casopitant + ketoconazole

casopitant + ketoconazole is a combination resulting from co-administration of casopitant, a highly selective and orally bioavailable neurokinin-1 (NK-1) receptor antagonist developed by GlaxoSmithKline, with ketoconazole, a potent oral antifungal agent and a strong inhibitor of cytochrome P450 3A4 (CYP3A4). While no fixed-dose co-formulation exists, this combination is examined primarily in the context of pharmacokinetic drug interaction studies. Casopitant is indicated for the prevention of chemotherapy-induced and postoperative nausea and vomiting. When administered with ketoconazole, systemic exposure of casopitant is markedly increased due to CYP3A4 inhibition, which may elevate the risk of adverse effects such as QTc interval prolongation.

Brand names

Zunrisa (for casopitant; no fixed-dose combination with ketoconazole)

Other names

casopitant plus ketoconazole