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前蛋白转化酶枯草溶菌素9(proprotein convertase subtilisin/kexin type 9,PCSK9)是一种由肝脏合成的丝氨酸激酶,可促使体内低密度脂蛋白胆固醇(LDL-C)累积,抑制PCSK9活性则可使LDL-C水平显著下降。Evolocumab(商品名Repatha)是由美国安进公司研发的全球第一个PCSK9抑制剂,2015年7月在欧盟上市,被批准用于治疗原发性和家族性高胆固醇血症。该药的特别之处在于能大幅降低他汀类药物耐受患者体内的LDL-C,因此可有效解决广泛使用他汀类药物后出现的大面积耐药问题。笔者就Evolocumab的基本性质、作用机制、药效学、药动学、临床应用、研发历程等情况作一概述,以期能为医院临床用药及药物开发提供参考。
Proprotein convertase subtilisin / kexin type 9 (PCSK9), a serine kinase synthesized by the liver, promotes the accumulation of low density lipoprotein cholesterol (LDL-C) in vivo and inhibits the activity of PCSK9 LDL-C levels decreased significantly. Evolocumab (trade name Repatha) is the world’s first PCSK9 inhibitor developed by Amgen. It was marketed in the EU in July 2015 and approved for the treatment of primary and familial hypercholesterolemia. The drug is unique in that it significantly reduces the LDL-C levels in statins-tolerant patients and therefore effectively addresses the large-area drug resistance problems that occur after the widespread use of statins. The author of Evolocumab basic properties, mechanism of action, pharmacodynamics, pharmacokinetics, clinical application, research and development process and so on to make an overview, with a view to clinical hospitals for the drug and drug development to provide a reference.