title: 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.affiliation: Indiana University School of Medicine, South Bend, 100 Raclin-Carmichael Hall, South Bend, IN 46617, USA. rnavari@nd.edu
authors.forename: Rudolph M
authors.initials: RM
authors.lastname: Navari
mesh_terms: D000818:Animals; D000932:Antiemetics / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D001008:Anxiety Disorders / Q000188:drug therapy; D002986:Clinical Trials as Topic; D000075202:Contraindications; D003865:Major Depressive Disorder / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D005260:Female; D005356:Fibromyalgia / Q000188:drug therapy; D006801:Humans; D009325:Nausea / Q000188:drug therapy*; D064729:Neurokinin-1 Receptor Antagonists; D010330:Patents as Topic; D010879:Piperazines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D010880:Piperidines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D020250:Postoperative Nausea and Vomiting / Q000188:drug therapy; D013329:Structure-Activity Relationship; D053201:Urinary Bladder, Overactive / Q000188:drug therapy; D014839:Vomiting / Q000188:drug therapy*; D014508:Urea
chemical_list: D000932:Antiemetics; D064729:Neurokinin-1 Receptor Antagonists; D010879:Piperazines; D010880:Piperidines; C531951:casopitant; D014508:Urea