Tonini Giuseppe, Vincenzi Bruno, Santini Daniele
University Campus Bio-Medico, Medical Oncology, Via E. Longoni 69, 00155, Rome, Italy.
Expert Opin Drug Metab Toxicol. 2005 Jun;1(1):143-9. doi: 10.1517/17425255.1.1.143.
Significant progress has been made in the development of effective, convenient and well-tolerated means to prevent chemotherapy-induced nausea and vomiting (CINV). Nevertheless, a substantial minority of patients continue to have suboptimal antiemetic control, and additional treatment approaches are needed. One avenue of investigation being pursued involves the evaluation of a new 5-hydroxytryptamine (5-HT(3)) receptor antagonist (palonosetron) that differs from available serotonin antagonists in its markedly longer half-life (40 h) and greater binding affinity for the type-3 serotonin receptor. Analysis of available clinical data demonstrates that palonosetron is an active and well-tolerated new 5-HT(3) antagonist. Moreover, single-dose palonosetron, prior to chemotherapy, has demonstrated improved control of CINV through the full period of emetic risk with a single dose. Palonosetron is recommended as the preferred treatment of acute and delayed emesis prevention with moderate emetic risk chemotherapy in the most recently published evidence-based antiemesis consensus guidelines. Further studies incorporating dexamethasone to 5-HT(3) antagonists will be necessary to determine the relative efficacy of palonosetron compared with available agents. These trials could open a new era in the treatment of CINV.
在开发有效、方便且耐受性良好的预防化疗引起的恶心和呕吐（CINV）的方法方面已取得重大进展。然而，仍有相当一部分患者的止吐控制效果欠佳，需要更多的治疗方法。正在进行的一项研究途径涉及评估一种新型5-羟色胺（5-HT(3)）受体拮抗剂（帕洛诺司琼），它与现有的血清素拮抗剂不同，其半衰期明显更长（40小时），并且对3型血清素受体具有更高的结合亲和力。对现有临床数据的分析表明，帕洛诺司琼是一种有效的且耐受性良好的新型5-HT(3)拮抗剂。此外，化疗前单剂量使用帕洛诺司琼已证明在整个呕吐风险期内单剂量即可改善对CINV的控制。在最近发布的基于证据的止吐共识指南中，帕洛诺司琼被推荐为预防中度呕吐风险化疗引起的急性和延迟性呕吐的首选治疗方法。将地塞米松与5-HT(3)拮抗剂联合使用的进一步研究对于确定帕洛诺司琼与现有药物相比的相对疗效是必要的。这些试验可能会开启CINV治疗的新时代。
