Inhibition of acyl-CoA cholesterol acyltransferase by F12511 (Eflucimibe): could it be a new antiatherosclerotic therapeutic?
Lipid-lowering strategies, particularly with statins, have been extremely useful in the prevention of cardiovascular disease. However, many patients who receive statin monotherapy do not achieve the desired cardiovascular benefits. Accumulation of cholesteryl esters within macrophages constitutes the hallmark of foam cells during atherogenesis. The action of acyl-coenzyme A (CoA): cholesterol acyltransferase (ACAT) leads to formation of cholesterol esters. There are two different ACAT isoforms: ACAT1 and ACAT2. A considerable interest to develop ACAT inhibitors has been emerging. This review has been focused on the current knowledge about a new ACAT inhibitor, F12511 or eflucimibe, and more particularly on its antiatherosclerotic properties.
López-Farré
Antonio José
AJ
Cardiovascular Research Unit, Cardiovascular Institute, Hospital Clínico San Carlos, Madrid, Spain.
Sacristán
Daniel
D
Zamorano-León
José J
JJ
San-Martín
Nuria
N
Macaya
Carlos
C
D000813:Anilides / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D050197:Atherosclerosis / Q000188:drug therapy*; D002986:Clinical Trials as Topic; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use* / Q000633:toxicity; D006801:Humans; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*
D000813:Anilides; D004791:Enzyme Inhibitors; C418062:eflucimibe; D002785:Sterol O-Acyltransferase