Key result
Orally active, small molecule CETP inhibitors have been shown to reduce CETP activity and increase HDL-cholesterol in animal models and Phase II clinical trials.
Why the study?
Do CETP inhibitors reduce CETP activity and raise HDL-cholesterol in patients with hypoalphalipoproteinaemia?
Do CETP inhibitors reduce CETP activity and raise HDL-cholesterol in patients with hypoalphalipoproteinaemia?
CETP inhibitors represent a potential new therapeutic class that successfully reduces CETP activity and raises HDL-cholesterol in early clinical trials.
Supports CETP inhibitor development for HDL elevation; leaves open whether this improves outcomes in CAD.
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.
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James A. Sikorski (2006) conducted a review in Coronary artery disease / Hypoalphalipoproteinaemia. Cholesteryl ester transfer protein (CETP) inhibitors was evaluated. Orally active, small molecule CETP inhibitors have been shown to reduce CETP activity and increase HDL-cholesterol in animal models and Phase II clinical trials.
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