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血脂异常与心血管疾病:聚焦前蛋白转化酶枯草溶菌素 9 抑制剂的作用。

Dyslipidaemias and Cardiovascular Disease: Focus on the Role of PCSK9 Inhibitors.

机构信息

School of Biomedical Engineering and Imaging Sciences, King's College London, 4th Floor, Lambeth Wing St. Thomas' Hospital, London SE1 7EH, United Kingdom.

UCL Institute of Cardiovascular Sciences, London, United Kingdom.

出版信息

Curr Med Chem. 2020;27(27):4494-4521. doi: 10.2174/0929867326666190827151012.

DOI:10.2174/0929867326666190827151012
PMID:31453780
Abstract

Genetic, experimental and clinical studies have consistently confirmed that inhibition of Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) can result in significant lowering of LDL-C and two fully human PCSK9 monoclonal antibodies have received regulatory approval for use in highrisk patients. Co-administration of PCSK9 with statins has resulted in extremely low LDL-C levels with excellent short-term safety profiles. While results from Phase III clinical trials provided significant evidence about the role of PCSK9 inhibitors in reducing cardiovascular event rates, their impact on mortality remains less clear. PCSK9 inhibitor therapy can be considered for high-risk patients who are likely to experience significant cardiovascular risk reduction.

摘要

遗传、实验和临床研究一致证实,抑制前蛋白转化酶枯草溶菌素/柯萨奇蛋白酶 9(PCSK9)可显著降低 LDL-C,两种完全人源化的 PCSK9 单克隆抗体已获得监管部门批准用于高危患者。PCSK9 与他汀类药物联合使用可使 LDL-C 水平极低,且具有极好的短期安全性。虽然 III 期临床试验的结果提供了关于 PCSK9 抑制剂在降低心血管事件发生率方面作用的重要证据,但它们对死亡率的影响尚不清楚。PCSK9 抑制剂治疗可考虑用于可能经历显著心血管风险降低的高危患者。

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