Rolapitant for the treatment of chemotherapy-induced nausea and vomiting: a review of the clinical evidence

Future Oncol. 2016 Mar;12(6):763-78. doi: 10.2217/fon.16.11. Epub 2016 Feb 4.

Abstract

Chemotherapy-induced nausea and vomiting (CINV), both acute and delayed, has a dramatic effect on the well-being and quality of life of patients with cancer. Improved understanding of the mechanisms involved in CINV has led to the development of agents targeting the 5-HT3 receptor as well as the NK-1 receptor. Antiemetic prophylaxis given to patients receiving highly emetogenic chemotherapy combines agents blocking the 5-HT3 and NK-1 receptors along with corticosteroids given regularly and repeatedly. Rolapitant is a long-acting NK-1 receptor antagonist with proven efficacy in controlling CINV as part of the prophylaxis regimen. This review will detail the clinical efficacy and safety of rolapitant in the treatment of patients with cancer receiving highly or moderately emetogenic chemotherapy.

Keywords: NK-1 receptor antagonist; antiemetic; aprepitant; chemotherapy-induced nausea and vomiting; delayed chemotherapy-induced nausea and vomiting; fosaprepitant; netupitant; palonosetron; rolapitant.

Publication types

  • Review

MeSH terms

  • Antiemetics / chemistry
  • Antiemetics / pharmacology
  • Antiemetics / therapeutic use*
  • Antineoplastic Agents / adverse effects*
  • Antineoplastic Agents / therapeutic use
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Drug Interactions
  • Humans
  • Nausea / drug therapy*
  • Nausea / etiology*
  • Neoplasms / complications*
  • Neoplasms / drug therapy
  • Neurokinin-1 Receptor Antagonists / pharmacology
  • Neurokinin-1 Receptor Antagonists / therapeutic use
  • Quality of Life
  • Receptors, Neurokinin-1 / metabolism
  • Spiro Compounds / chemistry
  • Spiro Compounds / pharmacology
  • Spiro Compounds / therapeutic use*
  • Treatment Outcome
  • Vomiting / drug therapy*
  • Vomiting / etiology*

Substances

  • Antiemetics
  • Antineoplastic Agents
  • Neurokinin-1 Receptor Antagonists
  • Receptors, Neurokinin-1
  • Spiro Compounds
  • rolapitant