CETP

Class

Cholesteryl ester transfer protein inhibitor

CETP (cholesteryl ester transfer protein) is a plasma protein that shuttles lipids between lipoprotein particles, transferring cholesteryl esters from high-density lipoprotein (HDL) to low-density lipoprotein (LDL) and very-low-density lipoprotein (VLDL), while moving triglycerides in the opposite direction. This exchange is part of normal lipid trafficking, but it also limits how much cholesterol HDL can return to the liver for excretion, a process called reverse cholesterol transport. Inhibiting CETP raises HDL cholesterol and lowers LDL cholesterol, a profile of interest for reducing atherosclerotic cardiovascular disease risk, since LDL delivers cholesterol into arterial walls while HDL is broadly associated with cholesterol removal. Small-molecule CETP inhibitors bind directly to the protein and block its lipid-shuttling activity. As a class, these agents have been explored for prevention of cardiovascular events, particularly in people with elevated LDL despite standard lipid-lowering therapy or with low HDL. Differences in chemical structure and potency among CETP inhibitors translate into differences in the degree of HDL raising and LDL lowering achieved, and this heterogeneity has been central to understanding which biological effects of CETP inhibition actually correspond to reduced cardiovascular risk rather than simply altered cholesterol numbers.