Chemotherapy-induced
nausea and
vomiting (CINV) are among the most feared and distressing symptoms experienced by patients with
cancer. The knowledge of the pathogenesis and neuropharmacology of CINV has expanded enormously over the last decades, the most significant discoveries being the role of
5-hydroxytryptamine (5-HT)(3)- and neurokinin (
NK)(1) receptors in the
emetic reflex arch. This has led to the development of two new classes of
antiemetics acting as highly selective antagonists at one of these receptors. These drugs have had a huge impact in the protection from
chemotherapy-induced
vomiting, whereas the effect on
nausea seems to be limited. The first
NK(1) receptor antagonist,
aprepitant, became clinically available in 2003, and
casopitant, the second in this class of
antiemetics, has now completed phase III trials. This review delineates the properties and clinical use of
casopitant in the prevention of CINV.