冠状动脉粥样硬化性心脏病（coronary atherosclerotic heart disease，CHD）的发病率及病死率居全球首位，而低密度脂蛋白胆固醇（low density lipoprotein-cholesterol，LDL-C）的升高是 CHD 的主要危险因素，因此降低 LDL-C 水平可有效减少 CHD 的发病风险。临床上降脂药物如他汀类虽能够有效降低 LDL-C 水平，但仍有部分患者无法达到降脂目标或者无法耐受。前蛋白转化酶枯草溶菌素 9（proprotein convertase subtilisin/kexin type 9，PCSK9）抑制剂作为新一代的降脂药物，越来越受到重视。其通过对 PCSK9 的抑制作用，增加低密度脂蛋白受体的循环利用，能够显著降低血清中 LDL-C 水平。目前 PCSK9 抑制剂已进入Ⅲ期临床试验，试验结果显示其具有良好的降脂效果和耐受性。该文就 PCSK9 抑制剂最新进展和面临的问题作一综述。

Coronary atherosclerotic heart disease (CHD) remains the leading cause of morbidity and mortality in the world, with elevated low density lipoprotein-cholesterol (LDL-C) levels as a major risk factor. Lower levels of LDL-C can effectively reduce the risk of CHD. To date, lipid-lowering medicines such as statins are effective in lowering LDL-C, but a proportion of patients do not achieve lipid reduction target with statins or are intolerant to statins. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are a new class of agents reducing LDL-C which gain more and more concerns. Through inhibitory effect on PCSK9 and increasing low-density lipoprotein receptors recycling, they can significantly reduce serum LDL-C levels. PCSK9 inhibitors are currently in phase Ⅲ of clinical trials, and the results showed that they had good lipid-lowering effects and tolerability. This review provided an overview of the latest advances and challenges about PCSK9 inhibitors.