References
- World Health Organization (WHO). The top 10 causes of death. Available from: www.who.int/mediacentre/factsheets/fs310/en/ [Last accessed on 28 August 2014]
- Segers D, Garcia-Garcia HM, Cheng C, et al. A primer on the immune system in the pathogenesis and treatment of atherosclerosis. EuroIntervention 2008;4:378-90
- Ross R. Atherosclerosis–an inflammatory disease. N Engl J Med 1999;340:115-26
- Hansson GK, Libby P. The immune response in atherosclerosis: a double-edged sword. Nat Rev Immunol 2006;6:508-19
- Virmani R, Kolodgie FD, Burke AP, et al. Lessons from sudden coronary death: a comprehensive morphological classification scheme for atherosclerotic lesions. Arterioscler Thromb Vasc Biol 2000;20:1262-75
- 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
- MacPhee CH, Moores KE, Boyd HF, et al. 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(Pt 2):479-87
- Garcia-Garcia HM, Jang IK, Serruys PW, et al. Imaging plaques to predict and better manage patients with acute coronary events. Circ Res 2014;114:1904-17
- Narula J, Nakano M, Virmani R, et al. Histopathologic characteristics of atherosclerotic coronary disease and implications of the findings for the invasive and noninvasive detection of vulnerable plaques. J Am Coll Cardiol 2013;61:1041-51
- Schaloske RH, Dennis EA. The phospholipase A2 superfamily and its group numbering system. Biochim Biophys Acta 2006;1761:1246-59
- Farr RS, Cox CP, Wardlow ML, Jorgensen R. Preliminary studies of an acid-labile factor (ALF) in human sera that inactivates platelet-activating factor (PAF). Clin Immunol Immunopathol 1980;15:318-30
- 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
- O’Donoghue M, Morrow DA, Sabatine MS, et al. Lipoprotein-associated phospholipase A2 and its association with cardiovascular outcomes in patients with acute coronary syndromes in the PROVE IT-TIMI 22 (PRavastatin Or atorVastatin evaluation and infection therapy-thrombolysis in myocardial infarction) trial. Circulation 2006;113:1745-52
- Oei HH, van der Meer IM, Hofman A, et al. Lipoprotein-associated phospholipase A2 activity is associated with risk of coronary heart disease and ischemic stroke: the Rotterdam Study. Circulation 2005;111:570-5
- Kolodgie FD, Burke AP, Skorija KS, et al. Lipoprotein-associated phospholipase A2 protein expression in the natural progression of human coronary atherosclerosis. Arterioscler Thromb Vasc Biol 2006;26:2523-9
- Wilensky RL, Shi Y, Mohler ER3rd, et al. Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development. Nat Med 2008;14:1059-66
- Shi Y, Zhang P, Zhang L, et al. Role of lipoprotein-associated phospholipase A2 in leukocyte activation and inflammatory responses. Atherosclerosis 2007;191:54-62
- Packard CJ, O’Reilly DS, Caslake MJ, et al. Lipoprotein-associated phospholipase A2 as an independent predictor of coronary heart disease. West of Scotland Coronary Prevention Study Group. N Engl J Med 2000;343:1148-55
- Lp PLASC, Thompson A, Gao P, et al. Lipoprotein-associated phospholipase A(2) and risk of coronary disease, stroke, and mortality: collaborative analysis of 32 prospective studies. Lancet 2010;375:1536-44
- Stafforini DM, Satoh K, Atkinson DL, et al. Platelet-activating factor acetylhydrolase deficiency. A missense mutation near the active site of an anti-inflammatory phospholipase. J Clin Invest 1996;97:2784-91
- Jang Y, Waterworth D, Lee JE, et al. Carriage of the V279F null allele within the gene encoding Lp-PLA(2) is protective from coronary artery disease in South Korean males. PLoS One 2011;6:e18208
- Blackie JA, Bloomer JC, Brown MJ, et al. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett 2003;13:1067-70
- Mohler ER3rd, Ballantyne CM, Davidson MH, et al. 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
- SB-480848 in subjects with coronary heart disease. Available from: http://clinicaltrials.gov/show/NCT00269048
- Serruys PW, Garcia-Garcia HM, Buszman P, et al. Effects of the direct lipoprotein-associated phospholipase A(2) inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 2008;118:1172-82
- Integrated biomarker and imaging study – 2. Available from: http://clinicaltrials.gov/show/NCT00268996
- The stabilization of atherosclerotic plaque by initiation of Darapladib therapy trial (STABILITY). Available from: http://clinicaltrials.gov/show/NCT00799903
- Investigators S, White HD, Held C, et al. Darapladib for preventing ischemic events in stable coronary heart disease. N Engl J Med 2014;370:1702-11
- White HD, Simes J, Stewart RA, et al. Changes in lipoprotein-Associated phospholipase A2 activity predict coronary events and partly account for the treatment effect of pravastatin: results from the Long-Term Intervention with Pravastatin in Ischemic Disease study. J Am Heart Assoc 2013;2:e000360
- The stabilization of plaques using Darapladib-Thrombolysis in myocardial infarction 52 trial (SOLID-TIMI 52). Available from: http://clinicaltrials.gov/show/NCT01000727
- O’Donoghue ML, Braunwald E, White HD, et al. Effect of darapladib on major coronary events after an acute coronary syndrome: the SOLID-TIMI 52 randomized clinical trial. Jama 2014;312:1006-15
- Rajamannan NM, Evans FJ, Aikawa E, et al. Calcific aortic valve disease: not simply a degenerative process: a review and agenda for research from the National Heart and Lung and Blood Institute Aortic Stenosis Working Group. Executive summary: Calcific aortic valve disease-2011 update. Circulation 2011;124:1783-91
- Stewart BF, Siscovick D, Lind BK, et al. Clinical factors associated with calcific aortic valve disease. Cardiovascular Health Study. J Am Coll Cardiol 1997;29:630-4
- Mahmut A, Boulanger MC, El Husseini D, et al. Elevated expression of lipoprotein-associated phospholipase A2 in calcific aortic valve disease: implications for valve mineralization. J Am Coll Cardiol 2014;63:460-9
- Wang WY, Zhang J, Wu WY, et al. Inhibition of lipoprotein-associated phospholipase A2 ameliorates inflammation and decreases atherosclerotic plaque formation in ApoE-deficient mice. PLoS One 2011;6:e23425
- Hu MM, Zhang J, Wang WY, et al. The inhibition of lipoprotein-associated phospholipase A2 exerts beneficial effects against atherosclerosis in LDLR-deficient mice. Acta Pharmacol Sin 2011;32:1253-8
- Zhang H, Zhang JY, Sun TW, et al. Amelioration of atherosclerosis in apolipoprotein E-deficient mice by inhibition of lipoprotein-associated phospholipase A2. Clin Invest Med 2013;36:E32-41
- Daida H, Iwase T, Yagi S, et al. Effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity in Japanese dyslipidemic patients, with exploratory analysis of a PLA2G7 gene polymorphism of Val279Phe. Circ J 2013;77:1518-25
- Johnson JL, Shi Y, Snipes R, et al. Effect of darapladib treatment on endarterectomy carotid plaque lipoprotein-associated phospholipase A2 activity: a randomized, controlled trial. PLoS One 2014;9:e89034
- Lp-PLA2, Progenitor cells and coronary atherosclerosis in humans AIM III. Available from: http://clinicaltrials.gov/show/NCT01067339
- A Phase 2 Clinical study to investigate effects of darapladib in subjects with diabetic macular edema. Available from: http://clinicaltrials.gov/show/NCT01506895
- To Estimate the potential effects of repeat doses of darapladib on the pharmacokinetics (PK) of rosuvastatin as well as evaluating safety and tolerability in healthy volunteers. Available from: http://clinicaltrials.gov/show/NCT01751074
- A healthy volunteer pharmacokinetic study of single and repeat doses of SB-480848. Available from: http://clinicaltrials.gov/show/NCT00743860
- A Study investigating the concentrations of darapladib in blood and the safety of this compound in healthy Japanese men. Available from: http://clinicaltrials.gov/show/NCT00551317
- A study with darapladib to collect tolerability information. Available from: http://clinicaltrials.gov/show/NCT00704431
- Study to determine the effect of repeated administration of diltiazem on the pharmacokinetics of darapladib (Sb-480848). Available from: http://clinicaltrials.gov/show/NCT01852565
- Pharmacokinetic interaction of Darapladib and CYP 3A4 in healthy subjects. Available from: http://clinicaltrials.gov/show/NCT01873339
- A Study to assess the pharmacokinetics, safety and tolerability of repeat oral doses of darapladib (SB-480848) in subjects with severe renal impairment. Available from: http://clinicaltrials.gov/show/NCT01711723
- Study of the effects of SB 480848 (Darapladib) On the electrical conduction of the heart. Available from: http://clinicaltrials.gov/show/NCT00411073
- Study to evaluate darapladib in moderately hepatically impaired subjects. Available from: http://clinicaltrials.gov/show/NCT01154114
- Effect of darapladib on cantharidin-induced inflammatory blisters in subjects with Type 2 Diabetes mellitus (T2DM). Available from: http://clinicaltrials.gov/show/NCT02058641