Relugolix is a non-peptide, orally active gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by binding to GnRH receptors in the pituitary gland. This action reduces the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn decreases the production of testosterone. By lowering testosterone levels, relugolix slows or stops the growth of prostate cancer cells that require this hormone to grow.

Relugolix is indicated for the treatment of adult patients with advanced prostate cancer. It is administered as a once-daily oral tablet. As a GnRH receptor antagonist, relugolix offers a rapid onset of action and avoids the testosterone flare associated with GnRH agonists, representing a significant advancement in the management of hormone-sensitive prostate cancer.