Van Belle Simon Jp, Cocquyt Veronique
University Hospital Ghent, Department of Medical Oncology, De Pintelaan 185, 9000 Ghent, Belgium.
Expert Opin Pharmacother. 2008 Dec;9(18):3261-70. doi: 10.1517/14656560802548463.
This paper reviews the existing literature on fosaprepitant, an intravenous neurokinin-1 anatgonist for the prevention of chemotherapy induced nausea and vomiting.
To describe the development of fosaprepitant and to situate the intravenous form of aprepitant in the current market of available antiemetics.
Literature was screened and selected in order to compare the intravenous form of the already commonly used NK-1 receptor antagonist aprepitant.
Aprepitant is the first and still the only marketed neurokinin-1 (NK-1) antagonist. Interestingly, the first studies were performed with fosaprepitant dimeglumine (MK-0517 or L-785,298), the water-soluble prodrug of aprepitant. Fosaprepitant is converted into aprepitant within 30 min after intravenous administration. Based on equivalence studies, 115 mg fosaprepitant seems to be the substitute for 125 mg orally administrated aprepitant. Tolerability of the prodrug is no different from the active drug. The number of efficacy studies with fosaprepitant is very limited and most data are derived from existing aprepitant results. Fosaprepitant has recently been approved by FDA and EMEA as an intravenous substitute for oral aprepitant on day 1 of the standard 3-day CINV prevention regimen, which also includes dexamethasone and a 5-HT3 antagonist.
本文综述了关于福沙匹坦的现有文献，福沙匹坦是一种静脉注射用神经激肽-1拮抗剂，用于预防化疗引起的恶心和呕吐。
描述福沙匹坦的研发过程，并将阿瑞匹坦的静脉注射剂型置于当前可用止吐药市场中进行定位。
筛选并选择文献，以比较已常用的NK-1受体拮抗剂阿瑞匹坦的静脉注射剂型。
阿瑞匹坦是首个且仍是唯一上市的神经激肽-1（NK-1）拮抗剂。有趣的是，最初的研究是用福沙匹坦二葡甲胺（MK-0517或L-785,298）进行的，它是阿瑞匹坦的水溶性前药。福沙匹坦在静脉给药后30分钟内转化为阿瑞匹坦。基于等效性研究，115mg福沙匹坦似乎可替代125mg口服阿瑞匹坦。前药的耐受性与活性药物无异。关于福沙匹坦的疗效研究数量非常有限，且大多数数据来自现有的阿瑞匹坦研究结果。福沙匹坦最近已被美国食品药品监督管理局（FDA）和欧洲药品管理局（EMEA）批准，作为标准3天化疗所致恶心和呕吐（CINV）预防方案第1天口服阿瑞匹坦的静脉替代药物，该方案还包括地塞米松和一种5-羟色胺3（5-HT3）拮抗剂。
