Relugolix (brand name Relugolix) has been approved for the treatment of advanced prostate cancer in adult patients. Relugolix is the first oral gonadotropin-releasing hormone (GnRH) receptor antagonist.

Relugolix is an orally active, non-peptide GnRH antagonist that binds to and blocks GnRH receptors in the anterior pituitary, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to a decrease in estrogen production by the ovaries in women and the production of testosterone by the testes in men.

In terms of major cardiovascular events, Relugolix outperformed leuprolide acetate (brand name Lupron), with data showing that the incidence of cardiovascular events was 2.9% for Relugolix tablets, compared to 6.2% for the leuprolide acetate treatment group. Furthermore, compared to leuprolide acetate, Relugolix has a faster onset of action (8 days vs. 30 days), a higher efficacy rate (96.7% vs. 88.8%), no "flare effect," and the advantage of maintaining bone density.