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Evolocumab for the treatment of hypercholesterolemia

机译：Evolocumab用于治疗高胆固醇血症

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Introduction: Evolocumab is a fully human monoclonal immunoglobulin G2 directed against human proprotein convertase subtilisin/kexin type 9 (PCSK9). It is administered by subcutaneous injection every 2weeks or once monthly.Area covered: Herein, the authors discuss the rationale for inhibiting PCSK9 and describe the pharmacodynamics, pharmacokinetics and clinical trials with evolocumab. Evolocumab reduces low density lipoprotein cholesterol (LDL-C) levels by 50 to 60% in most patients with and without background treatment with statins or other lipid lowering agents. The safety profile appears satisfactory from the completed clinical studies and concerns regarding the risk of neurocognitive events have largely been dispelled.Expert opinion: The reduction of LDL-C with evolocumab to previously unattainable levels has resulted in a reduction in the composite cardiovascular event endpoint in the FOURIER trial and this is likely to impact on future lipid management guidelines. The clinical outcome data and excellent tolerability profile clearly support the use of evolocumab in patients at high cardiovascular risk, including those with heterozygous or homozygous familial hypercholesterolemia, who are unable to achieve LDL-C targets with statins with or without other lipid-lowering drugs. The high cost of evolocumab will restrict its use, however.
机译：介绍：Evolocumab是针对人类普罗基蛋白转化酶枯草杆菌蛋白酶/ kexin型9（PCSK9）的全人单克隆免疫球蛋白G2。它通过皮下注射每2周或每月一次进行一次。覆盖：本文，本文讨论了抑制PCSK9的理由，并描述了与Evolocumab的药效学，药代动力学和临床试验。 Evolocumab在大多数患者和没有与他汀类药物或其他脂质降低剂的背景处理的患者中将低密度脂蛋白胆固醇（LDL-C）水平降低50至60％。安全型材从完成的临床研究中似乎令人满意，关于神经认知事件的风险的担忧在很大程度上已经消失了。普及意见：用Evolocumab的LDL-C还原到以前是无法实现的水平的情况导致复合心血管事件终点减少傅里叶试验和这可能会影响未来的脂质管理指南。临床结果数据和优异的耐受性分布清楚地支持在高血管内风险的患者中使用Evolocumab，包括杂合或纯合的家族性高胆固醇血症的患者，他们无法使用其他脂质降低药物的他汀类药物达到LDL-C靶标。然而，Evolocumab的高成本将限制其使用。

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