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前蛋白转化酶枯草溶菌素9(PCSK9)是前蛋白转化酶家族成员之一,它通过与肝细胞表面低密度脂蛋白受体(LDLR)结合,使体内低密度脂蛋白水平升高,引发高血脂。PSCK9抑制剂可以达到降低血脂的临床效果并已经成为重要的减少冠心病发病率的药物靶点。尤其是单克隆抗体药物,作为目前唯一的具有降脂功能的单克隆抗体,在临床试验上的表现对于家族遗传性高血脂的治疗及冠心病的防治都具有重要意义。本文将主要对PCSK9的作用机制及其单克隆抗体的研发现状、临床试验进展进行总结,旨在对降脂单抗药物研发与临床应用作为参考。
Prokaryotic invertase Subtilosin 9 (PCSK9) is a member of the proprotein convertase family that binds to low density lipoprotein receptors (LDLRs) on the surface of hepatocytes to raise the level of low density lipoprotein (LDL) in the body and trigger high Blood lipids. PSCK9 inhibitors can achieve the clinical effect of lowering blood fat and has become an important drug target for reducing the incidence of coronary heart disease. Especially monoclonal antibody drugs, as the only monoclonal antibody with lipid-lowering function in clinical trials, are of great significance for the treatment of familial hyperlipidemia and prevention and treatment of coronary heart disease. This article will mainly PCSK9 mechanism of action and monoclonal antibody research and development status, clinical trials are summarized, aimed at lipid-lowering monoclonal antibody drug development and clinical application as a reference.