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The British Journal of Diabetes & Vascular Disease
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Reviews

Review: Ezetimibe — clinical and pharmacological profile

Alan Rees

Cardiff and Vale NHS Trust, University Hospital of Wales, Heath Park, Cardiff, CF14 4XW, UK, alan.rees{at}cardiffandvale.wales.nhs.uk

The launch of ezetimibe, a novel cholesterol absorption inhibitor in 2003 may well herald the dawn of combination therapy in the management of dyslipidaemia. The recent identification of NPC 1L1 as the probable specific sterol permease involved in intestinal cholesterol absorption is an important breakthrough in the understanding of the mechanisms of cholesterol absorption. Combination of statin therapy with blockade of exogenous cholesterol absorption (the so called dual inhibition of cholesterol metabolism) is discussed together with the potential for tailoring therapy to the physiological profile of patients' cholesterol metabolism.

Key Words: cholesterol absorption blockers • ezetimibe • cholesterol transporter system • dual inhibition of cholesterol metabolism.

References

  • Scandinavian Simvastatin Survival Study Group. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Survival Study. Lancet 1994;344:1383-9.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Sacks FM, Pfieffer MA, Moye LA et al., for the Cholesterol and Recurrent Events Trial Investigators. The effect of Pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. N Engl J Med 1996;335:1001-09.[Abstract/Free Full Text]
  • The Long-Term Intervention with Pravastatin in Ischaemic Disease (LIPID) Study Group. Prevention of cardiovascular events and death with pravastatin in patients with coronary heart disease and a broad range of initial cholesterol levels. N Engl J Med 1998;339:1349-57.[Abstract/Free Full Text]
  • Heart Protection Study Collaborative Group MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20536 high-risk individuals: a randomised placebo-controlled trial. Lancet 2002;360:7-22.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Athyros VG, Papageorgiou AA, Mercouria BR et al. Treatment with atorvastatin to the `National Cholesterol Educations Program Goal' versus `usual' care in secondary coronary heart disease prevention: the GREek Atorvastatin and Coronary heart-disease Evaluation (GREACE) Study. Curr Med Res Opin 2002;18:220-8.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Shepherd J., Cobbe SM, Ford I. et al., for the West of Scotland Coronary Prevention Study Group Prevention of coronary heart disease with Pravastatin in men with hypercholesterolaemia. N Engl J Med 1995;333: 1301-07.[Abstract/Free Full Text]
  • Downs GR, Clearfield M., Weiss S. et al. Primary prevention of acute coronary events with lovastatin in men and women with average cholesterol levels results in the AFCAPS/TEXCAPS (Air Force/Texas Coronary Atherosclerosis Prevention Study). JAMA 1998;279:1615-22.[Abstract/Free Full Text]
  • Herbert PR, Gaziano JM, Chan KS, Hennekens CH Cholesterol lowering with sta W tin drugs, risk of stroke, and total mortality: an overview of randomised trials. JAMA 1997;278:313-21.[Abstract/Free Full Text]
  • Gordon DJ Cholesterol lowering reduces mortality. In: Grundy SM ed. Cholesterol lowering therapy: evaluation of clinical trial evidence. New York: Marcel Dekker, 2000:299-311.
  • Nissen SE, Tuzcu EM, Schoenhagen P. et al. for the REVERSAL Investigators. Effect of intensive compared with moderate lipid-lowering therapy on progression of coronary atherosclerosis: a randomised conrolled trial. JAMA 2004;291:1071-80.[Abstract/Free Full Text]
  • Cannon CP, Braunwald E., McCabe CH et al. Comparison of intensive and moderate lipid lowering with statins following acute coronary syndrome. N Eng J Med 2004;350:1495-504.[Abstract/Free Full Text]
  • Pasternak RC, Smith SC Jr, Bairey-Merz CN et al. ACC/AHA/NHLBI clinical advisory on the use and safety of statins. J Am Coll Cardiol 2002;40: 567-72.[Free Full Text]
  • Knopp RH Drug treatment of lipid disorders. N Engl J Med 1999;341: 498-511.[Free Full Text]
  • Schectman G., Hiatt J. Dose-response characteristics of cholesterol-lowering drug therapies: implication for treatment. Ann Intern Med 1996; 125:990-1000.[Abstract/Free Full Text]
  • Leiterdorf E. Cholesterol absorption inhibition: filling an unmet need in lipid-lowering management. Eur Heart J 2001;3(suppl E):E17-E23.[CrossRef]
  • Schoenheimer R. TITLE. Z Physiol Chem 1929;180:1.
  • Altmann SW, Davis HR Jr, Zhu LJ et al. Niemann-Pick C1 Like 1 protein is critical for intestinal cholesterol absorption. Science 2004;303:1201-04.[Abstract/Free Full Text]
  • Schulthess G., Compassi S., Boffelli D. et al. A comparative study of sterol absorption in different small-intestinal brush border membrane models. J Lipid Res 1996;37:2405-19.[Abstract]
  • Hauser H., Dyer JH, Nancy A. et al. Identification of a receptor mediating absorption of dietary cholesterol in the intestine. Biochemistry 1998; 37:17842-50.
  • Schulthess G., Compassi S., Werder M. et al. Intestinal sterol absorption mediated by scavenger receptors is competitively inhibited by amphipathic peptides and proteins. Biochemistry 2000;39:12623-31.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Catapano AL Ezetimibe: A selective inhibitor of cholesterol absorption. Eur Heart J 2001;3(suppl E):E6-E10.[CrossRef]
  • Bays H. Ezetimibe: Drug Evaluation. Expert Opin Investig Drugs 2002; 11:1587-604.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Salen G., Von-Bergmann K., Lutjohann D. et al. Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolaemia. Circulation 2004;109:966-71.[Abstract/Free Full Text]
  • Bays HE, Moore PB, Drehobl MA et al. Effectiveness and tolerability of Ezetimibe in patients with primary hypercholesterolaemia: pooled analysis of two phase II studies. Clin Ther 2001;23:1209-30.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Van Heek M., Farley C., Compton DS et al. The potent cholesterol absorption inhibitor, Ezetimibe, is glucuronidated in the intestine, localises to the intestine, and circulates enterohepatically. Atherosclerosis 2000;151: 5.
  • Dujovne CA, Ettinger MP, McNeer JF et al. Effectiveness and safety of a potent new selective cholesterol absorption inhibitor, Ezetimibe, in patients with primary hypercholesterolaemia. Am J Cardiol 2002;90: 1092-7.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Knopp RH, Gitter H., Truitt T. et al., for the Ezetimibe Study Group. Effects of Ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolaemia. Eur Heart J 2003;24:729-41.[Abstract/Free Full Text]
  • Knopp RH, Dujovne CA, Le Beaut A. et al. For the Ezetimibe Study Group. Evaluation of the Efficacy, safety and tolerability of Ezetimibe in primary hypercholesterolaemia: a pooled analysis from two controlled phase III clinical studies. Int J Clin Pract 2003;57:363-8.[Web of Science][Medline] [Order article via Infotrieve]
  • Davidson MH, McGarry T., Bettis R. et al. Ezetimibe co-administered with simvastatin in patients with primary hypercholesterolaemia. J Am Coll Cardiol 2002;40:2125-34.[Abstract/Free Full Text]
  • Kerzner B., Corbelli J., Sharp S. et al. Efficacy and safety of Ezetimibe co-administered with Lovastatin in patients with primary hypercholesterolaemia. Am J Cardiol 2003;91:418-24.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Melani L., Mills R., Hassman D. et al. Efficacy and safety of Ezetimibe co-administered with Pravastatin in patients with primary hypercholesterolaemia: A prospective randomised double blind trial. Eur Heart Journal 2003;24:717-28.[Abstract/Free Full Text]
  • Ballantyne C., Houri J., Notarbartolo A. et al. Ezetimibe co-administered with atrovastatin in 628 patients with primary hypercholesterolaemia. Circulation 2003;107:2409-15.[Abstract/Free Full Text]
  • Sudhop T., Von Bergmann K. Cholesterol absorption inhibitors for the treatment of hypercholesterolaemia. Drugs 2002;62:2333-47.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Gagne C., Bays HE, Weiss SR et al. For the Ezetimibe Study Group. Efficacy and safety of Ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolaemia. Am J Cardiol 2002;90:1084-91.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]
  • Gagne C., Gaudet D., Bruckert E. Efficacy and safety of ezetimibe co-administered with atorvastatin or simvastatin in patients with or simvastatin in patients with homozygous familial hypercholesterolaemia. Circulation 2002;105:2469.[Abstract/Free Full Text]
  • Thomson GR, O'Neill F., Seed M. Why some patients respond poorly to statins and how this might be remedied. Eur Heart J 2002;23:200-06.[Free Full Text]
  • Miettinen TA, Strandberg TE, Gylling H. For the Finnish Investigators of the Scandinavian Simvastatin Study Group. Non-cholesterol sterols and cholesterol-lowering by long-term simvastatin treatment in coronary patients: Relation to basal serum cholestanol. Arterioscler Thromb Vasc Biol 2000;20:1340-6.[Abstract/Free Full Text]
  • Ziajka PE, Reis M., Kreul S., King H. Initial low-density lipoprotein response to statin therapy predicts subsequent low-density lipoprotein response to the addition of Ezetimibe. Am J Cardiol 2004;93:779-80.[CrossRef][Web of Science][Medline] [Order article via Infotrieve]

The British Journal of Diabetes & Vascular Disease, Vol. 4, No. 3, 163-171 (2004)
DOI: 10.1177/14746514040040030501
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This Article
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