BioCentury
ARTICLE | Product Development

Elevating HDL

December 11, 2006 8:00 AM UTC

Elevating HDLHigh-density lipoprotein plays a pivotal role in reverse cholesterol transport, a process that transfers excess cellular cholesterol from peripheral tissues to the liver for biliary excretion. Low levels of HDL can lead to coronary heart disease even when total cholesterol levels are normal. Although no drugs primarily aim to raise HDL, there are three major types of cardiovascular drugs that do increase HDL while lowering other cholesterol: fibrates, statins and niacin. By contrast, Pfizer's torcetrapib was intended to increase HDL by inhibiting a protein, CETP, involved in reverse cholesteol transport.

[1]Free cholesterol (FC) is generated in part by the hydrolysis of intracellular cholesteryl ester (CE) stores. Reverse cholesterol transport starts when excess FC is transferred out of peripheral cells, such as macrophages, by ATP binding cassette transporter 1 (ABC1) following ABC1's interaction with newly synthesized lipid-poor apolipoprotein A-I (Apo A-1). ...