Effects of the acyl coenzyme A:cholesterol acyltransferase inhibitor avasimibe on human atherosclerotic lesions

Circulation

Volumn 110, Issue 21, 2004, Pages 3372-3377

  Tardif, Jean Claude ^a   Grégoire, Jean ^a   L'Allier, Philippe L ^a   Anderson, Todd J ^a   Bertrand, Olivier ^a   Reeves, Francois ^a   Title, Lawrence M ^a   Alfonso, Fernando ^a   Schampaert, Erick ^a   Hassan, Alita ^a   McLain, Richard ^a   Pressler, Milton L ^a   Ibrahim, Reda ^a   Lespérance, Jacques ^a   Blue, John ^a   Heinonen, Therese ^a   Rodés Cabau, Josep ^a  

^a MONTREAL HEART INSTITUTE   (Canada)

Author keywords

Atherosclerosis; Enzymes; Ultrasonics

Indexed keywords

APOLIPOPROTEIN B; AVASIMIBE; C REACTIVE PROTEIN; CHOLESTEROL; CHOLESTEROL ACYLTRANSFERASE; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; LOW DENSITY LIPOPROTEIN CHOLESTEROL; PLACEBO; TRIACYLGLYCEROL;

ADULT; AGED; ANGIOCARDIOGRAPHY; ARTICLE; ATHEROSCLEROTIC PLAQUE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CORONARY ARTERY ATHEROSCLEROSIS; DEATH; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG EFFICACY; DRUG TOLERABILITY; ENZYME INHIBITION; FEMALE; HEART INFARCTION; HUMAN; INTRAVASCULAR ULTRASOUND; LIPOPROTEIN BLOOD LEVEL; LIVER DYSFUNCTION; MACROPHAGE; MALE; MULTICENTER STUDY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; STATISTICAL ANALYSIS;

ACETATES; AGED; ANTILIPEMIC AGENTS; APOLIPOPROTEINS B; BIOLOGICAL MARKERS; C-REACTIVE PROTEIN; CHOLESTEROL, LDL; CORONARY ARTERIOSCLEROSIS; DOUBLE-BLIND METHOD; DRUG THERAPY, COMBINATION; FEMALE; HUMANS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; IMAGE PROCESSING, COMPUTER-ASSISTED; MALE; MIDDLE AGED; STEROL O-ACYLTRANSFERASE; SULFONIC ACIDS; TREATMENT FAILURE; ULTRASONOGRAPHY, INTERVENTIONAL;

EID: 20844449696     PISSN: 00097322     EISSN: None     Source Type: Journal    
DOI: 10.1161/01.CIR.0000147777.12010.EF     Document Type: Article

References (29)

1. Heinonen TM. Inhibition of acyl coenzyme A-cholesterol acyltransferase: a possible treatment of atherosclerosis. Curr Atheroscler Rep. 2002;4:65-70.
2. Suckling KE, Stange EF. Role of acyl-CoA-cholesterol acyl-transferase in cellular cholesterol metabolism. J Lipid Res. 1985;26:647-671.
3. Chang CC, Huh HY, Cadigan KM, Chang TY. Molecular cloning and functional expression of human acyl-coenzyme A:cholesterol acyltransferase cDNA in mutant Chinese hamster ovary cells. J Biol Chem. 1993;268:20747-20755.
4. Miyazaki A, Sakashita N, Lee O, Takahashi K, Horiuchi S, Hakamata H, Morganelli PM, Chang CC, Chang TY. Expression of ACAT-1 protein in human atherosclerotic lesions and cultured human monocytes-macrophages. Arterioscler Thromb Vasc Biol. 1998;18:1568-1574.
5. Cases S, Novak S, Zheng YW, Myers HM, Lear SR, Sande E, Welch CB, Lusis AJ, Spencer TA, Krause BR, Erickson SK, Farese RV Jr. ACAT-2, a second mammalian acyl-CoA:cholesterol acyltransferase: its cloning, expression and characterization. J Biol Chem. 1998;273:26755-26764.
6. Bocan TMA, Mueller SB, Uhlendorf PD. Inhibition of acyl-CoA cholesterol O-acyltransferase reduces the cholesteryl ester enrichment of atherosclerotic lesions in the Yucatan micropig. Atherosclerosis. 1993;99:175-186.
7. Kusunoki J, Hansoty DK, Aragane K, Fallon JT, Badimon JJ, Fisher EA. Acyl-CoA:cholesterol acyltransferase inhibition reduces atherosclerosis in apolipoprotein E-deficient mice. Circulation. 2001;103:2604-2609.
8. Wilcox LJ, Barren PH, Newton RS, Huff MW. ApoB100 secretion from HepG2 cells is decreased by the ACAT inhibitor CI-1011: an effect associated with enhanced intracellular degradation of apoB. Arterioscler Thromb Vasc Biol. 1999;19:939-949.
9. Taghibiglou C, Van Iderstine S, Kulinski A, Rudy D, Adeli K. Intracellular mechanisms mediating the inhibition of apoB-containing lipoprotein synthesis and secretion in HepG2 cells by avasimibe (CI-1011), a novel acyl-coenzyme Axholesterol acyltransferase (ACAT) inhibitor. Biochem Pharmacol. 2002;63:349-360.
10. Delsing DJ, Offerman EH, van Duyvenvoorde W, van Der Boom H, de Wit EC, Gijbels MJ, van Der Laarse A, Jukema JW, Havekes LM, Princen HM. Acyl-CoA:cholesterol acyltransferase inhibitor avasimibe reduces atherosclerosis in addition to its cholesterol-lowering effect in ApoE*3-Leiden mice. Circulation. 2001;103:1778-1786.
11. Nicolosi RJ, Wilson TA, Krause BR. The ACAT inhibitor, CI-1011, is effective in the prevention and regression of aortic fatty streak area in hamsters. Atherosclerosis. 1998;137:77-85.
12. Bocan TM, Krause BR, Rosebury WS, Mueller SB, Lu X, Dagle C, Major T, Lathia C, Lee H. The ACAT inhibitor avasimibe reduces macrophages and matrix metalloproteinase expression in atherosclerotic lesions of hypercholesterolemic rabbits. Arterioscler Thromb Vasc Biol. 2000;20:70-79.
13. Bocan TM, Krause BR, Rosebury WS, Lu X, Dagle C, Bak Mueller S, Auerbach B, Sliskovic DR. The combined effect of inhibiting both ACAT and HMG-CoA reductase may directly induce atherosclerotic lesion regression. Atherosclerosis. 2001;157:97-105.
14. Bocan TM, Mueller SB, Brown EQ, Lee P, Bocan MJ, Rea T, Pape ME. HMG-CoA reductase and ACAT inhibitors act synergistically to lower plasma cholesterol and limit atherosclerotic lesion development in the cholesterol-fed rabbit. Atherosclerosis. 1998;139:21-30.
15. Insull W Jr, Koren M, Davignon J, Sprecher D, Schrott H, Keilson LM, Brown AS, Dujovne CA, Davidson MH, McLain R, Heinonen T. Efficacy and short-term safety of a new ACAT inhibitor, avasimibe, on lipids, lipoproteins, and apolipoproteins, in patients with combined hyperlipidemia. Atherosclerosis. 2001;157:137-144.
16. Raal FJ, Marais AD, Klepack E, Lovalvo J, McLain R, Heinonen T. Avasimibe, an ACAT inhibitor, enhances the lipid lowering effect of atorvastatin in subjects with homozygous familial hypercholesterolemia. Atherosclerosis. 2003;171:273-279.
17. Tardif JC, Gregoire J, Lesperance J, Lambert J, L'Allier PL, Rodes J, Anderson T, Blue JW, Imus J, Heinonen T. Design features of the avasimibe and progression of coronary lesions assessed by intravascular ultrasound (A-PLUS) clinical trial. Am Heart J. 2002;144:589-596.
18. Nissen SE, Tsunoda T, Tuzcu EM, Schoenhagen P, Cooper CJ, Yasin M, Eaton GM, Lauer MA, Sheldon WS, Grines CL, Halpern S, Crowe T, Blankenship JC, Kerensky R. Effect of recombinant ApoA-I Milano on coronary atherosclerosis in patients with acute coronary syndromes: a randomized controlled trial. JAMA. 2003;290:2292-2300.
19. Tardif JC, Gregoire J, Schwartz L, Title L, Laramee L, Reeves F, Lesperance J, Bourassa MG, L'Allier PL, Glass M, Lambert J, Guertin MC, Canadian Antioxidant Restenosis Trial (CART-1) Investigators. Effects of AGI-1067 and probucol after percutaneous coronary interventions. Circulation. 2003;107:552-558.
20. Nissen SE, Tuzcu EM, Schoenhagen P, Brown BG, Ganz P, Vogel RA, Crowe T, Howard G, Cooper CJ, Brodie B, Grines CL, DeMaria AN, REVERSAL Investigators. Effect of intensive compared with moderate lipid-lowering therapy on progression of coronary atherosclerosis: a randomized controlled trial. JAMA. 2004;291:1071-1080.
21. Tardif JC. Clinical results with AGI-1067: a novel antioxidant vascular protectant. Am J Cardiol. 2003;91(suppl):41A-49A.
22. Lee HS, Tardif JC, Harel F, Cote G, Joyal M, Gosselin G, L'Allier PL, Doucet S, de Guise P, Lesperance J, Gregoire JC, Couturier A. Effects of plaque composition on vascular remodeling after angioplasty in the MultiVitamins and Probucol (MVP) trial. Can J Cardiol. 2002;18:271-275.
23. Di Mario C, Gorge G, Peters R, Kearney P, Pinto F, Hausmann D, von Birgelen C, Colombo A, Mudra H, Roelandt J, Erbel R. Clinical application and image interpretation in intracoronary ultrasound. Eur Heart J. 1998;19:207-229.
24. Palmer ND, Northridge D, Lessells A, McDicken WN, Fox KA. In vitro analysis of coronary atheromatous lesions by intravascular ultrasound: reproducibility and histological correlation of lesion morphology. Eur Heart J. 1999;20:1701-1706.
25. Sahi J, Milad MA, Zheng X, Rose KA, Wang H, Stilgenbauer L, Gilbert D, Jolley S, Stern RH, LeCluyse EL. Avasimibe induces CYP3A4 and multiple drug resistance protein 1 gene expression through activation of the pregnane X receptor. J Pharmacol Exp Ther. 2003;306:1027-1034.
26. Burnett JR, Wilcox LJ, Telford DE, Kleinstiver SJ, Barren PH, Newton RS, Huff MW. Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs. J Lipid Res. 1999;40:1317-1327.
27. Perrey S, Legendre C, Matsuura A, Guffroy C, Binet J, Ohbayashi S, Tanaka T, Ortuno JC, Matsukura T, Laugel T, Padovani P, Bellamy F, Edgar AD. Preferential pharmacological inhibition of macrophage ACAT increases plaque formation in mouse and rabbit models of atherogenesis. Atherosclerosis. 2001;155:359-370.
28. Accad M, Smith SJ, Newland DL, Sanan DA, King LE Jr, Linton MF, Fazio S, Farese RV Jr. Massive xanthomatosis and altered composition of atherosclerotic lesions in hyperlipidemic mice lacking acyl CoA:cholesterol acyltransferase 1. J Clin Invest. 2000;105:711-719.
29. Guedes A, Tardif JC. Intravascular ultrasound assessment of atherosclerosis. Curr Atheroscler Rep. 2004;6:219-224.