The atheroprotective role of high-density lipoprotein cholesterol (HDL-C) in cardiovascular disease has been unequivocally established, and epidemiological data have clearly demonstrated a strong inverse relationship between HDL-C levels and the risk of cardiovascular events, which is independent of the low-density lipoprotein cholesterol (LDL-C) levels. Thus, it would be logical to hypothesize that raising HDL-C might potentially lead to a reduction of cardiovascular risk. Cholesteryl ester transfer protein (CETP) promotes the transfer of cholesteryl esters from HDL to very low-density lipoprotein and LDL. Therefore, CETP inhibition raises HDL-C levels and decreases LDL-C levels. The first trials with CETP inhibitors failed to show a reduction in cardiovascular events. However, newer CETP inhibitors with more favorable effects on lipids are presently being tested in clinical trials with the hope that their use may lead to a reduction in cardiovascular risk. This review aims to provide the current evidence regarding CETP inhibition, as well as the clinical and scientific data pertaining to the new CETP inhibitors in development.

ABSTRACT:The role of low-density lipoprotein cholesterol (LDL-C) in the pathophysiology of atherosclerosis is well recognized, and statin therapy represents the standard of care for LDL-C lowering and reduction of cardiovascular risk. However, many patients fail to achieve LDL-C goals, whereas others are intolerant to statins due to side effects. Unfortunately, until recently, the efficacy of other nonstatin LDL-C-lowering agents was limited, achieving an LDL-C reduction of no more than 20%. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors represent a new class of LDL-lowering agents, producing large reductions in LDL-C. Alirocumab is a PCSK9 inhibitor, which was recently approved by the Food and Drug Administration as an adjunct to diet and maximally tolerated statin therapy for treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease who require additional lowering of LDL-C levels. This review aims to provide the current clinical and scientific data pertaining to the treatment of hypercholesterolemia with alirocumab.

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