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Palonosetron

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Management of Chemotherapy-Induced Nausea and Vomiting

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Abstract

With the recognition that the 5-hydroxytryptamine receptor was important in mediating cisplatin-induced emesis, work at several pharmaceutical companies focused on creating drugs that interfered with serotonin binding utilizing a variety of medicinal chemistry strategies. The first-generation 5-hydroxytryptamine receptor antagonists (5-HT3 RAs) ondansetron, granisetron, tropisetron, and dolasetron were structurally similar and showed activity in preventing chemotherapy-induced nausea and vomiting. However, complete response during the acute phase after cisplatin was achieved in only 50–70 % of patients and was substantially less effective in the delayed phase for control of both emesis and nausea. The first-generation 5-HT3 RAs do not improve control of delayed CINV over dexamethasone alone [1], nor does prolonged administration provide much additional benefit [2]. In addition, the first-generation 5-HT3 RAs were therapeutically equivalent with several large trials comparing these drugs to one another demonstrating similar efficacy [3, 4]. A plateau in 5-HT3 RA activity had been reached. Efforts persisted to find potentially more active agents based on the understanding of the central importance of this specific serotonin receptor in ameliorating chemotherapy-induced emesis.

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  1. Division of Hematology/Oncology, Department of Medicine, University of Tennessee Health Science Center, Memphis, TN, USA

    Lee Schwartzberg MD, FACP

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  1. Indiana University School of Medicine, South Bend, Indiana, USA

    Rudolph M. Navari

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Schwartzberg, L. (2016). Palonosetron. In: Navari, R. (eds) Management of Chemotherapy-Induced Nausea and Vomiting. Adis, Cham. https://doi.org/10.1007/978-3-319-27016-6_4

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