Rolapitant for the treatment of chemotherapy-induced nausea and vomiting

Expert Rev Anticancer Ther. 2015;15(10):1127-33. doi: 10.1586/14737140.2015.1088787. Epub 2015 Sep 14.

Abstract

Chemotherapy-induced nausea and vomiting is a significant clinical issue which affects patient's quality of life and treatment decisions. Significant improvements in the control of chemotherapy-induced nausea and vomiting have occurred in the past 15 years with the introduction of new antiemetic agents 5-HT3, receptor antagonists, neurokinin-1 (NK-1) receptor antagonists, and olanzapine. Aprepitant was the first NK-1 receptor antagonist introduced (2003) for the prevention of chemotherapy-induced nausea and vomiting in combination with a 5-HT3 receptor antagonist and dexamethasone. A second NK-1 receptor antagonist netupitant was approved for use in October 2014. Phase III clinical trials of an additional NK-1 receptor antagonist rolapitant have been completed, and the data have been submitted for regulatory approval. A description of rolapitant and its role in chemotherapy-induced nausea and vomiting will be presented, along with a comparison of the other neurolinin-1 receptor antagonists aprepitant and netupitant.

Keywords: 5-hydroxytryptamine-3 receptor antagonists; antiemetics; aprepitant; chemotherapy-induced nausea and vomiting; netupitant; rolapitant.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Antiemetics / pharmacology
  • Antiemetics / therapeutic use
  • Antineoplastic Agents / adverse effects
  • Aprepitant
  • Humans
  • Morpholines / pharmacology
  • Morpholines / therapeutic use
  • Nausea / chemically induced
  • Nausea / drug therapy*
  • Neurokinin-1 Receptor Antagonists / pharmacology
  • Neurokinin-1 Receptor Antagonists / therapeutic use
  • Pyridines / pharmacology
  • Pyridines / therapeutic use
  • Quality of Life
  • Spiro Compounds / pharmacology
  • Spiro Compounds / therapeutic use*
  • Vomiting / chemically induced
  • Vomiting / drug therapy*

Substances

  • Antiemetics
  • Antineoplastic Agents
  • Morpholines
  • Neurokinin-1 Receptor Antagonists
  • Pyridines
  • Spiro Compounds
  • Aprepitant
  • netupitant
  • rolapitant