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5-HT3 Receptor Antagonists

An Overview of their Present Status and Future Potential in Cancer Therapy-Induced Emesis

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Summary

The serotonin (5-hydroxytryptamine, 5-HT) antagonists, which bind at the type 3 receptor (5-HT3 receptor), have been evaluated in several preclinical models and found to be effective in alleviating cancer therapy-related emesis. The antiemetic efficacy of ondansetron (GRF-38032F, odanserin), granisetron (BRL-43694), tropisetron (ICS-205930), MDL-72222 and MDL-73147EF, batanopride (BMY-25801-01) and several others is at various stages of investigation. Ondansetron is currently marketed in several countries and the same will soon be true for granisetron.

At this stage it is not yet possible to evaluate the comparative efficacy of each of these compounds, although recent preclinical data reveal some differences in the affinity of these compounds for other receptors. Side effects related to these agents have been minor, consisting mainly of slight headaches; possible rises in liver enzymes related to some compounds need further evaluation. Future studies will need to determine the exact role of 5-HT3 antagonists, although their cost may confine their use to patients at high risk for side effects from metoclopramide.

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  1. Division d’Onco-Hématologie, Hôpital Cantonal Universitaire, Genève 4, 1211, Switzerland

    Matti S. Aapro (Médecin-Consultant)

  2. Centre Anticancéreux, Genolier, Switzerland

    Matti S. Aapro (Médecin-Consultant)

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Aapro, M.S. 5-HT3 Receptor Antagonists. Drugs 42, 551–568 (1991). https://doi.org/10.2165/00003495-199142040-00002

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