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Drug Evaluations

Varespladib methyl in cardiovascular disease

, MD, , PhD, , PhD & , MD
Pages 1245-1255 | Published online: 01 Sep 2010

Bibliography

  • Smith SC Jr, Allen J, Blair SN, AHA/ACC guidelines for secondary prevention for patients with coronary and other atherosclerotic vascular disease: 2006 Update. Circulation 2006;113:2363-72
  • Pepine CJ. Residual risk for secondary ischemic events in patients with atherothrombotic disease: opportunity for future improvements in patient care. Ann Med 2010;42:19-35
  • Ridker PM, Rifai N, Pfeffer MA, ; Cholesterol and Recurrent Events (CARE) Investigators. Inflammation, pravastatin, and the risk of coronary events after myocaridal infarction in patients with average cholesterol levels. Circulation 1998;98:839-44
  • Ridker PM, Cannon CP, Morrow D, ; Pravastatin or atorvastatin evaluation and infection therapy-thrombolysis in myocardial infarction 22 (PROVE IT-TIMI 22) investigators. C-reactive protein levels and outcomes after statin therapy. N Engl J Med 2005;352:20-8
  • Morrow DA, deLemos JA, Sabatine MS, Clinical relevance of C-reactive protein during follow-up of patients with acute coronary syndromes in the Aggrestat-to-Zocor Trial. Circulation 2006;114:281-8
  • Rosenson RS. Novel therapies affecting the vascular wall. In: Ballantyne CM, editor, Braunwald's Clinical Lipidology. Saunders Elsevier, Philadelphia, PA; 2008. p 553-67
  • Rosenson RS, Gelb MH. Secretory phospholipase A2: a multifaceted family of proatherogenic enzymes. Curr Cardiol Rep 2009;11:445-51
  • Delahoy PJ, Magliano DJ, Webb K, The relationship between reduction in low-density lipoprotein cholesterol by statins and reduction in risk of cardiovascular outcomes: an updated meta-analysis. Clin Ther 2009;31:236-44
  • Miller M, Cannon CP, Murphy SA, Impact of triglyceride levels beyond low-density lipoprotein cholesterol after acute coronary syndrome in the PROVE IT-TIMI 22 trial. J Am Coll Cardiol 2008;19:724-30
  • Ginsberg HN, Elam MB, ACCORD Study Group, Effects of combination lipid therapy in type 2 diabetes mellitus. N Engl J Med 2010;362:1563-74
  • Mora S, Otvos JD, Rifai N, Lipoprotein particle profiles by nuclear magnetic resonance compared with standard lipid and apolipoproteins in predicting incident cardiovascular disease in women. Circulation 2009;119:931-9
  • Otvos JD, Collins D, Freedman DS, Low-density lipoprotein and high-density lipoprotein particle subclasses predict coronary events and are favorably changed by gemfibrozil therapy in the Veterans Affairs High-Density Lipoprotein Intervention Trial. Circulation 2006;113:1556-63
  • Barter P, Gotto AM, LaRosa JC, HDL cholesterol, very low levels of LDL cholesterol, and cardiovascular events. N Engl J Med 2007;357:1301-10
  • Ishigaki Y, Oka Y, Katagiri H. Circulating oxidized LDL: a biomarker and a pathogenic factor. Curr Opin Lipidol 2009;20:363-9
  • Thompson A, Gao P, Lp-PLA(2) Studies Collaboration, The Lp-PLA2 Studies Collaboration Lipoprotein-associated phospholipase A2 and risk of coronary disease, stroke, and mortality: collaborative analysis of 32 prospective studies. Lancet 2010;375:1536-44
  • Rosenson RS. Lipoprotein-associated phospholipase A2 and risk of atherosclerotic vascular disease. Lancet 2010;375:1498-500
  • Plihtari R, Hurt-Camejo E, Oorni K, Kovanen PT. Proteolysis of LDL particles sensitizes them to phospholipolysis by secretory phospholipase A2 and secretory sphingomyelinase – a novel mechanism of enhanced LDL retention. J Lipid Res 2010. [Epub ahead of print]
  • Nissen SE, Tuzcu EM, Schoenhagen P, Statin therapy, LDL cholesterol, C-reactive protein, and coronary artery disease. N Engl J Med 2005;352:29-38
  • Ridker PM, Danielson E, Fonseca FA, Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein. N Engl J Med 2008;359:2195-207
  • Ridker PM, Morrow DA, Rose LM, Relative efficacy of atorvastatin 80 mg and pravastatin 40 mg in achieving the dual goals of low-density lipoprotein cholesterol < 70 mg/dl and C-reactive protein < 2 mg/l: an analysis of the PROVE-IT TIMI-22 trial. J Am Coll Cardiol 2005;45:1644-8
  • Burke JE, Dennis EA. Phospholipase A2 biochemistry. Cardiovasc Drugs Ther 2009;23:49-59
  • Kimura-Matsumoto M, Ishikawa Y, Komiyama K, Expression of secretory phospholipase A2s in human atherosclerosis development. Atherosclerosis 2008;196:81-91
  • Sato H, Kato R, Isogai Y, Analyses of group III secreted phospholipase A2 transgenic mice reveal potential participation of this enzyme in plasma lipoprotein modification, macrophage foam cell formation, and atherosclerosis. J Biol Chem 2008;283:33483-97
  • Ivandic B, Castellani LW, Wang XP, Role of group II secretory phospholipase A2 in atherosclerosis: 1. Increased atherogenesis and altered lipoproteins in transgenic mice expressing group IIa phospholipase A2. Arterioscler Thromb Vasc Biol 1999;19:1284-90
  • Webb NR, Bostrom MA, Szilvassy SJ, Macrophage-expressed group IIA secretory phospholipase A2 increases atherosclerotic lesion formation in LDL receptor-deficient mice. Arterioscler Thromb Vasc Biol 2003;23:263-8
  • Bostrom MA, Boyanovsky BB, Jordan CT, Group V secretory phospholipase A2 promotes atherosclerosis: evidence from genetically altered mice. Arterioscler Thromb Vasc Biol 2007;27:600-6
  • Boyanovsky B, Zack M, Forrest K, Webb NR. The capacity of group V sPLA2 to increase atherogenicity of ApoE-/- and ldlr-/- mouse LDL in vitro predicts its atherogenic role in vivo. Arterioscler Thromb Vasc Biol 2009;29:532-8
  • Boyanovsky BB, van der Westhuyzen DR, Webb NR. Group V secretory phospholipase A2-modified low density lipoprotein promotes foam cell formation by a SR-A- and CD36-independent process that involves cellular proteoglycans. J Biol Chem 2005;280:32746-52
  • Hurt-Camejo E, Camejo G. Potential involvement of type II phospholipase A2 in atherosclerosis. Atherosclerosis 1997;132:1-8
  • Hurt-Camejo E, Andersen S, Standal R, Localization of nonpancreatic secretory phospholipase A2 in normal and atherosclerotic arteries: Activity of the isolated enzyme on low-density lipoproteins. Arterioscler Thromb Vasc Biol 1997;17:300-9
  • Jonsson-Rylander AC, Lundin S, Rosengren B, Role of secretory phospholipases in atherogenesis. Curr Atheroscler Rep 2008;10:252-9
  • Rosengren B, Peilot H, Umaerus M, Secretory phospholipase A2 group V: lesion distribution, activation by arterial proteoglycans, and induction in aorta by a western diet. Arterioscler Thromb Vasc Biol 2006;26:1579-85
  • Tietge UJ, Pratico D, Ding T, Macrophage-specific expression of group IIA sPLA2 results in accelerated atherogenesis by increasing oxidative stress. J Lipid Res 2005;46:1604-14
  • Singer AG, Ghomashchi F, Le Calvez C, Interfacial kinetic and binding properties of the complete set of human and mouse groups I, II, V, X, and XII secreted phospholipases A2. J Biol Chem 2002;277:48535-49
  • Karabina SA, Brocheriou I, Le Naour G, Atherogenic properties of LDL particles modified by human group X secreted phospholipase A2 on human endothelial cell function. FASEB J 2006;20:2547-9
  • Hanasaki K, Yamada K, Yamamoto S, Potent modification of low density lipoprotein by group X secretory phospholipase A2 is linked to macrophage foam cell formation. J Biol Chem 2002;277:29116-24
  • Park D-W, Kim J-R, Kim S-Y, Akt as a mediator of secretory phospholipase A2 receptor-involved inducible nitric oxide synthase expression. J Immunol 2003;170:2093-99
  • Leitinger N, Watson AD, Hama SY, Role of group II secretory phospholipase A2 in atherosclerosis: 2. Potential involvement of biologically active oxidized phospholipids. Arterioscler Thromb Vasc Biol 1999;19:1291-8
  • Balboa MA, Balsinde J, Winstead MV, Novel group V phospholipase A2 involved in arachidonic acid mobilization in murine P388D1 macrophages. J Biol Chem 1996;271:32381-4
  • Kim YJ, Kim KP, Han SK, Group V phospholipase A2 induces leukotriene biosynthesis in human neutrophils through the activation of group iva phospholipase A2. J Biol Chem 2002;277:36479-88
  • Saegusa J, Akakura N, Wu C-Y, Pro-inflammatory secretory phospholipase A2 type IIA binds to integrins {alpha}v{beta}3 and {alpha}4{beta}1 and induces proliferation of monocytic cells in an integrin-dependent manner. J Biol Chem 2008;283:26107-15
  • Antonov AS, Kolodgie FD, Munn DH, Regulation of macrophage foam cell formation by {alpha}V{beta}3 integrin: potential role in human atherosclerosis. Am J Pathol 2004;165:247-58
  • Mallat Z, Benessiano J, Simon T, Circulating secretory phospholipase A2 activity and risk of incident coronary events in healthy men and women: the EPIC-NORFOLK Study. Arterioscler Thromb Vasc Biol 2007;27:1177-83
  • Koenig W, Vossen CY, Mallat Z, Association between type II secretory phospholipase A2 plasma concentrations and activity and cardiovascular events in patients with coronary heart disease. Eur Heart J 2009;30:2742-8
  • Kugiyama K, Ota Y, Takazoe K, Circulating levels of secretory type II phospholipase A2 predict coronary events in patients with coronary artery disease. Circulation 1999;100:1280-4
  • Liu PY, Li YH, Tsai WC, Prognostic value and the changes of plasma levels of secretory type II phospholipase A2 in patients with coronary artery disease undergoing percutaneous coronary intervention. Eur Heart J 2003;24:1824-32
  • Kugiyama K, Ota Y, Sugiyama S, Prognostic value of plasma levels of secretory type II phospholipase A2 in patients with unstable angina pectoris. Am J Cardiol 2000;86:718-22
  • Porela P, Pulkki K, Voipio-Pulkki LM, Level of circulating phospholipase A2 in prediction of the prognosis of patients with suspected myocardial infarction. Basic Res Cardiol 2000;95:413-17
  • Hartford M, Wiklund O, Mattsson Hulten L, CRP, interleukin-6, secretory phospholipase A2 group IIA, and intercellular adhesion molecule-1 during the early phase of acute coronary syndromes and long-term follow-up. Int J Cardiol 2006;108(1):55-62
  • Wiklund O, Mattsson-Hulten L, Hurt-Camejo E, Oscarsson J. Effects of simvastatin and atorvastatin on inflammation markers in plasma. J Intern Med 2002;251:338-47
  • Ryu SK, Mallat Z, Schwartz GG, The effect of high dose statin therapy on lipoprotein-associated and secretory phospholipase A2 mass and activity and ischemic events in patients with acute coronary syndromes. J Am Coll Cardiol 2010; In press
  • Grundy SM, Cleeman JI, Merz CN, Implications of recent clinical trials for the National Cholesterol Education Program Adult Treatment Panel III guidelines. Circulation 2004;110:227-39
  • LaRosa JC, Grundy SM, Waters DD, Intensive lipid lowering with atorvastatin in patients with stable coronary disease. N Engl J Med 2005;352:1425-35
  • Waters DD, Brotons C, Chiang CW, Lipid treatment assessment project 2: a multinational survey to evaluate the proportion of patients achieving low-density lipoprotein cholesterol goals. Circulation 2009;120:28-34
  • Ridker PM, Danielson E, Fonseca FA, Reduction in C-reactive protein and LDL cholesterol and cardiovascular event rates after initiation of rosuvastatin: a prospective study of the JUPITER trial. Lancet 2009;373:1175-82
  • Marathe GK, Harrison KA, Murphy RC, Bioactive phospholipid oxidation products. Free Radic Biol Med 2000;28:1762-70
  • Thommesen L, Sjursen W, Gasvik K, Selective inhibitors of cytosolic or secretory phospholipase A2 block TNF-induced activation of transcription factor nuclear factor-kappaB and expression of ICAM-1. J Immunol 1998;161:3421-30
  • Schevitz RW, Bach NJ, Carlson DG, Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2. Nat Struct Biol 1995;2(6):458-65
  • Baeuerle PA, Henkel T. Function and activation of NF-kappa B in the immune system. Annu Rev Immunol 1994;12:141-79
  • Thomas G, Bertrand F, Saunier B. The differential regulation of group II(A) and group V low molecular weight phospholipases A(2) in cultured rat astrocytes. J Biol Chem 2000;275:10876-86
  • Thommesen L, Sjursen W, Gasvik K, Selective inhibitors of cytosolic or secretory phospholipase A2 block TNF-induced activation of transcription factor nuclear factor-kappa B and expression of ICAM-1. J Immunol 1998;161:3421-30
  • Fujioka D, Saito Y, Kobayashi T, Reduction in myocardial ischemia/reperfusion injury in group X secretory phospholipase A2-deficient mice. Circulation 2008;117(23):2977-85
  • Snyder DW, Bach NJ, Dillard RD, Pharmacology of A–001/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: a new class of anti-inflammatory drugs, SPI. J Pharmacol Exp Ther 1999;288:1117-24
  • Fraser H, Hislop C, Christie RM, Varespladib (A-002), an sPLA2 inhibitor, reduces atherosclerosis and aneurysm formation in ApoE-/- mice. J Cardiovasc Pharm 2009;53:60-5
  • Schevitz RW, Bach NJ, Carlson DG, Structure-based design of the first potent and selective inhibitor of human non-pancreatic secretory phospholipase A2. Nat Struct Biol 1995;2:458-65
  • Mihelich ED, Schevitz RW. Structure-based design of a new class of anti-inflammatory drugs: secretory phospholipase A2 inhibitors, SPI. Biochim Biophys Acta 1999;1441:223-8
  • Draheim SE, Bach NJ, Dillard RD, Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides. J Med Chem 1996;39:5159-75
  • Sanz R, Castroviejo MP, Guilarte V, Regioselective synthesis of 4- and 7-alkoxyindoles from 2,3-dihalophenols: application to the preparation of indole inhibitors of phospholipase A2. J Org Chem 2007;72:5113-18
  • Dillard RD, Bach NJ, Draheim SE, Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides. J Med Chem 1996;39(26):5119-36
  • Shaposhnik Z, Wang X, Trias J, The synergistic inhibition of atherogenesis in ApoE-/- mice between pravastatin and the sPLA2 inhibitor varespladib (A-002). J Lipid Res 2009;50:623-9
  • Leite JO, Vaishnav U, Puglisi M, A-002 (Varespladib), a phospholipase A2 inhibitor, reduces atherosclerosis in guinea pigs. BMC Cardiovasc Disord 2009;9:7
  • Kennedy BP, Payette P, Mudgett J, A natural disruption of the secretory group II phospholipase A2 gene in inbred mouse strains. J Biol Chem 1995;270:22378-85
  • Shih DM, Xia YR, Wang XP, Combined serum paraoxonase knockout/apolipoprotein E knockout mice exhibit increased lipoprotein oxidation and atherosclerosis. J Biol Chem 2000;275:17527-35
  • Quarck R, De Geest B, Stengel D, Adenovirus-mediated gene transfer of human platelet-activating factor-acetylhydrolase prevents injury-induced neointima formation and reduces spontaneous atherosclerosis in apolipoprotein E-deficient mice. Circulation 2001;103:2495-500
  • Hase M, Tanaka M, Yokota M, Yamada Y. Reduction in the extent of atherosclerosis in apolipoprotein E-deficient mice induced by electroporation-mediated transfer of the human plasma platelet-activating factor acetylhydrolase gene into skeletal muscle. Prostaglandins Other Lipid Mediat 2002;70:107-18
  • De Geest B, Stengel D, Landeloos M, Effect of overexpression of human apo A-I in C57BL/6 and C57BL/6 apo E-deficient mice on 2 lipoprotein-associated enzymes, platelet-activating factor acetylhydrolase and paraoxonase. Comparison of adenovirus-mediated human apo A-I gene transfer and human apo A-I transgenesis. Arterioscler Thromb Vasc Biol 2000;20:E68-75
  • Rosenson RS, Hislop C, McConnell D, Effects of 1-h-indole-3-glyoxamide (A-002) on concentration of secretory phospholipase A2 (PLASMA study): a phase II double-blind, randomised, placebo-controlled trial. Lancet 2009;373:649-58
  • Beck S, Lambeau G, Scholz-Pedretti K, Potentiation of tumor necrosis factor alpha-induced secreted phospholipase A2-IIA expression in mesangial cells by an autocrine loop involving sPLA2 and peroxisome proliferator-activated receptor alpha activation. J Biol Chem 2003;278:29799-812
  • Rosenson RS, Elliott M, Stasiv Y, Hislop C. Randomized trial of an inhibitor of secretory phospholipase A2 on atherogenic lipoprotein subclasses in statin-treated patients with coronary heart disease. Eur Heart J 2010; In press
  • Rosenson RS, Hislop C, Elliott M, Effects of varespladib methyl on biomarkers and major cardiovascular events in acute coronary syndrome patients. J Am Coll Cardiol 2010; In press
  • Dzavik V, Cantor WJ, Overgaard CB, The SPLA2 inhibition to decrease enzyme release after percutaneous coronary intervention (SPIDER-PCI) trial. J Am Coll Cardiol 2010;55:A207. E1952
  • Tardif JC, McMurray JJ, Klug E, Effects of succinobucol (AGI-1067) after an acute coronary syndrome: a randomised, double-blind, placebo-controlled trial. Lancet 2008;371:1761-8
  • Serruys PW, Garcia-Garcia HM, Buszman P, Effects of the direct lipoprotein-associated phospholipase A(2) inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 2008;118:1172-82

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