Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy-induced emesis

G. Kesava Reddy, Richard J. Gralla, Paul J. Hesketh

Research output: Contribution to journalReview article

18 Scopus citations

Abstract

Despite significant advances in supportive care in oncology, many patients with cancer still experience chemotherapy-induced nausea and vomiting (CINV). Historically, there were only 3 neurotransmitter receptors (dopamine D2, cannabinoid-1, and 5-hydroxytryptamine-3) that were the known targets for antiemetic therapy. Major advances in the management of chemotherapy-induced emesis were seen with the introduction of 5-hydroxytryptamine-3 receptor antagonists, which include palonosetron, ondansetron, tropisetron, dolasetron, and granisetron. However, recently, selective inhibitors of substance P have shown promising activity in the management of CINV in patients with cancer. Substance P mediates a number of biologic effects by binding to a specific neuroreceptor, neurokinin-1 (NK-1). Among the NK-1 receptor antagonists, aprepitant has been approved for the treatment of CINV. Currently, several other NK-1 receptor antagonists, including casopitant, vestipitant, netupitant, and SCH619734, are undergoing clinical evaluation for the prevention of CINV in patients with a variety of malignancies. The clinical potential of these novel NK-1 receptor antagonists and their respective ongoing clinical trials for the management of chemotherapy-induced emesis are discussed briefly herein.

Original languageEnglish (US)
Pages (from-to)140-142
Number of pages3
JournalSupportive Cancer Therapy
Volume3
Issue number3
DOIs
StatePublished - Apr 2006

Keywords

  • 5-Hydroxytryptamine-3 receptor antagonists
  • Aprepitant
  • Casopitant
  • Nausea
  • Vomiting

ASJC Scopus subject areas

  • Oncology
  • Pharmacology
  • Cancer Research

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