relugolix + ritonavir

Relugolix + ritonavir is an investigational drug combination being evaluated by the University of Chicago for the treatment of advanced prostate cancer. Relugolix is an oral, small-molecule gonadotropin-releasing hormone (GnRH) receptor antagonist that works by competitively binding to GnRH receptors in the anterior pituitary gland, thereby inhibiting the release of luteinizing hormone and follicle-stimulating hormone and suppressing testosterone production. Ritonavir is a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme and the P-glycoprotein (P-gp) efflux transporter. In this therapeutic regimen, ritonavir is utilized as a pharmacokinetic enhancer (booster) to increase the systemic exposure and prolong the half-life of relugolix. The primary goal of this combination is to enable a transition from the standard daily dosing of relugolix to a less frequent (e.g., weekly) schedule, potentially improving patient adherence and reducing the economic burden of treatment.

Brand names

OrgovyxNorvir

Other names

Relugolix and Ritonavir