Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting
Rudolph M Navari,1 Lee S Schwartzberg2 1Department of Hematology/Oncology, University of Alabama at Birmingham, Birmingham, AL, USA; 2Division of Hematology/Oncology, Department of Medicine, University of Tennessee Health Science Center and West Cancer Center, Memphis, TN, USA Abstract: To examine...
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doaj-37c0b37bb3a04279a74d5ad503f737432020-11-25T00:48:54ZengDove Medical PressOncoTargets and Therapy1178-69302018-10-01Volume 116459647841106Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomitingNavari RMSchwartzberg LSRudolph M Navari,1 Lee S Schwartzberg2 1Department of Hematology/Oncology, University of Alabama at Birmingham, Birmingham, AL, USA; 2Division of Hematology/Oncology, Department of Medicine, University of Tennessee Health Science Center and West Cancer Center, Memphis, TN, USA Abstract: To examine pharmacologic and clinical characteristics of neurokinin 1 (NK1)-receptor antagonists (RAs) for preventing chemotherapy-induced nausea and vomiting (CINV) following highly or moderately emetogenic chemotherapy, a literature search was performed for clinical studies in patients at risk of CINV with any approved NK1 RAs in the title or abstract: aprepitant (capsules or oral suspension), HTX019 (intravenous [IV] aprepitant), fosaprepitant (IV aprepitant prodrug), rolapitant (tablets or IV), and fixed-dose tablets combining netupitant or fosnetupitant (IV netupitant prodrug) with the 5-hydroxytryptamine type 3 (5HT3) RA palonosetron (oral or IV). All NK1 RAs are effective, but exhibit important differences in efficacy against acute and delayed CINV. The magnitude of benefit of NK1-RA-containing three-drug vs two-drug regimens is greater for delayed vs acute CINV. Oral rolapitant has the longest half-life of available NK1 RAs, but as a consequence should not be administered more frequently than every 2 weeks. In general, NK1 RAs are well tolerated; however, IV rolapitant was recently removed from US distribution, due to hypersensitivity and anaphylaxis, and IV fosaprepitant is associated with infusion-site reactions and hypersensitivity presumed related to its polysorbate 80 excipient. Also, available NK1 RAs have potential drug–drug interactions. Adding an NK1 RA to 5HT3 RA and dexamethasone significantly improves CINV control vs the two-drug regimen. Newer NK1 RAs offer more formulation options, higher acute-phase plasma levels, or improved tolerability, and increase clinicians’ opportunities to maximize benefits of this important class of antiemetics. Keywords: aprepitant, chemotherapy-induced nausea and vomiting, fosaprepitant, netupitant, neurokinin 1-receptor antagonists, rolapitanthttps://www.dovepress.com/evolving-role-of-neurokinin-1-receptor-antagonists-for-chemotherapy-in-peer-reviewed-article-OTTaprepitantchemotherapy-induced nausea and vomitingfosaprepitantnetupitantneurokinin 1 receptor antagonistsrolapitant |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Navari RM Schwartzberg LS |
spellingShingle |
Navari RM Schwartzberg LS Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting OncoTargets and Therapy aprepitant chemotherapy-induced nausea and vomiting fosaprepitant netupitant neurokinin 1 receptor antagonists rolapitant |
author_facet |
Navari RM Schwartzberg LS |
author_sort |
Navari RM |
title |
Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
title_short |
Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
title_full |
Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
title_fullStr |
Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
title_full_unstemmed |
Evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
title_sort |
evolving role of neurokinin 1-receptor antagonists for chemotherapy-induced nausea and vomiting |
publisher |
Dove Medical Press |
series |
OncoTargets and Therapy |
issn |
1178-6930 |
publishDate |
2018-10-01 |
description |
Rudolph M Navari,1 Lee S Schwartzberg2 1Department of Hematology/Oncology, University of Alabama at Birmingham, Birmingham, AL, USA; 2Division of Hematology/Oncology, Department of Medicine, University of Tennessee Health Science Center and West Cancer Center, Memphis, TN, USA Abstract: To examine pharmacologic and clinical characteristics of neurokinin 1 (NK1)-receptor antagonists (RAs) for preventing chemotherapy-induced nausea and vomiting (CINV) following highly or moderately emetogenic chemotherapy, a literature search was performed for clinical studies in patients at risk of CINV with any approved NK1 RAs in the title or abstract: aprepitant (capsules or oral suspension), HTX019 (intravenous [IV] aprepitant), fosaprepitant (IV aprepitant prodrug), rolapitant (tablets or IV), and fixed-dose tablets combining netupitant or fosnetupitant (IV netupitant prodrug) with the 5-hydroxytryptamine type 3 (5HT3) RA palonosetron (oral or IV). All NK1 RAs are effective, but exhibit important differences in efficacy against acute and delayed CINV. The magnitude of benefit of NK1-RA-containing three-drug vs two-drug regimens is greater for delayed vs acute CINV. Oral rolapitant has the longest half-life of available NK1 RAs, but as a consequence should not be administered more frequently than every 2 weeks. In general, NK1 RAs are well tolerated; however, IV rolapitant was recently removed from US distribution, due to hypersensitivity and anaphylaxis, and IV fosaprepitant is associated with infusion-site reactions and hypersensitivity presumed related to its polysorbate 80 excipient. Also, available NK1 RAs have potential drug–drug interactions. Adding an NK1 RA to 5HT3 RA and dexamethasone significantly improves CINV control vs the two-drug regimen. Newer NK1 RAs offer more formulation options, higher acute-phase plasma levels, or improved tolerability, and increase clinicians’ opportunities to maximize benefits of this important class of antiemetics. Keywords: aprepitant, chemotherapy-induced nausea and vomiting, fosaprepitant, netupitant, neurokinin 1-receptor antagonists, rolapitant |
topic |
aprepitant chemotherapy-induced nausea and vomiting fosaprepitant netupitant neurokinin 1 receptor antagonists rolapitant |
url |
https://www.dovepress.com/evolving-role-of-neurokinin-1-receptor-antagonists-for-chemotherapy-in-peer-reviewed-article-OTT |
work_keys_str_mv |
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