Rolapitant hydrochloride: prophylactic treatment for chemotherapy-induced nausea and vomiting

Drugs Today (Barc). 2016 Aug;52(8):431-438. doi: 10.1358/dot.2016.52.8.2525738.

Abstract

Chemotherapy-induced nausea and vomiting (CINV) is a significant clinical issue which affects patients' quality of life as well as treatment decisions. Significant improvements in the control of CINV have occurred in the past 15 years with the introduction of new antiemetic agents: 5-HT3 receptor antagonists, tachykinin NK1 receptor antagonists and olanzapine. Aprepitant was the first NK1 receptor antagonist introduced (2003) for the prevention of CINV in combination with a 5-HT3 receptor antagonist and dexamethasone. Two additional NK1 receptor antagonists, netupitant and rolapitant, were approved by the FDA in 2014 and 2015, respectively. A description of rolapitant and its role in CINV will be presented, along with a comparison to the other NK1 receptor antagonists, aprepitant and netupitant.

Keywords: 5-HT3 receptor antagonists; Antiemetics; Aprepitant; Chemotherapy-induced nausea and vomiting; Netupitant; Rolapitant.

Publication types

  • Review

MeSH terms

  • Antiemetics / therapeutic use*
  • Antineoplastic Agents / adverse effects*
  • Clinical Trials as Topic
  • Humans
  • Nausea / prevention & control*
  • Neurokinin-1 Receptor Antagonists / therapeutic use*
  • Spiro Compounds / adverse effects
  • Spiro Compounds / therapeutic use*
  • Vomiting / prevention & control*

Substances

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