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Palonosetron as an anti-emetic and anti-nausea agent in oncology

Authors Matti S Aapro

Published 15 January 2008 Volume 2007:3(6) Pages 1009—1020

Matti S Aapro

Clinique de Genolier, Genolier, Switzerland

Abstract: Palonosetron (Aloxi®, Onicit®, Paloxi®) is a second-generation 5-HT3 receptor antagonist (RA) with an extended half-life of ~40 hours and high binding affi nity for the 5-HT3 receptor that is markedly different from other 5-HT3 RAs. Phase III trials demonstrate that a single dose of palonosetron compared with traditional 5-HT3 RAs is more effective in preventing chemotherapy-induced nausea and vomiting (CINV) during the first 24 hours following chemotherapy (acute CINV), and also exhibits prolonged efficacy to provide significantly better protection from CINV in the delayed and overall phases. This superior and extended protection from CINV conferred by palonosetron following a single intravenous dose before chemotherapy simplifies dosing schedules. Recent research has focused on optimization of palonosetron-based antiemetic regimens, particularly in combination with steroids and neurokinin-1 RAs. The available clinical data indicate high control rates for palonosetron, suggesting a synergistic potential for protection in patients scheduled to receive emetogenic drug regimens.

Keywords: palonosetron, CINV, 5-HT3 receptor antagonists, moderately emetogenic chemotherapy (MEC), highly emetogenic chemotherapy (HEC)

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