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Drug Evaluations

Darapladib

, MD & , MD
Pages 161-168 | Published online: 10 Dec 2009

Bibliography

  • Smith SC, Allen J, Blair SN, AHA/ACC guidelines for secondary prevention for patients with coronary and other atherosclerotic vascular disease: 2006 update: endorsed by the National Heart, Lung, and Blood Institute. Circulation 2006;113:2363-72
  • Rosamond W, Flegal K, Friday G, Heart disease and stroke statistics – 2007 update. Circulation 2007;115:e69-171
  • Cannon CP, Braunwald E, McCabe CH, Pravastatin or atorovastatin evaluation, infection, therapy-thombolysis in myocardial infarction 22 investigators: intensive versus moderate lipid lowering with statins after acute coronary syndromes. N Engl J Med 2004;350:1495-504
  • Heart Protection Study Collaborative Group. MRC/BHF heart protection study of cholesterol lowering with simvastatin in 20,536 high-risk individuals: a randomized placebo-controlled trial. Lancet 2002;360:7-22
  • Steg PG, Bhatt DL, Wilson PW, One-year cardiovascular event rates in outpatients with atherothrombosis. JAMA 2007;297:1197-206
  • Hasson GK. Inflammation, atherosclerosis, and coronary artery disease. N Engl J Med 2005;352:1685-95
  • Wilensky RL, Hamamdzic D. Molecular basis for the vulnerable plaque: potential therapeutic role for immunomodulation. Curr Opin Cardiol 2007;22:545-51
  • Wymann MP, Schnieter R. Lipid signalling in disease. Nat Rev 2008;9:162-76
  • Zalewski A, Nelson JJ, Hegg L, Macphee C. Lp-PLA2: a new kid on the block. Clin Chem 2006;52:1645-50
  • Rosenson RS. Future role of selective phospholipase A2 inhibitors in the prevention atherosclerotic cardiovascular disease. Cardiovasc Drugs Ther 2009;23:93-101
  • Tjoelker LW, Wilder C, Eberhardt C, Anti-inflammatory properties of a platelet-activating factor acetylhydrolase. Nature 1995;374:549-53
  • Six DA, Dennis EA. The expanding superfamily of phospholipase A(2) enzymes: classification and and characterization. Biochem Biophys Acta 2000;1488:1-19
  • Min JH, Jain MK, Wilder C, Membrane-bound platelet activating factor acetylhydrolase acts on substrate in the aqueous phase. Biochemistry 1999;38:12935-42
  • Stafforini DM, Elstad MR, McIntyre TM, Human macrophages secrete platelet-activating factor acetylhydrolase. J Biol Chem 1990;265:9682-7
  • Stafforini DM, Tjoelker LW, McCormick SP, Molecular basis of the interaction between plasma platelet-activating factor-acetylhydrolase and low density lipoprotein. J Biol Chem 1999;274:7018-24
  • Tsimikas S, Tsironis LD, Tselepis AD. New insights into the role of lipoprotein(a)-associated lipoprotein-associated phospholipase A2 in atherosclerosis and cardiovascular disease. Arterioscler Thromb Vasc Biol 2007;27:2094-9
  • Benítez S, Camacho M, Arcelus R, Increased lysophosphotidylcholine and non-esterified fatty acid content in LDL induces chemokine release in endothelial cells. Relationship with electronegative LDL. Atherosclerosis 2004;177:299-305
  • Watson AD, Leitinger N, Navab M, Structural identification by mass spectrometry of oxidized phospholipids in minimally oxidized low density lipoprotein that induce monocyte/endothelial interactions and evidence for their presence in vivo. J Biol Chem 1997;272:13597-607
  • Subbanagounder G, Leitinger N, Schwenke DC, Determinants of bioactivity of oxidized phospholipids: Specific oxidized fatty acyl groups at the sn-2 position. Arterioscler Thromb Vasc Biol 2000;20:2248-54
  • Subbanagounder G, Wong JW, Lee H, Epoxyisoprostane and epoxycyclopentenone phospholipids regulate monocyte chemotactic protein-1 and interleukin –8 synthesis. Formation of these oxidized phospholipids in response to interleukin-1beta. J Biol Chem 2002;277:7271-81
  • Hara A, Taketomi T. Characterization and change of phospholipids in the aorta of Watanabe hereditable hyperlipidemic rabbit. Jpn J Exp Med 1990;60:311-18
  • Packard CJ, O'Reilly DS, Caslake MJ, Lipoprotein-associated phospholipase A2 as an independent predictor of coronary heart disease: West of Scotland Coronary Prevention Group. N Engl J Med 2000;343:1148-55
  • Ballantyne CM, Hoogeveen RC, Bang H, Lipoprotein-associated phospholipase A2, high-sensitivity C-reactive protein and risk for incident coronary heart disease in middle-aged men and women in the Atherosclerosis Risk in Communities (ARIC) study. Circulation 2004;109:837-42
  • Oei HH, van der Meer IM, Hofman A, Lipoprotein-associated phospholipase A2 activity is associated with risk of coronary heart disease and ischemic stroke: the Rotterdam Study. Circulation 2005;111:570-5
  • Anderson JL. Lipoprotein-associated phospholipase A2: an independent predictor of coronary artery disease events in primary and secondary prevention. Am J Cardiol 2008;101:23-33F
  • Bui QT, Prempeh M, Wilensky WL. Atherosclerotic plaque development. Int J Biochem Cell Biol 2009;41:2109-13
  • Zalewski A, Macphee C. Role of lipoprotein-associated phospholipase A2 in atherosclerosis: biology, epidemiology, and possible therapeutic target. Arterioscler Thromb Vasc Biol 2005;25:923-31
  • Kume N, Cybulsky MI, Gimbrone MA Jr. Lysophosphatidylcholine, a component of atherogenic lipoproteins, induces mononuclear leukocyte adhesion molecules in cultured human and rabbit arterial endothelial cells. J Clin Invest 1992;90:1138-44
  • Zhu Y, Lin JH, Liao HL, Activation of ICAM-1 promoter by lysophosphatidylcholine: possible involvement of protein tyrosine kinases. Biochim Biophys Acta 1997;1345:93-8
  • McMurray HF, Parthasarathy S, Steinberg D. Oxidatively modified low density lipoprotein is a chemoattractant for human T lymphocytes. J CIin Invest 1993;92:1004-8
  • Chai YC, Howe PH, DiCorleto PE, Chisolm GM. Oxidized low density lipoprotein and lysophosphatidylcholine stimulate cell cycle entry in vascular smooth muscle cells. Evidence for release of fibroblast growth factor 2. J Biol Chem 1996;271:17791-7
  • Chang MY, Tsoi C, Wight TN, Chait A. Lysophosphatidylcholine regulates synthesis of biglycan and the proteoglycan form of macrophage colony stimulating factor. Arterioscler Thromb Vasc Biol 2003;23:809-15
  • MacPhee CH, Moores KE, Boyd HF, Lipoprotein-associated phospholipase A2, platelet-activating factor acetylhydrolase, generates two bioactive products during the oxidation of low-density lipoprotein: use of a novel inhibitor. Biochem J 1999;338:479-87
  • Macphee CH. Lipoprotein-associate phospholipase A2: a potential new risk factor for coronary artery disease and therapeutic target. Curr Opin Pharmacol 2001;1:121-5
  • Mangin EL, Kugiyama K, Nguy JH, Effects of lysolipids and oxidatively modified low density lipoprotein on endothelium-dependent relaxation of rabbit aorta. Circ Res 1993;72:161-6
  • Takahashi M, Takahashi S, Shimpo M, beta-very low density lipoprotein enhances inducible nitric oxide synthase expression in cytokine-stimulated vascular smooth muscle cells. Atherosclerosis 2002;162:307-13
  • Hsieh CC, Yen MH, Liu HW, Lau YT. Lysophosphatidylcholine induces apoptotic and non-apoptotic death in vascular smooth muscle cells: in comparison with oxidized LDL. Atherosclerosis 2000;151:481-91
  • Carpenter KL, Dennis IF, Challis IR, Inhibition of lipoprotein-associated phospholipase A2 diminishes the death-inducing effects of oxidized LDL on human monocyte-macrophages. FEBS Lett 2001;505:357-63
  • Mohler ER III, Sarov-Blat L, Shi Y, Site-specific atherogenic gene expression correlates with subsequent variable lesion development in coronary and peripheral vasculature. Arterioscler Thromb Vasc Biol 2008;28:850-5
  • Shi Y, Zhang P, Zhang L, Role of lipoprotein-associated phospholipase A2 in leukocyte activation and inflammatory response. Atherosclerosis 2007;191:54-62
  • Wilensky RL, Shi Y, Mohler ER 3rd, Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development. Nat Med 2008;14:1059-66
  • Häkkinen T, Luoma JS, Hiltunen MO, Lipoprotein-associated phospholipase A(2), platelet-activating factor acetylhydrolase, is expressed by macrophages in human and rabbit atherosclerotic lesions. Arterioscler Thromb Vasc Biol 1999;19:2909-17
  • Kolodgie FD, Burke AP, Skorija KS, Lipoprotein-associated phospholipase A2 protein expression in the natural progression of human coronary atherosclerosis. Arterioscler Thromb Vasc Biol 2006;26:2523-9
  • Rosenson RS, Vracar-Grabar M, Helenowski I. Lipoprotein associated phospholipase A2 inhibition reduces generation of oxidized fatty acids: Lp-LPA2 reduces oxidized fatty acids. Cardiovasc Drugs Ther 2008;22:55-8
  • Stafforini DM, Satoh K, Atkinson DL, Platelet-activating factor acetylhydrolase deficiency. A missense mutation near the active site of an anti-inflammatory phospholipase. J CIin Invest 1996;97:2689-90
  • Ishihara M, Iwasaki T, Nagano M, Functional impairment of two novel mutations detected in lipoprotein-associated phospholipase A2 (Lp-PLA2) deficiency patients. J Hum Genet 2004;49:302-7
  • Hiramoto M, Yoshida H, Imaizumi T, A mutation in plasma platelet-activating factor acetylhydrolase (Val279→Phe) is a genetic risk factor for stroke. Stroke 1997;28:2417-20
  • Yamada Y, Ichihara S, Fujimura T, Yokota M. Identification of the G994 → T missense in exon 9 of the plasma platelet-activating factor acetylhydrolase gene as an independent risk factor for coronary artery disease in Japanese men. Metabolism 1998;47:177-81
  • Unno N, Nakamura T, Kaneko H, Plasma platelet-activating factor acetylhydrolase deficiency is associated with atherosclerotic occlusive disease in Japan. J Vasc Surg 2000;32:263-7
  • Unno N, Nakamura T, Mitsuoka H, Association of a G994 → T missense mutation in the plasma platelet-activating factor acetylhydrolase gene with risk of abdominal aortic aneurysm in Japanese. Ann Surg 2002;235:297-302
  • Yamada Y, Izawa H, Ichihara S, Prediction of the risk of myocardial infarction from polymorphisms in candidate genes. N Engl J Med 2002;347:1916-23
  • Darapladib chemical structure; internet communication (Wikimedia). Available from: http://commons.wikimedia.org/wiki/File:Darapladib_structure.svg [last accessed 29 March 2009]
  • Blackie JA, Bloomer JC, Brown MJ, The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett 2003;13:1067-70
  • Schaloske RH, Dennis EA. The phospholipase A2 superfamily and its group numbering system. Biochim Biophys Acta 2006;1761:1246-59
  • Johnson A, Zalewski A, Janmohamed S, Lipoprotein-associated phospholipase A2 activity, an emerging CV risk marker, can be inhibited in atherosclerotic lesions and plasma by novel pharmacologic intervention: the results of a multicenter clinical study. Circulation 2004;110:III-590
  • Mohler ER 3rd, Ballantyne CM, Davidson MH, ; Darapladib Investigators. The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. J Am Coll Cardiol 2008;51:1632-41
  • Serruys PW, García-García HM, Buszman P, ; Integrated Biomarker and Imaging Study-2 Investigators. Effects of the direct lipoprotein-associated phospholipase A(2) inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 2008;118:1172-82
  • STABILITY. ClincialTrials.gov. 2009 (Internet communication). Available from: http://www.clinicaltrials.gov/ct2/show/NCT00799903?term=darapladib+stability&rank=1 [last accessed 3 December 2009]
  • McConnell JP, Jaffe AS. The spin stops here: inhibition of lipoprotein-associated Phospholipase A2 – a promising target but a negative initial trial? Clin Chem 2009;55:21-3

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