Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a novel circulating protein, which plays an important role in the regulation of cholesterol metabolism. Over the past decade, experimental and clinical studies have established that over- or poor expression of PCSK9 had a key impact not only on circulating PCSK9 and low density lipoprotein cholesterol (LDL-C) levels but also on cardiovascular risk and atherosclerotic process. Since the first discovery of PCSK9-related gene in 2003, factors that can influence circulating PCSK9 concentration are of great interest in a variety of medical fields, especially in pharmacology. In this review we focus on the impact of lipid-lowering drugs on circulating PCSK9 concentration and its clinical implications in order to optimal consideration for the current strategies with regard to cholesterol control.