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.