Darapladib: An emerging therapy for atherosclerosis

Therapeutic Advances in Cardiovascular Disease

Volumn 4, Issue 4, 2010, Pages 241-248

  Corson, Marshall A ^a  

^a UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

Author keywords

Atherosclerosis; Cardiovascular agent; Darapladib; Phospholipases

Indexed keywords

ATORVASTATIN; CHOLESTEROL; DARAPLADIB; PHOSPHOLIPASE A2; PLACEBO; TRIACYLGLYCEROL;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANGINA PECTORIS; ATHEROSCLEROSIS; ATHEROSCLEROTIC PLAQUE; CHOLESTEROL BLOOD LEVEL; CORONARY ARTERY; DOSE RESPONSE; DRUG EFFICACY; DRUG FATALITY; DRUG MEGADOSE; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; ENZYME ACTIVITY; GASTROINTESTINAL SYMPTOM; HEART INFARCTION; HUMAN; IC 50; ISCHEMIC HEART DISEASE; LOW DRUG DOSE; MORTALITY; NONHUMAN; PRIORITY JOURNAL; REVIEW; SIDE EFFECT; STROKE; TASTE AVERSION; TRIACYLGLYCEROL BLOOD LEVEL;

1-ALKYL-2-ACETYLGLYCEROPHOSPHOCHOLINE ESTERASE; ANIMALS; ATHEROSCLEROSIS; BENZALDEHYDES; CARDIOVASCULAR DISEASES; ENZYME INHIBITORS; EVIDENCE-BASED MEDICINE; HUMANS; HYPOLIPIDEMIC AGENTS; LIPIDS; OXIMES; TREATMENT OUTCOME;

EID: 77955342203     PISSN: 17539447     EISSN: None     Source Type: Journal    
DOI: 10.1177/1753944710375820     Document Type: Article

References (26)

1. Study Group (1994) Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: The Scandinavian Simvastatin Survival Study (4s). Lancet 344: 1383-1389.
2. ACCORD Study Group, Ginsberg, H.N., Elam, M.B., Lovato, L.C., Crouse 3rd, J.R., Leiter, L.A., Linz, P. et al. (2010) Effects of combination lipid therapy in type 2 diabetes mellitus. N Engl J Med 362 (17): 1563-1574 [Epub 2010 March 14]. Erratum in: N Engl J Med. 2010 May 6; 362 (18): 1748.
3. Blackie, J.A., Bloomer, J.C., Brown, M.J., Cheng, H.Y., Hammond, B., Hickey, D.M. et al. (2003) The identification of clinical candidate Sb-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett 13: 1067-1070.
4. Brown, B.G., Zhao, X.Q., Chait, A., Fisher, L.D., Cheung, M.C., Morse, J.S. et al. (2001) Simvastatin and niacin, antioxidant vitamins, or the combination for the prevention of coronary disease. N Engl J Med 345: 1583-1592.
5. CDP Research Group (1975) Clofibrate and niacin in coronary heart disease. JAMA 231: 360-381.
6. Corson, M.A., Jones, P.H. and Davidson, M.H. ( 2008) Review of the evidence for the clinical utility of lipoprotein-associated phospholipase A 2 as a cardiovascular risk marker. Am J Cardiol 101: 41F-50F.
7. Crandall, M.A. and Corson, M.A. ( 2008) Use of biomarkers to develop treatment strategies for atherosclerosis. Curr Treat Options Cardiovasc Med 10: 304-315.
8. Hayward, R.A., Hofer, T.P. and Vijan, S. ( 2006) Narrative review: lack of evidence for recommended low-density lipoprotein treatment targets: a solvable problem. Ann Intern Med 145: 520-530.
9. HPS Collaborative Group (2002) MRC / BHF heart protection study of cholesterol lowering with simvastatin in 20,536 high-risk individuals: a randomised placebo-controlled trial. Lancet 360: 7-22.
10. Jang, I.K., Tearney, G.J., Macneill, B., Takano, M., Moselewski, F., Iftima, N. et al. (2005) In vivo characterization of coronary atherosclerotic plaque by use of optical coherence tomography. Circulation 111: 1551-1555.
11. Johnson, A., Zalewski, A., Janmohamed, S., Sawyer, J., Rolfe, T., Staszkiewicz, W. et al. (2004) Lipoprotein-associated phospholipase A 2 activity, an emerging CV risk marker, can be inhibited in atherosclerotic lesions and plasma by a novel pharmacologic intervention: the results of a multicenter clinical study. Circulation 110: 17-22.
12. Karasawa, K., Harada, A., Satoh, N., Inoue, K. and Setaka, M. ( 2003) Plasma platelet activating factoracetylhydrolase (PAF-AH). Prog Lipid Res 42: 93-114.
13. Keech, A., Simes, R.J., Barter, P., Best, J., Scott, R., Taskinen, M.R. et al. (2005) Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD Study): randomised controlled trial. Lancet 366: 1849-1861.
14. Kolodgie, F.D., Burke, A.P., Skorija, K.S., Ladich, E., Kutys, R., Makuria, A.T. et al. (2006) Lipoprotein-associated phospholipase A 2 protein expression in the natural progression of human coronary atherosclerosis. Arterioscler Thromb Vasc Biol 26: 2523-2529.
15. Larosa, J.C., Grundy, S.M., Waters, D.D., Shear, C., Barter, P., Fruchart, J.C. et al. (2005) Intensive lipid lowering with atorvastatin in patients with stable coronary disease. N Engl J Med 352: 1425-1435.
16. Lavi, S., Mcconnell, J.P., Rihal, C.S., Prasad, A., Mathew, V., Lerman, L.O. et al. (2007) Local production of lipoprotein-associated phospholipase A 2 and lysophosphatidylcholine in the coronary circulation: association with early coronary atherosclerosis and endothelial dysfunction in humans. Circulation 115: 2715-2721.
17. LIPID Study Group (1998) Prevention of cardiovascular events and death with pravastatin in patients with coronary heart disease and a broad range of initial cholesterol levels. The Long-Term Intervention with Pravastatin in Ischaemic Disease (LIPID) Study Group. N Engl J Med 339: 1349-1357.
18. Mohler III, E.R., Ballantyne, C.M., Davidson, M.H., Hanefeld, M., Ruilope, L.M., Johnson, J.L. et al. (2008) The effect of darapladib on plasma lipoprotein-associated phospholipase A 2 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 51: 1632-1641.
19. Riley, R.F. and Corson, M.A. (2009) Darapladib, a reversible lipoprotein-associated phospholipase A 2 Inhibitor, for the oral treatment of atherosclerosis and coronary artery disease. IDrugs 12: 648-655.
20. Sacks, F.M., Pfeffer, M.A., Moye, L.A., Rouleau, J.L., Rutherford, J.D., Cole, T.G. et al. (1996) The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. Cholesterol and Recurrent Events Trial Investigators. N Engl J Med 335: 1001-1009.
21. Schaloske, R.H. and Dennis, E.A. ( 2006) The phospholipase A 2 superfamily and its group numbering system. Biochim Biophys Acta 1761: 1246-1259.
22. Serruys, P.W., Garcia-Garcia, H.M., Buszman, P., Erne, P., Verheye, S., Aschermann, M. et al. (2008) Effects of the direct lipoprotein-associated phospholipase A (2) inhibitor darapladib on human coronary atherosclerotic plaque. Circulation 118: 1172-1182.
23. Tsimikas, S., Tsironis, L.D. and Tselepis, A.D. ( 2007) New insights into the role of lipoprotein(a)-associated lipoprotein-associated phospholipase A 2 in atherosclerosis and cardiovascular disease. Arterioscler Thromb Vasc Biol 27: 2094-2099.
24. Wilensky, R.L., Shi, Y., Mohler III, E.R., Hamamdzic, D., Burgert, M.E., Li, J. et al. (2008) Inhibition of lipoprotein-associated phospholipase A 2 reduces complex coronary atherosclerotic plaque development. Nat Med 14: 1059-1066.
25. Yang, E.H., Mcconnell, J.P., Lennon, R.J., Barsness, G.W., Pumper, G., Hartman, S.J. et al. (2006) Lipoprotein-associated phospholipase A 2 is an independent marker for coronary endothelial dysfunction in humans. Arterioscler Thromb Vasc Biol 26: 106-111.
26. Zalewski, A. and Macphee, C. ( 2005) Role of lipoprotein-associated phospholipase A 2 in atherosclerosis: biology, epidemiology, and possible therapeutic target. Arterioscler Thromb Vasc Biol 25: 923-931.