Palonosetron hydrochloride for the prevention of chemotherapy-induced nausea and vomiting

A large number of different 5-hydroxytryptamine (HT)₃ receptor antagonists have been marketed with the indication of preventing nausea and vomiting induced by chemotherapy - palonosetron is the most recently developed of these. Pharmacologic studies have revealed that palonosetron has a long half-life, a high affinity for 5-HT₃ receptors, exhibits allosteric binding to 5-HT₃ receptors and possess positive cooperativity. Although interesting, pharmacologic differences are only useful if they result in clinical advantages, such as an increase in efficacy and/or an improvement in tolerability. We summarize preclinical and clinical studies of palonosetron and compare the efficacy and tolerability with the other 5-HT₃ receptor antagonists, ondansetron, granisetron and dolasetron.