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二十碳五烯酸乙酯:重度高甘油三酯血症应用综述

Icosapent ethyl: a review of its use in severe hypertriglyceridemia.

作者信息

Kim Esther S, McCormack Paul L

机构信息

Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand,

出版信息

Am J Cardiovasc Drugs. 2014 Dec;14(6):471-8. doi: 10.1007/s40256-014-0099-7.

Abstract

Icosapent ethyl (Vascepa®) is a high-purity ethyl ester of eicosapentaenoic acid (EPA) that is de-esterified to EPA following oral administration. Both EPA and docosahexaenoic acid (DHA) are long-chain omega-3 fatty acids that have been associated with triglyceride (TG)-lowering. However, DHA has been associated with increased low-density lipoprotein cholesterol (LDL-C) levels. Icosapent ethyl contains ≥96 % of the EPA ethyl ester, does not contain DHA, and is approved in the USA for use as an adjunct to diet to lower TG levels in adult patients with severe (≥500 mg/dL [≥5.65 mmol/L]) hypertriglyceridemia. In a pivotal phase III trial, oral icosapent ethyl 4 g/day significantly decreased the placebo-corrected median TG levels by 33.1 %. It did not increase LDL-C, had favorable effects on other lipid parameters, and had a tolerability profile similar to that of placebo. Therefore, icosapent ethyl is an effective and well-tolerated agent for the treatment of severe hypertriglyceridemia in adults.

摘要

二十碳五烯酸乙酯(Vascepa®)是一种高纯度的二十碳五烯酸(EPA)乙酯,口服给药后会脱酯化为EPA。EPA和二十二碳六烯酸(DHA)都是长链ω-3脂肪酸,都与降低甘油三酯(TG)有关。然而,DHA与低密度脂蛋白胆固醇(LDL-C)水平升高有关。二十碳五烯酸乙酯含有≥96%的EPA乙酯,不含DHA,在美国被批准作为饮食辅助药物,用于降低重度(≥500mg/dL[≥5.65mmol/L])高甘油三酯血症成年患者的TG水平。在一项关键的III期试验中,口服二十碳五烯酸乙酯4g/天可使安慰剂校正后的TG中位数水平显著降低33.1%。它不会升高LDL-C,对其他血脂参数有有利影响,并且耐受性与安慰剂相似。因此,二十碳五烯酸乙酯是治疗成人重度高甘油三酯血症的一种有效且耐受性良好的药物。

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