Odense University Hospital, Department of Oncology, Sdr. Boulevard 29, DK-5000 Odense C, Denmark.
Expert Rev Anticancer Ther. 2010 Feb;10(2):137-48. doi: 10.1586/era.09.175.
A large number of different 5-hydroxytryptamine (HT)(3) receptor antagonists have been marketed with the indication of preventing nausea and vomiting induced by chemotherapy--palonosetron is the most recently developed of these. Pharmacologic studies have revealed that palonosetron has a long half-life, a high affinity for 5-HT(3) receptors, exhibits allosteric binding to 5-HT(3) receptors and possess positive cooperativity. Although interesting, pharmacologic differences are only useful if they result in clinical advantages, such as an increase in efficacy and/or an improvement in tolerability. We summarize preclinical and clinical studies of palonosetron and compare the efficacy and tolerability with the other 5-HT(3) receptor antagonists, ondansetron, granisetron and dolasetron.
大量不同的 5-羟色胺（HT）（3）受体拮抗剂已被推向市场，用于预防化疗引起的恶心和呕吐——帕洛诺司琼是这些药物中最新开发的一种。药理研究表明，帕洛诺司琼半衰期长，对 5-HT（3）受体具有高亲和力，对 5-HT（3）受体表现出变构结合，并具有正协同作用。虽然很有趣，但如果药理差异能带来临床优势，如提高疗效和/或改善耐受性，那么这些差异才是有用的。我们总结了帕洛诺司琼的临床前和临床研究，并将其与其他 5-HT（3）受体拮抗剂昂丹司琼、格拉司琼和多拉司琼的疗效和耐受性进行了比较。
