Casopitant, a neurokinin-1 receptor antagonist with anti-emetic and anti-nausea activities.

Abstract

Casopitant, an inhibitor of the neurokinin-1 receptor, and its mesylate salt, are being developed by GlaxoSmithKline plc for the potential treatment of chemotherapy-induced nausea and vomiting (CINV), post-operative nausea and vomiting (PONV), as well as for anxiety, depression and insomnia. Phase II trials are ongoing for anxiety, depression and insomnia, and further results are awaited from phase III trials of CINV and PONV. At the time of publication, it was expected that applications to the FDA for regulatory approval for CINV and PONV would be filed in 2008. Casopitant was previously being developed for the treatment of overactive bladder; however, in September 2007, this indication was no longer listed on the company's product pipeline.

• Authors: Rudolph M Navari
• Journal: Current opinion in investigational drugs (London, England : 2000) (Curr Opin Investig Drugs) Vol. 9 Issue 7 Pg. 774-85 (Jul 2008) ISSN: 1472-4472 [Print] England
• PMID: 18600583 (Publication Type: Journal Article, Review)

Chemical References

• Antiemetics
• Neurokinin-1 Receptor Antagonists
• Piperazines
• Piperidines
• casopitant

Topics

• Animals
• Antiemetics (adverse effects, pharmacokinetics, pharmacology, therapeutic use, toxicity)
• Anxiety Disorders (drug therapy)
• Clinical Trials as Topic
• Contraindications
• Depressive Disorder, Major (drug therapy)
• Drug Evaluation, Preclinical
• Female
• Fibromyalgia (drug therapy)
• Humans
• Nausea (drug therapy)
• Neurokinin-1 Receptor Antagonists
• Patents as Topic
• Piperazines (pharmacokinetics, pharmacology, therapeutic use, toxicity)
• Piperidines (pharmacokinetics, pharmacology, therapeutic use, toxicity)
• Postoperative Nausea and Vomiting (drug therapy)
• Structure-Activity Relationship
• Urinary Bladder, Overactive (drug therapy)
• Vomiting (drug therapy)