Neurokinin-1 receptor antagonists: review of their role for the prevention of chemotherapy-induced nausea and vomiting in adults

Meinolf Karthaus, Xaver Schiel, Christina H. Ruhlmann, Luigi Celio

Research output: Contribution to journalReview articlepeer-review


Introduction: The addition of neurokinin-1 receptor antagonists (NK1RAs) to standard prophylaxis of 5-hydroxytryptamine-3 RA (5-HT3RA) plus dexamethasone more effectively prevents chemotherapy-induced nausea and vomiting (CINV) associated with highly and moderately emetogenic chemotherapy. Areas covered: This review presents the evidence base for the use of oral and intravenous (IV) NK1RAs, focusing on the pharmacologic and clinical properties as a class, and highlighting differences between agents. A PubMed literature search was conducted from 2000 to 2018. Expert opinion: Adherence to international antiemetic guidelines remains a clinical challenge. Strategies to simplify antiemetic regimens and facilitate their administration may improve compliance and treatment outcomes. The use of fixed-combination antiemetics offers clinical utility, in combining an NK1RA with a 5-HT3RA in a single oral dose. The use of long-lasting NK1RAs and administering CINV prophylaxis closer to the time of chemotherapy may also assist with guideline and treatment compliance, diminishing the need for home-based administration, and potentially reducing resource utilization. The availability of IV and oral formulations of NK1RAs and NK1RA–5-HT3RA fixed combinations offers further utility, particularly for those patients unsuited for oral administration. However, safety considerations with respect to injection site toxicity and hypersensitivity reactions of the new NK1RA IV formulations deserve close attention.

Original languageEnglish
Pages (from-to)661-680
Number of pages20
JournalExpert Review of Clinical Pharmacology
Issue number7
Publication statusPublished - Jul 3 2019


  • adherence
  • antiemetics
  • Chemotherapy-induced nausea and vomiting (CINV)
  • emesis
  • guidelines

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)


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