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Palonosetron

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Abstract

  • ▴ Palonosetron is a potent and highly selective serotonin 5-HT3 receptor antagonist that has been evaluated for the prevention of chemotherapy-induced nausea and vomiting.

  • ▴ Intravenously administered palonosetron has a linear pharmacokinetic profile, with a long terminal elimination half-life (≈40 hours) and moderate (62%) plasma protein binding.

  • ▴ In two randomised, double-blind trials in 1132 cancer patients receiving moderately emetogenic chemotherapy, intravenous palonosetron 0.25mg was more effective than intravenous ondansetron 32mg in producing a complete reponse (no emesis, no use of rescue medication) during acute (0–24 hours) or delayed (24–120 hours) phases, and similar to intravenous dolasetron 100mg in acute, but more effective in delayed phase. Palonosetron 0.75mg was similar to ondansetron (acute and delayed phase) or dolasetron (acute phase), but more effective than dolasetron in delayed phase.

  • ▴ In patients receiving highly emetogenic chemotherapy (n = 667), the complete response rates during acute and delayed phases with intravenous palonosetron (0.25 or 0.75mg) were similar to those seen in intravenous ondansetron 32mg recipients in a randomised, double-blind trial.

  • ▴ Intravenous palonosetron was generally well tolerated in clinical trials, with few adverse events being treatment related. Palonosetron had no significant effect on the corrected QT interval or laboratory parameters.

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Notes

  1. The use of trade names is for product identification purposes only and does not imply endorsement.

References

  1. Gralla RJ, Osoba D, Kris MG, et al., for the American Society of Clinical Oncology. Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines. J Clin Oncol 1999; 17(9): 2971–94

    PubMed  CAS  Google Scholar 

  2. National Cancer Institute. Physician Data Query (PDQ®) supportive care summaries (health professional version): nausea and emesis [online]. Available from URL: http://cancer.gov/ [Accessed 2004 Apr 15]

  3. National Comprehensive Cancer Network antiemesis panel. Clinical practice guidelines in oncology — antiemesis version 1.2004 [online]. Available from URL: http://www.nccn.org [Accessed 2004 Apr 15]

  4. Coates A, Abraham S, Kaye SB, et al. On the receiving end-patient perception of the side-effects of cancer chemotherapy. Eur J Cancer Clin Oncol 1983; 19(2): 203–8

    Article  PubMed  CAS  Google Scholar 

  5. American Society of Health-System Pharmacists (ASHP) Commission on Therapeutics. ASHP therapeutic guidelines on the pharmacologic management of nausea and vomiting in adult and pediatric patients receiving chemotherapy or radiation therapy or undergoing surgery. Am J Health Syst Pharm 1999; 56(8): 729–64

    Google Scholar 

  6. de Boer-Dennert M, de Wit R, Schmitz PIM, et al. Patient perceptions of the side-effects of chemotherapy: the influence of 5-HT3 antagonists. Br J Cancer 1997; 76(8): 1055–61

    Article  PubMed  Google Scholar 

  7. Laszlo J. Nausea and vomiting as major complications of cancer chemotherapy. Drugs 1983; 25 Suppl. 1: 1–7

    Article  PubMed  Google Scholar 

  8. Fauser AA, Fellhauer M, Hoffmann M, et al. Guidelines for anti-emetic therapy: acute emesis. Eur J Cancer 1999 Mar; 35(3): 361–70

    Article  PubMed  CAS  Google Scholar 

  9. Tavorth R, Hesketh PJ. Drug treatment of chemotherapy-induced delayed emesis. Drugs 1996; 52(5): 639–48

    Article  Google Scholar 

  10. Wong EHF, Clark R, Leung E, et al. The interaction of RS 25259-197, a potent and selective antagonist, with 5-HT3 receptors, in vitro. Br J Pharmacol 1995; 114(4): 851–9

    Article  PubMed  CAS  Google Scholar 

  11. Eglen RM, Lee C-H., Smith WL, et al. Pharmacological characterization of RS 25259-197, a novel and selective 5-HT3 receptor antagonist, in vivo. Br J Pharmacol 1995 Feb; 114(4): 860–6

    Article  PubMed  CAS  Google Scholar 

  12. Gatti S, Stolz R, Tei M, et al. A novel anti-emetic agent, palonosetron: evidence from phase I trials [poster]. Multinational Association of Supportive Care in Cancer (MASCC)/ International Society of Oral Oncology (ISOO) 13th Annual International Symposium on Supportive Care in Cancer; 2001 June 14–16; Copenhagen

  13. Piraccini G, Stolz R, Tei M, et al. An interesting 5-HT3 receptor antagonist antiemetic for patients undergoing chemotherapy-based conditioning regimens? [abstract no. 5169]. Blood 2001; 98(11 Pt 2): 350b

    Google Scholar 

  14. Piraccini G, Stolz R, Tei M, et al. Pharmacokinetic features of a novel 5-HT3 receptor antagonist: palonosetron (RS-25259-197) [abstract no. 1595]. Proc Am Soc Clin Oncol 2001; 20 Pt 1: 400a

    Google Scholar 

  15. Eisenberg P, MacKintosh FR, Ritch P, et al. Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol 2004; 15(2): 330–7

    Article  PubMed  CAS  Google Scholar 

  16. Aloxi™ (palonosetron hydrochloride) Injection, 0.25 mg/5ml [product information]. Switzerland: Helsinn Healthcare SA, 2003 Jul

  17. Gralla R, Lichinitser M, Van Der Vegt S, et al. Palonosetron improves prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy: results of a double-blind randomized phase III trial comparing single doses of palonosetron with ondansetron. Ann Oncol 2003 Oct; 14(10): 1570–7

    Article  PubMed  CAS  Google Scholar 

  18. Eisenberg P, Figueroa-Vadillo J, Zamora R, et al. Improved prevention of moderately emetogenic chemotherapy-induced nausea and vomiting with palonosetron, a pharmacologically novel 5-HT3 receptor antagonist: results of a phase III, singledose trial versus dolasetron. Cancer 2003 Dec 1; 98(11): 2473–82

    Article  PubMed  CAS  Google Scholar 

  19. Aapro MS, Bertoli L, Lordick K, et al. Palonosetron (PALO) is effective in preventing acute and delayed chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly emetogenic chemotherapy (HEC) [abstract]. Multinational Association of Supportive Care in Cancer (MASCC)/International Society for Oral Oncology (ISOO) 15th International Symposium on Supportive Care in Cancer; 2003 June 18–21; Berlin

  20. Helsinn Healthcare S.A. Aloxi™ (palonosetron hydrochloride) Injection NDA no. 021–372 submitted to the US FDA by Helsinn Healthcare S.A. [online]. Available from URL: http://www.fda.gov/cder [Accessed 2004 Apr 15]

  21. Crtmell AD, Ferguson S, Yanagihara R, et al. Protection against chemotherapy-induced nausea and vomiting (CINV) is maintained over multiple cycles of moderately or highly emetogenic chemotherapy by palonosetron (PALO), a potent 5-HT3 receptor antagonist (RA) [abstract no. 3041]. Proc Am Soc Clin Oncol 2003; 22: 756. Plus poster presented at the 39th Annual Meeting of the American Society of Clinical Oncology; 2003 May 31–Jun

    Google Scholar 

  22. Helsinn Healthcare S.A., MGI Pharma. HELSINN and MGI PHARMA summarise palonosetron HCl injection (Aloxi in USA) phase III clinical data presented at the Multinational Association of Supportive Care in Cancer (MASCC) 15th International Symposium [media release]. 23 Jun 2003

  23. S-FDA. Drugs@FDA, a catalog of FDA approved drug products [online]. Available from URL: http://www.fda.gov/cder [Accessed 2004 Apr 15]

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Correspondence to M. Asif A. Siddiqui.

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Siddiqui, M.A.A., Scott, L.J. Palonosetron. Drugs 64, 1125–1132 (2004). https://doi.org/10.2165/00003495-200464100-00006

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