PCSK9
医学
可欣
高脂血症
低密度脂蛋白受体
前蛋白转化酶
剩余风险
他汀类
胆固醇
内科学
脂蛋白
内分泌学
药理学
糖尿病
作者
Xiaolan Lin,Lele Xiao,Zhi‐Han Tang,Zhi‐Sheng Jiang,Mi‐Hua Liu
标识
DOI:10.1016/j.biopha.2018.05.024
摘要
Elevated plasma low-density lipoprotein cholesterol (LDL-C) is an important risk factor for cardiovascular diseases. Statins are the most widely used therapy for patients with hyperlipidemia. However, a significant residual cardiovascular risk remains in some patients even after maximally tolerated statin therapy. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a new pharmacologically therapeutic target for decreasing LDL-C. PCSK9 reduces LDL intake from circulation by enhancing LDLR degradation and preventing LDLR recirculation to the cell surface. Moreover, PCSK9 inhibitors have been approved for patients with either familial hypercholesterolemia or atherosclerotic cardiovascular disease, who require additional reduction of LDL-C. In addition, PCSK9 inhibition combined with statins has been used as a new approach to help reduce LDL-C levels in patients with either statin intolerance or unattainable LDL goal. This review will discuss the emerging anti-PCSK9 therapies in the regulation of cholesterol metabolism and atherosclerosis.
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