Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a crucial protein in low density lipoprotein cholesterol (LDL-C) metabolism. It binds the low density lipoprotein receptor (LDLR) and returns the LDLR to degradation in the lysosome and thereby raises the plasma levels of LDL-C. Gain-of-function (GOF) and loss-of-function (LOF) of PCSK9 mutations result in hypercholesterolemia and hypocholesterolemia, respectively. Several studies have reported the classical lipid-lowering drugs (e.g. statin, ezetamibe, fibrates) caused the increasing of PCSK9 in serum and thus failed to protect patients from cardiovascular events. Consequently, the inhibition of PCSK9 has emerged as a novel target for lipid lowering therapy. In this review, the current PCSK9 inhibitors including gene silencing, mimic peptides, and monoclonal antibodies which are developing and evaluating in the clinical trials are summarized.