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

Abstract

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.

Keywords::

• 5-hydroxytryptamine receptor antagonist
• chemotherapy
• emesis
• nausea
• palonosetron hydrochloride
• RS 25259–197

Financial & competing interests disclosure

Jørn Herrstedt was previously (2008 and earlier) an ad hoc consultant (no running contracts) to Merck, GSK, Helsinn, Schering-Plough and Amgen, and received speakers’ honoraria from Merck and GSK in 2009. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.