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Palonosetron: a second generation 5-hydroxytryptamine 3 receptor antagonist
1Indiana University School of Medicine South Bend, Walther Cancer Research Center, University Notre Dame, South Bend, IN 46617, USA. navari.1@nd.edu
Expert Opinion on Drug Metabolism & Toxicology
|November 26, 2009
Summary
Palonosetron, a novel 5-HT3 receptor antagonist, effectively prevents chemotherapy-induced nausea and vomiting (CINV). It offers superior control for both acute and delayed CINV, improving patient quality of life.
Area of Science:
- Oncology
- Pharmacology
Background:
- Chemotherapy-induced nausea and vomiting (CINV) significantly impairs patient quality of life.
- Risk factors for CINV include chemotherapy agent emetogenicity, treatment cycles, and patient characteristics like female gender and motion sickness history.
Purpose of the Study:
- To provide a comprehensive overview of palonosetron, a second-generation 5-HT3 receptor antagonist.
- To review the chemistry, pharmacology, and clinical trial data of palonosetron.
Main Methods:
- Review of palonosetron's chemical and pharmacological properties.
- Analysis of data from initial and recent clinical trials evaluating palonosetron's efficacy and safety.
Main Results:
- Palonosetron exhibits a longer half-life and higher binding affinity compared to first-generation 5-HT3 antagonists.
- Approved for preventing acute CINV (moderate/high emetogenicity) and delayed CINV (moderate emetogenicity).
- Palonosetron combined with dexamethasone shows improved delayed CINV control in highly emetogenic chemotherapy regimens.
Conclusions:
- Palonosetron demonstrates superior efficacy in managing both acute and delayed CINV.
- No unique adverse reactions were identified beyond the known class effects of 5-HT3 receptor antagonists.
- Palonosetron shows promise for managing CINV in complex treatments like multi-day chemotherapy and bone marrow transplantation.
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