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Casopitant  mesylate

Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Casopitant (trade names Rezonic (US), Zunrisa (EU)) is an neurokinin 1 (NK1) receptor antagonist undergoing research for the treatment of chemotherapy-induced nausea and vomiting (CINV).  It is currently under development by GlaxoSmithKline (GSK). In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn in September 2009 because GSK decided that further safety assessment was necessary. (see: http://en.wikipedia.org/wiki/Casopitant).

Current developer: GlaxoSmithKline

  1: Kirby LC, Johnson BM, Adams LM, Eberwein DJ, Zhang K, Murray SC, Lates CD, Blum RA, Morris SR. Effect of casopitant, a novel NK-1 receptor antagonist, on the pharmacokinetics and pharmacodynamics of steady-state warfarin. J Clin Pharmacol. 2010 May;50(5):566-75. Epub 2010 Mar 10. PubMed PMID: 20220045.

2: Johnson BM, Adams LM, Zhang K, Gainer SD, Kirby LC, Blum RA, Apseloff G, Morrison RA, Schutz RA, Lebowitz PF. Ketoconazole and Rifampin Significantly Affect the Pharmacokinetics, But Not the Safety or QTc Interval, of Casopitant, a Neurokinin-1 Receptor Antagonist. J Clin Pharmacol. 2010 Feb 2. [Epub ahead of print] PubMed PMID: 20124517.

3: Quartara L, Altamura M, Evangelista S, Maggi CA. Tachykinin receptor antagonists in clinical trials. Expert Opin Investig Drugs. 2009 Dec;18(12):1843-64. Review. PubMed PMID: 19938899.

4: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Sep;31(7):463-93. PubMed PMID: 19907722.

5: Gridelli C, Haiderali AM, Russo MW, Blackburn LM, Lykopoulos K. Casopitant improves the quality of life in patients receiving highly emetogenic chemotherapy. Support Care Cancer. 2009 Oct 31. [Epub ahead of print] PubMed PMID: 19882176.

6: Arpornwirat W, Albert I, Hansen VL, Levin J, Bandekar RR, Grunberg SM. Phase 2 trial results with the novel neurokinin-1 receptor antagonist casopitant in combination with ondansetron and dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in cancer patients receiving moderately emetogenic chemotherapy. Cancer. 2009 Dec 15;115(24):5807-16. PubMed PMID: 19834961.

7: Herrstedt J, Apornwirat W, Shaharyar A, Aziz Z, Roila F, Van Belle S, Russo MW, Levin J, Ranganathan S, Guckert M, Grunberg SM. Phase III trial of casopitant, a novel neurokinin-1 receptor antagonist, for the prevention of nausea and vomiting in patients receiving moderately emetogenic chemotherapy. J Clin Oncol. 2009 Nov 10;27(32):5363-9. Epub 2009 Oct 5. PubMed PMID: 19805683.

8: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 May;31(4):263-98. PubMed PMID: 19557204.

9: Roila F, Rolski J, Ramlau R, Dediu M, Russo MW, Bandekar RR, Grunberg SM. Randomized, double-blind, dose-ranging trial of the oral neurokinin-1 receptor antagonist casopitant mesylate for the prevention of cisplatin-induced nausea and vomiting. Ann Oncol. 2009 Nov;20(11):1867-73. Epub 2009 Jun 18. PubMed PMID: 19541792.

10: Ruhlmann C, Herrstedt J. Casopitant: a novel NK(1)-receptor antagonist in the prevention of chemotherapy-induced nausea and vomiting. Ther Clin Risk Manag. 2009 Apr;5(2):375-84. Epub 2009 May 20. PubMed PMID: 19536319; PubMed Central PMCID: PMC2697542.

11: Khojasteh A, Khojasteh A, Thornburg BG, Maher KR. Casopitant: a new warrior in the antiemetic crusade. Expert Opin Pharmacother. 2009 Jun;10(8):1367-76. Review. PubMed PMID: 19445564.

12: Grunberg SM, Rolski J, Strausz J, Aziz Z, Lane S, Russo MW, Wissel P, Guckert M, Wright O, Herrstedt J. Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenic chemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58. Epub 2009 May 8. PubMed PMID: 19428297.

13: Pellegatti M, Bordini E, Fizzotti P, Roberts A, Johnson BM. Disposition and metabolism of radiolabeled casopitant in humans. Drug Metab Dispos. 2009 Aug;37(8):1635-45. Epub 2009 May 6. PubMed PMID: 19420128.

14: Navari RM. Pharmacological management of chemotherapy-induced nausea and vomiting: focus on recent developments. Drugs. 2009;69(5):515-33. doi: 10.2165/00003495-200969050-00002. Review. PubMed PMID: 19368415.

15: Navari RM. Antiemetic control: toward a new standard of care for emetogenic chemotherapy. Expert Opin Pharmacother. 2009 Mar;10(4):629-44. Review. PubMed PMID: 19284365.

16: Johnson B, Adams L, Lu E, Zhang K, Lebowitz P, Lates C, Blum R. Impact of casopitant, a novel NK-1 antagonist, on the pharmacokinetics of ondansetron and dexamethasone. Support Care Cancer. 2009 Sep;17(9):1177-85. Epub 2009 Feb 10. PubMed PMID: 19205755; PubMed Central PMCID: PMC2726912.

17: Adams LM, Johnson B, Zhang K, Yue L, Kirby LC, Lebowitz P, Stoltz R. Effect of casopitant, a novel NK-1 antagonist, on the pharmacokinetics of dolasetron and granisetron. Support Care Cancer. 2009 Sep;17(9):1187-93. Epub 2009 Feb 10. PubMed PMID: 19205754; PubMed Central PMCID: PMC2726911.

18: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Oct;30(8):643-72. PubMed PMID: 19088949.

19: Reddy GK, Gralla RJ, Hesketh PJ. Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy-induced emesis. Support Cancer Ther. 2006 Apr 1;3(3):140-2. PubMed PMID: 18632487.

20: Navari RM. Casopitant, a neurokinin-1 receptor antagonist with anti-emetic and anti-nausea activities. Curr Opin Investig Drugs. 2008 Jul;9(7):774-85. Review. PubMed PMID: 18600583.

21: Minthorn E, Mencken T, King AG, Shu A, Rominger D, Gontarek RR, Han C, Bambal R, Davis CB. Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret. Drug Metab Dispos. 2008 Sep;36(9):1846-52. Epub 2008 Jun 12. PubMed PMID: 18556439.

22: Lohr L. Chemotherapy-induced nausea and vomiting. Cancer J. 2008 Mar-Apr;14(2):85-93. Review. PubMed PMID: 18391612.

23: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Dec;28(10):719-40. PubMed PMID: 17235418.