Improved prevention of moderately emetogenic chemotherapy-induced nausea and vomiting with palonosetron, a pharmacologically novel 5-HT3 receptor antagonist: results of a phase III, single-dose trial versus dolasetron

Cancer. 2003 Dec 1;98(11):2473-82. doi: 10.1002/cncr.11817.

Abstract

Background: Palonosetron, a highly selective and potent 5-HT(3) receptor antagonist with a strong binding affinity and a long plasma elimination half-life (approximately 40 hours), has shown efficacy in Phase II trials in preventing chemotherapy-induced nausea and vomiting (CINV) resulting from highly emetogenic chemotherapy. The current Phase III trial evaluated the efficacy and safety of palonosetron in preventing acute and delayed CINV after moderately emetogenic chemotherapy.

Methods: In the current study, 592 patients were randomized to receive a single, intravenous dose of palonosetron 0.25 mg, palonosetron 0.75 mg, or dolasetron 100 mg, 30 minutes before receiving moderately emetogenic chemotherapy. The primary efficacy endpoint was the proportion of patients with a complete response (CR; defined as no emetic episodes and no rescue medication) during the first 24 hours after chemotherapy. Secondary endpoints included assessment of prevention of delayed emesis (2-5 days postchemotherapy).

Results: In the current study, 569 patients received study medication and were included in the intent-to-treat efficacy analyses. CR rates during the first 24 hours were 63.0% for palonosetron 0.25 mg, 57.1% for palonosetron 0.75 mg, and 52.9% for dolasetron 100 mg. CR rates during the delayed period (24-120 hours after chemotherapy) were superior for palonosetron compared with dolasetron. Adverse events (AEs) were mostly mild to moderate and not related to study medication, with similar incidences among groups. There were no serious drug-related AEs.

Conclusions: A single dose of palonosetron is as effective as a single dose of dolasetron in preventing acute CINV and superior to dolasetron in preventing delayed CINV after moderately emetogenic chemotherapy, with a comparable safety profile for all treatment groups.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antiemetics / adverse effects
  • Antiemetics / pharmacology
  • Antiemetics / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Double-Blind Method
  • Female
  • Humans
  • Indoles / adverse effects
  • Indoles / pharmacology
  • Indoles / therapeutic use*
  • Infusions, Intravenous
  • Isoquinolines / adverse effects
  • Isoquinolines / pharmacology
  • Isoquinolines / therapeutic use*
  • Male
  • Middle Aged
  • Neoplasms / drug therapy
  • Palonosetron
  • Quinolizines / adverse effects
  • Quinolizines / pharmacology
  • Quinolizines / therapeutic use*
  • Quinuclidines / adverse effects
  • Quinuclidines / pharmacology
  • Quinuclidines / therapeutic use*
  • Severity of Illness Index
  • Treatment Outcome
  • Vomiting / chemically induced*
  • Vomiting / prevention & control*

Substances

  • Antiemetics
  • Indoles
  • Isoquinolines
  • Quinolizines
  • Quinuclidines
  • Palonosetron
  • dolasetron