Yes.The US Food and Drug Administration on 18 December 2020 approved the first oral gonadotropin-releasing hormone (GnRH) receptor antagonist, relugolix for adult patients with advanced prostate cancer.

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.

The most common adverse reactions (≥10%) in patients receiving relugolix in HERO were hot flush, musculoskeletal pain, fatigue, diarrhea, and constipation. The most common laboratory abnormalities (≥15%) were increased glucose, triglycerides, alanine aminotransferase, and aspartate aminotransferase. Decreased hemoglobin was also observed. The recommended relugolix dose is a loading dose of 360 mg on the first day followed by a daily oral dose of 120 mg at approximately the same time with or without food.

References:

[1] SHIRLEY M. Relugolix: A Review in Advanced Prostate Cancer.[J]. Targeted Oncology, 2023. DOI:10.1007/s11523-022-00944-4.