FDA approved the first ever oral formulation of Relugolix (a gonadotropin-releasing hormone antagonist) on 18th December, 2020 for the treatment of advanced prostate cancer.

The existing FDA-approved therapies for prostate cancer are either injected or positioned as small implants under the skin rendering it inconvenient and requiring clinic visits for its administration. But, Relugolix may be helpful in decreasing clinic visits and can be particularly effective in helping patients with cancer stay home and dodge exposure during the COVID-19 pandemic.

Relugolix works by preventing the pituitary gland from making luteinizing (LSH) and follicle-stimulating hormone (FSH), thus reducing testosterone production.

The effectiveness of Relugolix was examined in a randomized, open-label trial comprising of advanced prostate cancer patients. Patients were either given Relugolix OD or leuprolide injections, every 3 months for a period of 48 weeks’. This trial aimed to reveal if Relugolix attained and sustained low enough testosterone levels (castrate levels) by day 29 through end of treatment period. A 96.7% castration rate was observed in 622 patients who received Relugolix.

Augmented glucose and triglycerides; hot flush; musculoskeletal pain; decreased hemoglobin, weakness, diarrhea, constipation, etc. were some commonly described side effects. Physicians should consider regular monitoring of electrocardiograms and electrolytes as Relugolix may cause electrolyte anomalies. As it can induce harmful effects in pregnant female, caution needs to be taken considering contraception as directed by the physician.