Pintó Xavier, García Gómez María Carmen
Unidad de Lípidos y Riesgo Vascular, Servicio de Medicina Interna, Hospital Universitario de Bellvitge, L'Hospitalet de Llobregat, Barcelona, España; Centro de Investigación Biomédica en Red de Fisiopatología de la Obesidad y Nutrición (CIBERobn), Universidad de Barcelona, Barcelona, España.
Servicio de Reumatología, Consorci Sanitari de Terrassa, Terrassa, Barcelona, España.
Med Clin (Barc). 2016 Feb 19;146(4):172-7. doi: 10.1016/j.medcli.2015.01.016. Epub 2015 Mar 24.
An elevated proportion of high cardiovascular risk patients do not achieve the therapeutic c-LDL goals. This owes to physicians' inappropriate or insufficient use of cholesterol lowering medications or to patients' bad tolerance or therapeutic compliance. Another cause is an insufficient efficacy of current cholesterol lowering drugs including statins and ezetimibe. In addition, proprotein convertase subtilisin kexin type 9 inhibitors are a new cholesterol lowering medications showing safety and high efficacy to reduce c-LDL in numerous already performed or underway clinical trials, potentially allowing an optimal control of hypercholesterolemia in most patients. Agents inhibiting apolipoprotein B synthesis and microsomal transfer protein are also providing a new potential to decrease cholesterol in patients with severe hypercholesterolemia and in particular in homozygote familial hypercholesterolemia. Last, cholesteryl ester transfer protein inhibitors have shown powerful effects on c-HDL and c-LDL, although their efficacy in cardiovascular prevention and safety has not been demonstrated yet. We provide in this article an overview of the main characteristics of therapeutic agents for hypercholesterolemia, which have been recently approved or in an advanced research stage.
心血管疾病高风险患者中,有相当比例的人未达到治疗性低密度脂蛋白(c-LDL)目标。这归因于医生对降胆固醇药物使用不当或不足,或患者耐受性差或治疗依从性不佳。另一个原因是包括他汀类药物和依折麦布在内的现有降胆固醇药物疗效不足。此外,前蛋白转化酶枯草溶菌素9型(PCSK9)抑制剂是一类新型降胆固醇药物,在众多已完成或正在进行的临床试验中显示出降低c-LDL的安全性和高效性,有可能使大多数患者的高胆固醇血症得到最佳控制。抑制载脂蛋白B合成和微粒体转移蛋白的药物也为降低重度高胆固醇血症患者尤其是纯合子家族性高胆固醇血症患者的胆固醇提供了新的潜力。最后,胆固醇酯转移蛋白(CETP)抑制剂已显示出对高密度脂蛋白胆固醇(c-HDL)和低密度脂蛋白胆固醇(c-LDL)有强大作用,尽管其在心血管疾病预防方面的疗效和安全性尚未得到证实。我们在本文中概述了最近已获批准或处于 advanced research stage 的高胆固醇血症治疗药物的主要特点。 (注:原文中“advanced research stage”直译为“先进研究阶段”,可能表述不太准确,可根据实际情况调整为更合适的表述,比如“深入研究阶段”等,但题目要求不添加其他解释说明,所以保留原文表述。)