HDL biology
Review focuses on CETP inhibitors and ABC1-inducing nuclear receptor agonists as new HDL-raising drug approaches (Mini Rev Med Chem 2002)
Original title: New approaches to raising the HDL cholesterol level
This review argues that, alongside high LDL-cholesterol, low HDL-cholesterol is a critical risk factor for atherosclerosis and coronary heart disease, and that existing HDL-raising drugs (fibrates, niacin) have unsatisfactory effects, creating demand for better options. Among the many possible approaches to raising HDL cholesterol, the review specifically focuses on inhibitors of cholesteryl ester transfer protein (CETP) and on nuclear orphan receptor agonists that induce expression of the ATP-binding cassette transporter 1 (ABC1).
Original abstract
Not only a high level of low-density lipoprotein (LDL) cholesterol, but also a low level of high-density lipoprotein (HDL) cholesterol, is a critical risk factor for atherosclerosis and coronary heart disease. Although fibrates and niacin can be used to improve low HDL cholesterol levels, their effect is not wholly satisfactory, so better drugs for the elevation of HDL cholesterol are desired. Among the many methods that may be used to raise HDL cholesterol levels, this review focuses on inhibitors of cholesteryl ester transfer protein (CETP) and on nuclear orphan receptor agonists that mediate the expression of ATP-binding cassette transporter 1 (ABC1).
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.