New approaches to atherosclerotic cardiovascular disease. the potentialities of torcetrapib.

Abstract

Atherosclerosis is the leading cause of death and disability in the developed world. Although the low-density lipoprotein (LDL) cholesterol lowering drugs reduce the mortality and morbidity associated with coronary artery disease, considerable mortality and morbidity remains. Reverse cholesterol transport mediated by high-density lipoproteins (HDL) may provide an independent pathway for lipid removal from atheroma. The current NCEP ATPIII include HDL-cholesterol > or =1.6 mmol/l as a negative risk factor. Torcetrapib is an inhibitor of cholesteryl ester-transfer protein (CETP) that increases high-density lipoprotein (HDL) cholesterol levels. The drug increases HDL-cholesterol and apolipoprotein A-I levels and decreases LDL-cholesterol and apolipoprotein B levels. The effect is showed in monotherapy and when administered in combination with statins. In addition, torcetrapib did not significantly change the serum levels of cholesterol and triglycerides. The raising HDL-cholesterol with torcetrapib could be a new approach to atherosclerotic cardiovascular disease although new trials based on hard clinical end points are necessary.

• Authors: Jose Luis Pérez-Castrillon, Antonio Dueñas-Laita
• Journal: Recent patents on cardiovascular drug discovery (Recent Pat Cardiovasc Drug Discov) Vol. 1 Issue 1 Pg. 109-14 (Jan 2006) United Arab Emirates
• PMID: 18221079 (Publication Type: Journal Article, Review)

Chemical References

• Anticholesteremic Agents
• Cholesterol Ester Transfer Proteins
• Cholesterol, HDL
• Quinolines
• torcetrapib
• Cholesterol

Topics

• Animals
• Anticholesteremic Agents (therapeutic use)
• Atherosclerosis (drug therapy)
• Cholesterol (metabolism)
• Cholesterol Ester Transfer Proteins (antagonists & inhibitors)
• Cholesterol, HDL (physiology)
• Humans
• Macrophages (metabolism)
• Quinolines (pharmacology, therapeutic use)