Relugolix (Myovant Sciences/Takeda) is a gonadotropin-releasing hormone (GnRH) receptor antagonist that directly inhibits GnRH receptors, rapidly reducing the circulating gonadotropin’s luteinizing hormone (LH) and follicle-stimulating hormone (FSH) and leading to the suppression of testosterone in men. This mechanism of action stands in contrast to GnRH agonists that, over time, down-regulate and desensitize GnRH receptors in the pituitary, leading to reduced secretion of LH and downstream testosterone. GnRH agonists are also accompanied by an initial surge in testosterone known as a flare that typically requires co-administration of antiandrogens to help prevent flare side effects such as skeletal pain, spinal cord compression, and, very rarely, death.
Relugolix is a GnRH receptor antagonist being trialed in androgen-sensitive advanced prostate cancer patients in the Phase III HERO trial. Relugolix is similar to the approved GnRH antagonist Firmagon (degarelix; Ferring/Astellas), as both drugs deplete androgen levels without an accompanying flare of testosterone that occurs with GnRH agonist treatment. Despite this advantage, GnRH agonists like leuprolide continue to dominate treatment of hormone-sensitive prostate cancer due to their established efficacy, physician familiarity, and convenient dosing schedules. Thus, relugolix faces competition not only from Firmagon, but from several GnRH agonists as well, which will significantly limit the drug’s commercial potential.
relugolix: Prostate cancer
List of Figures
Figure 1: Relugolix for prostate cancer - SWOT analysis
Figure 2: Drug assessment summary of relugolix for prostate cancer
Figure 3: Drug assessment summary of relugolix for prostate cancer
Figure 4: Relugolix sales for prostate cancer across the US, Japan, and five major EU markets, by country, 2017-26
List of Tables
Table 1: Relugolix drug profile
Table 2: Relugolix Phase III trials in prostate cancer
Table 3: Relugolix Phase II data in prostate cancer
Table 4: Relugolix sales for prostate cancer across the US, Japan, and five major EU markets, by country ($m), 2017-26