Cholesteryl ester transfer protein inhibitors as potential new therapies for coronary artery disease

Abstract

Cholesteryl ester transfer protein (CETP) inhibitors represent a potential new approach for treating cardiovascular disease in hypoalphalipoproteinaemia patients who are at particularly high risk by having low high-density lipoprotein (HDL)-cholesterol (HDLc). Although challenging and controversial as a drug target, several companies have recently identified multiple, diverse, potent inhibitor classes that reduce CETP activity and raise HDLc after oral dosing in animal models. Two candidates have independently completed successful Phase II clinical trails demonstrating a reduction in CETP activity and a concomitant increase in HDLc after oral dosing. This review highlights recent developments and patent activities for orally active, small molecule inhibitors of CETP.

Keywords::

• CETP
• cardiovascular risk
• CETP inhibitors
• cholesterol
• cholesteryl ester
• cholesteryl ester transfer protein
• coronary artery disease
• high-density lipoprotein
• JTT-705
• low-density lipoprotein
• reverse cholesterol transport
• torcetrapib