Elevated levels of low-density cholesterol (LDL-C) are highly correlated with increased risk of cardiovascular diseases (CVD). Thus, current guidelines have recommended progressively lower LDL-C for cholesterol treatment and CVD prevention as the primary goal of therapy. Even so, some patients in the high risk category fail to achieve recommended LDL-C targets with currently available medications. Thereby, additional pharmaceutical strategies are urgently required. In the review, we aim to provide an overview of both current and emerging LDL-C lowering drugs. As for current available LDL-C lowering agents, attentions are mainly focused on statins, niacin, bile acid sequestrants, ezetimibe, fibrates and omega-3 fatty acids. On the other hand, the emerging drugs differ from mechanisms are including: intervention of cholesterol biosynthesis downstream enzyme (squalene synthase inhibitors), inhibition of lipoprotein assembly (antisense mRNA inhibitors of apolipoprotein B and microsomal transfer protein inhibitors), enhanced lipoprotein clearance (proprotein convertase subtilisin kexin type 9, thyroid hormone analogues), inhibition of intestinal cholesterol absorption (Niemann-Pick C1-like 1 protein and acyl coenzyme A:cholesterol acyltransferase inhibitors) and interrupting enterohepatic circulation (apical sodium-dependent bile acid transporter inhibitors). Several ongoing agents are in their different stages of clinical trials, in expectation of promising antihyperlipidemic drugs. Therefore, alternative drugs monotherapy or in combination with statins will be sufficient to reduce LDL-C concentrations to optimal levels, and a new era for better LDL-C managements is plausible.
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