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Netupitant/Palonosetron: A Review in the Prevention of Chemotherapy-Induced Nausea and Vomiting

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Abstract

An oral fixed combination of netupitant/palonosetron (NEPA; Akynzeo®) is available for use in the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Netupitant is a highly selective neurokinin-1 receptor antagonist and palonosetron is a serotonin 5-HT3 receptor antagonist with a distinct pharmacological profile. Complete response rates during the delayed, acute and overall phases were significantly higher with single-dose netupitant 300 mg plus palonosetron 0.5 mg than with single-dose palonosetron 0.5 mg in cycle 1 of cisplatin-based highly emetogenic chemotherapy (HEC) in a phase II trial and with single-dose netupitant/palonosetron 300/0.5 mg than with single-dose palonosetron 0.5 mg in cycle 1 of anthracycline–cyclophosphamide (AC) moderately emetogenic chemotherapy (MEC) in a phase III trial; the greater efficacy of netupitant/palonosetron was maintained over repeated cycles of AC MEC in the phase III trial. In another phase III trial, netupitant/palonosetron 300/0.5 mg was effective over repeated cycles of non-AC MEC or HEC. Netupitant/palonosetron was well tolerated, with no cardiac safety concerns. The convenience of administering netupitant/palonosetron as a single dose in a fixed combination has the potential to improve adherence to CINV prevention guidelines. In conclusion, netupitant/palonosetron is an important option to consider in the prevention of acute and delayed CINV in patients receiving MEC or HEC.

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Acknowledgments

During the peer review process, the manufacturer of netupitant/palonosetron was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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    Gillian M. Keating

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  1. Gillian M. Keating
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Correspondence to Gillian M. Keating.

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The preparation of this review was not supported by any external funding.

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Gillian Keating is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.

Additional information

The manuscript was reviewed by: P. L. Andrews, Division of Biomedical Sciences, St George’s University of London, London, UK; A. Antonuzzo, Unit of Medical Oncology 1, Azienda Ospedaliero-Universitaria Pisana, Istituto Toscano Tumori Pisa, Pisa, Italy; L. Celio, Medical Oncology Unit 1, Department of Medical Oncology, Fondazione IRCCS Istituto Nazionale Tumori, Milan, Italy; J. Mezger, Department of Internal Medicine II, St. Vincentius-Kliniken Karlsruhe, Karlsruhe, Germany; R. M. Navari, Indiana University School of Medicine, South Bend, IN, USA.

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Keating, G.M. Netupitant/Palonosetron: A Review in the Prevention of Chemotherapy-Induced Nausea and Vomiting. Drugs 75, 2131–2141 (2015). https://doi.org/10.1007/s40265-015-0512-9

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