The Food and Drug Administration (FDA) has approved OrgovyxTM (relugolix tablets; Myovant Sciences) for the treatment of adult patients with advanced prostate cancer.

Orgovyx is an oral nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist that competitively binds to pituitary GnRH receptors, thereby, reducing the release of luteinizing hormone and follicle-stimulating hormone, and consequently testosterone. The approval was based on data from the HERO trial, an open-label study in men with advanced prostate cancer requiring at least 1 year of androgen deprivation therapy and defined as biochemical (PSA) or clinical relapse following local primary intervention, newly diagnosed castration-sensitive metastatic disease, or advanced localized disease.

Patients were randomized to receive Orgovyx (n=622) or leuprolide acetate injection (n=308) for 48 weeks. The primary end point of the study was medical castration rate, defined as achieving and maintaining serum testosterone suppression to castrate levels (<50ng/dL) by day 29 through 48 weeks of treatment.

Results through week 48 showed a castration rate of 96.7% (95% CI, 94.9-97.9) in the Orgovyx arm vs 88.8% (95% CI, 84.6-91.8) in the leuprolide acetate group. By day 29, testosterone levels of less than 50ng/dL and less than 20ng/dL were attained by 99% and 95% of Orgovyx-treated patients, respectively, compared with 82% and 57% of leuprolide-treated patients. Additionally, PSA levels were observed to be on average 65%, 83%, and 92% lower after 2 weeks, 4 weeks, and 3 months of Orgovyx treatment, respectively.

The most common adverse reactions reported in the study included hot flush, increased glucose increased, increased triglycerides, musculoskeletal pain, decreased hemoglobin, increased alanine aminotransferase (ALT), fatigue, increased aspartate aminotransferase (AST), constipation, and diarrhea. Additionally, the treatment may prolong the QT/QTc interval.

Orgovyx is supplied as 120mg tablets and is expected to be available in January 2021.

“Today’s approval marks the first oral drug in this class and it may eliminate some patients’ need to visit the clinic for treatments that require administration by a health care provider,” said Richard Pazdur, MD, director of the FDA’s Oncology Center of Excellence and acting director of the Office of Oncologic Diseases in the FDA’s Center for Drug Evaluation and Research.

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1.      FDA approves first oral hormone therapy for treating advanced prostate cancer. [press release]. December 18, 2020.

2.      Myovant Sciences announces FDA approval of ORGOVYX™ (relugolix), the first and only oral gonadotropin-releasing hormone (GnRH) receptor antagonist for advanced prostate cancer. [press release]. December 18, 2020.

3.      Orgovyx prescribing information. Brisbane, CA: Myovant Sciences; 2020.