and in the EU for advanced hormone-sensitive prostate cancer. In the pivotal phase III HERO trial in men with advanced prostate cancer, once-daily oral relugolix (with a loading dose on day 1) led to a sustained castration rate over 48 weeks of treatment of > 90%, a rate that was non-inferior to that provided by intramuscular leuprolide depot every 3 months (with an exploratory analysis further indicating the superiority of relugolix over leuprolide). Relugolix was generally well tolerated, having an adverse event profile that is consistent with testosterone suppression. Furthermore, there is evidence that relugolix may be associated with a lower risk of major adverse cardiac events compared with leuprolide. With the ability to provide the rapid testosterone suppression (with no initial surge in testosterone upon treatment initiation) combined with the benefits of oral administration and potentially improved cardiac safety, relugolix presents a valuable treatment option for men with advanced prostate cancer where androgen deprivation therapy is indicated.

Plain language summary

Androgen deprivation therapy (ADT), a key component of prostate cancer treatment, reduces testosterone production to slow disease progression. Relugolix (Orgovyx®), from a class of drugs known as gonadotropin-releasing hormone (GnRH) receptor antagonists, is approved for the treatment of advanced prostate cancer. Whereas some ADT agents (i.e. GnRH agonists) produce an initial surge in testosterone levels (with the potential to cause a flare in disease symptoms), GnRH receptor antagonists, of which relugolix is the first available as an oral medication, provide rapid testosterone suppression with no initial surge. In a key clinical trial in men with advanced prostate cancer, once-daily relugolix provided sustained castration in > 90% of patients, with a sustained castration rate that was non-inferior to that of a comparator agent (leuprolide) administered by intramuscular injection every 3 months. Relugolix was generally well tolerated and may be associated with a lower risk of major adverse cardiac events than leuprolide. Providing rapid and sustained testosterone suppression, combined with the benefits of oral administration and potentially improved cardiac safety, relugolix presents a valuable treatment option for ADT in men with advanced prostate cancer.

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Conflict of interest statement

Matt Shirley is a salaried employee of Adis International Ltd/Springer Nature, and declares no relevant conflicts of interest. All authors contributed to the review and are responsible for the article content.

Figures

Fig. 1
Fig. 1
Trial design of the randomized, open-label, active-controlled phase III HERO trial in patients with advanced prostate cancer [12]. The primary endpoint of the trial was the sustained castration rate (defined as the cumulative probability of testosterone suppression to < 50 ng/dL) from day 29 through 48 weeks. Efficacy results are reported in the animated figure (available online). BGD between-group difference, mo months, pts patients
Fig. 2
Fig. 2
Adverse events (AEs) occurring in > 10% of patients in either treatment group in the phase III HERO trial [12].
See this image and copyright information in PMC

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