FDA Approves Relugolix as First Oral Hormone Therapy for Advanced Prostate Cancer


Relugolix (Orgovyx) is the first oral drug in its class to receive FDA approval for the treatment of adults with advanced prostate cancer.

The FDA has approved relugolix (Orgovyx) as the first oral hormone therapy for the treatment of adults with advanced prostate cancer, according to an FDA press release.1

The safety and efficacy of relugolix was examined in the randomized, open-label phase 3 HERO trial (NCT03085095) in men with advanced prostate cancer.2 Participants randomly received either relugolix once daily or injections of leuprolide (Lupron), another hormone-targeting drug, every 3 months for 48 weeks.

The study was designed to establish if relugolix could achieve and maintain low enough castrate levels by day 29 through the end of the treatment course. Of the 622 patients who received relugolix, the castration rate was revealed to be 96.7%.

Regarding safety, the most common adverse events (AEs) observed with relugolix included hot flush (54%), increased glucose (44%), increased triglycerides (35%), musculoskeletal pain (30%), decreased hemoglobin (28%), fatigue (26%), constipation (12%), diarrhea (12%), and increased levels of certain liver enzymes.

“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,” 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, said in a press release. “This potential to reduce clinic visits can be especially beneficial in helping patients with cancer stay home and avoid exposure during the coronavirus pandemic.”

Importantly, concurrent use of relugolix with drugs that inhibit P-glycoprotein, which plays a role in pumping toxins out of cells, is contraindicated. According to the FDA, androgen deprivation therapies such as relugolix may affect the heart’s electrical properties or cause electrolyte abnormalities, thus healthcare providers should consider periodic monitoring of electrocardiograms and electrolytes.

Moreover, based on findings in animals and the agent’s mechanism of action, relugolix can cause fetal harm and loss of pregnancy when administered to a pregnant female. Therefore, it is advised that males with female partners of reproductive potential use effective contraception during treatment and for 2 weeks after the last dose of relugolix. Further, diagnostic test results of the pituitary gonadotropic and gonadal functions conducted during and after taking relugolix may be affected due to the drug’s suppression of the pituitary gonadal system.


1. FDA Approves First Oral Hormone Therapy for Treating Advanced Prostate Cancer [news release]. Published December 18, 2020. Accessed December 18, 2020. https://www.fda.gov/news-events/press-announcements/fda-approves-first-oral-hormone-therapy-treating-advanced-prostate-cancer?utm_medium=email&utm_source=govdelivery

2. FDA. HIGHLIGHTS OF PRESCRIBING INFORMATION. FDA website. Published December 2020. Accessed December 18, 2020. https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/214621s000lbl.pdf

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