Ezetimibe

American Journal of Cardiovascular Drugs

Volumn 3, Issue 1, 2003, Pages 67-76

  Darkes, Malcolm J M ^a   Poole, Raewyn M ^a   Goa, Karen L ^a  

^a ADIS INTERNATIONAL INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,4 BIS(4 METHOXYPHENYL) 3 (3 PHENYLPROPYL) 2 AZETIDINONE; 2,2 DIMETHYL N (2,4,6 TRIMETHOXYPHENYL)DODECANAMIDE; ACYL COENZYME A; ANTACID AGENT; ATORVASTATIN; CAFFEINE; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; CIMETIDINE; CYCLOSPORIN; DAPSONE; DEXTROMETHORPHAN; ETHINYLESTRADIOL; EZETIMIBE; FENOFIBRATE; FLUINDOSTATIN; GEMFIBROZIL; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; HYPOCHOLESTEROLEMIC AGENT; LOW DENSITY LIPOPROTEIN CHOLESTEROL; MEVINOLIN; MIDAZOLAM; NORGESTREL; PD 12804; PRAVASTATIN; SCH 60663; SIMVASTATIN; TOLBUTAMIDE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN;

ANGINA PECTORIS; APPENDICITIS; ARTHRALGIA; ATHEROSCLEROSIS; BACKACHE; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL TRANSPORT; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG HALF LIFE; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENTIATION; DRUG TOLERABILITY; GASTROINTESTINAL SYMPTOM; HEADACHE; HUMAN; HYPERCHOLESTEROLEMIA; INCIDENCE; INTESTINE ABSORPTION; MAXIMUM PERMISSIBLE DOSE; MYALGIA; NONHUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; REVIEW; TRIACYLGLYCEROL BLOOD LEVEL; UPPER RESPIRATORY TRACT INFECTION; VIRUS INFECTION;

ANIMALS; ANTICHOLESTEREMIC AGENTS; AZETIDINES; CHOLESTEROL, LDL; CLINICAL TRIALS; HUMANS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; HYPERCHOLESTEROLEMIA;

EID: 0037280850     PISSN: 11753277     EISSN: None     Source Type: Journal    
DOI: 10.2165/00129784-200303010-00007     Document Type: Review

References (68)

1. Shepherd J, Cobbe SM, Ford I, et al. Prevention of coronary heart disease with pravastatin in men with hypercholesterolemia. N Eng J Med 1995; 333 (20): 1301-7
2. Assmann G, Schulte H. Relation of high-density lipoprotein cholesterol and triglycerides to incidence of atherosclerotic coronary artery disease (the PROCAM experience). Am J Cardiol 1992; 70: 733-7
3. Cullen P. Evidence that triglycerides are an independent coronary heart disease risk factor. Am J Cardiol 2000; 86: 943-9
4. Castelli WP, Garrison RJ, Wilson WF, et al. Incidence of coronary heart disease and lipoprotein cholesterol levels: the Framingham study. 1986; 256 (20): 2835-8
5. Després J-P, Lemieux I, Daganais G-R, et al. HDL-cholesterol as a marker of coronary heart disease risk: the Québec cardiovascular study. Atherosclerosis 2000; 153: 263-72
6. Assmann G, Schulte H, von Eckardstein A, et al. High-density lipoprotein cholesterol as a predictor of coronary heart disease risk. The PROCAM experience and pathophysiological implications for reverse cholesterol transport. Atherosclerosis 1996; 124 Suppl.: S11-20
7. Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults. Executive summary of the Third Report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III). JAMA 2001; 285 (19): 2486-97
8. American Diabetes Association. Management of dyslipidemia in adults with diabetes. Diabetes Care 2002; 25 Suppl. 1: S74-7
9. Wood D, de Backer G, Faergeman O, et al, Prevention of coronary heart disease in clinical practice: recommendations of the Second Joint Task Force of European and other Societies on Coronary Prevention. Eur Heart J 1998; 19 (Oct): 1434-503
10. Faergeman O. The revised joint guidelines. Atherosclerosis Suppl 2000; 1: 3-7
11. Ros E. Intestinal absorption of triglyceride and cholesterol. Dietary and pharmacological inhibition to reduce cardiovascular risk. Atherosclerosis 2000; 151: 357-79
12. Kramer W, Glombik H, Petry S, et al. Identification of binding proteins for cholesterol absorption inhibitors as components of the intestinal cholesterol transporter. FEBS Lett 2000 Dec 29; 487 (2): 293-7
13. Anonymous. Statin therapy - what now? Drug Ther Bull 2001; 39 (3): 17-21
14. Libby P. Atherosclerosis: the new view. Sci Am 2002; May: 29-37
15. Primatesta P, Poulter NR. Lipid concentrations and the use of lipid lowering drugs: evidence from a national cross sectional survey. BMJ 2000; 321: 1322-5
16. Leitersdorf E. Selective cholesterol absorption inhibition: a novel strategy in lipid- lowering management. Int J Clin Pract 2002 Mar; 56 (2): 116-9
17. Brown WV. Novel approaches to lipid lowering: what is on the horizon? Am J Cardiol 2001 Mar 8; 87 (5A): 23B-7B
18. Kastelein JJP, van Dam MJ. A new role for combination therapy in lipid management. Br J Cardiol 2001; 8 (11): 639-53
19. Gallup E, Dujovne C. New pharmacological agents under clinical investigation for treating disorders of lipoprotein regulation leading to atherosclerosis. Expert Opin Invest Drugs 2001; 10 (3): 561-7
20. Miettinen TA. Cholesterol absorption inhibition: a strategy for cholesterol-lowering therapy. Int J Clin Pract 2001; 55 (10): 710-6
21. van Heek M, Farley C, Compton DS, etal. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharmacol 2001; 134 (2): 409-17
22. Sudhop T, Von Bergmann K. Cholesterol absorption inhibitors for the treatment of hypercholesterolaemia. Drugs 2002; 62 (16): 2333-47
23. van Heek M, France CF, Compton DS, et al. In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH58235, in the rat and rhesus monkey through the identification of the active metabolites of SCH48461. J Pharmacol Exp Ther 1997 Oct; 283 (1): 157-63
24. van Heek M, Farley C, Compton DS, et al. Comparison of the activity and disposition of the novel cholesterol absorption inhibitor, SCH58235, and its glucuronide, SCH60663. Br J Pharmacol 2000 Apr; 129 (8): 1748-54
25. Davis HR, Compton DS, Hoos L, et al. Ezetimibe (SCH58235) localizes to the brush border of small intestinal enterocyte and inhibits entertocyte cholesterol uptake and absorption [abstract no. P3500]. Eur Heart J 2000 Aug; 21 (Abstr. Suppl.): 636
26. Sudhop T, Lutjohann D, Kodal A, et al. Inhibition of intestinal cholesterol absorption by ezetimibe in humans. Circulation 2002 Oct 8; 106 (15): 1943-8
27. Salisbury BG, Davis HR, Burrier RE, et al. Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461. Atherosclerosis 1995; 115: 45-63
28. Clader JW, Burnett DA, Caplan MA, et al. 2-Azetidinone cholesterol absorption inhibitors: structure-activity relationships on the heterocyclic nucleus. J Med Chem 1996; 39 (19): 3684-93
29. van Heek M, Compton DS, Davis HR. The cholesterol absorption inhibitor, ezetimibe, decreases diet-induced hypercholesterolemia in monkeys. Eur J Pharmacol 2001; 415 (1): 79-84
30. Davis HR, Watkins RW, Compton DS, et al. The cholesterol absorption inhibitor SCH58235 and lovastatin synergistically lower plasma cholesterol and inhibit the development of artherosclerosis [abstract no. 1044-56]. J Am Coll Cardiol 2000; 35 Suppl. A: 252A
31. van Heek M, Austin TM, Farley C, et al. Ezetimibe, a potent cholesterol absorption inhibitor, normalizes combined dyslipidemia in obese hyperinsulinemic hamsters. Diabetes 2001; 50 (6): 1330-5
32. Davis Jr HR, Pula KK, Alton KB, et al. The synergistic hypocholesterolemic activity of the potent cholesterol absorption inhibitor, ezetimibe, in combination with 3-hydroxy-3- methylglutaryl coenzyme A reductase inhibitors in dogs. Metabolism 2001; 50 (10): 1234-41
33. Kosoglou T, Guillaume M, Sun S, et al. Pharmacodynamic interaction between fenofibrate and the cholesterol absorption inhibitor ezetimibe [abstract no. W6.1]. Atherosclerosis 2001; 2 Suppl.: 38
34. Davis Jr HR, Compton DS, Hoos L, et al. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice. Arterioscler Thromb Vasc Biol 2001; 21 (12): 2032-8
35. Reyderman L, Kosoglou T, Maxwell S, et al. Dose-proportionality of ezetimibe [abstract]. Clin Pharmacol Ther 2002 Feb; 71: P97
36. Ezzet F, Wexler D, Statkevich P, et al. The plasma concentration and LDL-C relationship in patients receiving ezetimibe. J Clin Pharmacol 2004, Sep; 41 (9): 943-9
37. Courtney RD, Kosoglou T, Statkevich P, et al. Effect of food on the oral bioavailability of ezetimibe [abstract]. Clin Pharmacol Ther 2002 Feb; 71: P80
38. Dujovne C, Held J, Lipka L, et al. Does cholesterol and/or fat intake affect plasma lipid efficacy of ezetimibe? [abstract] J Am Coll Cardiol 2002 Mar; 39 Suppl. A: 227A
39. Patrick JE, Kosoglou T, Stauber KL, et al. Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects. Drug Metab Dispos 2002 Apr; 30 (4): 430-7
40. Ezzet F, Krishna G, Wexler DB, et al. A population pharmacokinetic model that describes multiple peaks due to enterohepatic recirculation of ezetimibe. Clin Ther 2001; 23 (6): 871-85
41. Kosoglou T, Kakkar T, Statkevich P, et al. Multiple-dose safety and pharmacokinetics of ezetimibe in adolescent children [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P52
42. Reyderman L, Kosoglou T, Statkevich P, et al. Pharmacokinetics of ezetimibe in subjects with normal renal function or severe chronic renal insufficiency [abstract]. Clin Pharmacol Ther 2002 Feb; 71: P27
43. Bays HE, Moore PB, Drehobl MA, et al. Effectiveness and tolerability of ezetimibe in patients with primary hypercholesterolemia: pooled analysis of two phase II studies. Clin Ther 2001 Aug; 23 (8): 1209-30
44. Statkevich P, Zhu Y, Kosoglou T, et al. SCH 58235 does not affect the pharmacokinetics of simvastatin [abstract]. Clin Pharmacol Ther 2000 Feb; 67: 146
45. Reyderman L, Kosoglou T, Statkevich P, et al. No pharmacokinetic drug interaction between ezetimibe and lovastatin [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P66
46. Kosoglou T, Meyer I, Musiol B, et al. Pharmacodynamic interaction between fluvastatin and ezetimibe has favorable clinical implications [abstract]. Athersoclerosis Suppl. 2001; 2 (2): 89
47. Zhu Y, Statkevich P, Kosoglou T, et al. Lack of a pharmacokinetic interaction between ezetimibe and atorvastatin [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P68
48. Zetiab™ (ezetimibe) tablets. Prescribing information. Merck/Schering-Plough Pharmaceuticals 2002 Oct
49. Bauer KS, Kosoglou T, Statkevich P, et al. Ezetimibe does not affect the pharmacokinetics or pharmacodynamics of warfarin [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P5
50. Statkevich P, Reyderman L, Kosoglou T, et al. Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of glipizide [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P67
51. Keung ACF, Kosoglou T, Statkevich P, et al. Ezetimibe does not affect the pharmacokinetics of oral contraceptives [abstract]. Clin Pharmacol Ther 2001 Feb; 69: P55
52. Courtney RD, Kosoglou T, Statkevich P, et al. Effect of antacid on the pharmacokinetics of ezetimibe [abstract]. Clin Pharmacol Ther 2002 Feb; 71: P80
53. Krishna G, Kosoglou T, Ezzet F, et al. Effect of cimetidine on the pharmacokinetics of ezetimibe [online]. Available from URL: http://www.aapspharmaceutica.corn/search/abstractviewasp?id=304 [Accessed 2002 Dec 4]
54. Zhu Y, Statkevich P, Kosoglou T, et al. Effect of SCH 58235 on the activity of drug metabolizing enzymes in vivo [abstract]. Clin Pharmacol Ther 2000 Feb; 67: 152
55. Gagné C, Bays HE, Weiss SR, et al. Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia. Am J Cardio 2002; 90 (15 Nov): 1084-91
56. Dujovne CA, Ettinger MP, McNeer JF, et al. Efficacy and safety of a potent new selective cholesterol absorption inhibitor, ezetimibe, in patients with primary hypercholesterolemia. Am J Cardiol 2002 Nov 15; 90: 1092-7
57. Gagné C, Gaudet D, Bruckert E. Efficacy and safety of ezetimibe coadministered with atorvastatin or simvastatin in patients with homozygous familial hypercholesterolemia. Ezetimibe Study Group. Circulation 2002; 105 (21): 2469-75
58. Davidson M, McGarry T, Bettis R, et al. Ezetimibe co-administered with simvastatin in patients with primary hypercholesterolemia. J Am Coll Cardiol 2002 Dec 18; 40 (12): 2125-34
59. Stein E. Results of phase I/II clinical trials with ezetimibie, a novel selective cholesterol absorption inhibitor. Eur Heart J Suppl 2001 Oct; 3 Suppl. E: E11-6
60. Knopp RH, Gitter H, Truitt T, et al. Ezetimibe reduces low-density lipoprotein cholesterol: results of a phase III, randomized, double-blind, placebo-controlled trial [abstract no. W6.2]. Atherosclerosis Suppl 2001 May; 2 (2):38
61. Mata P, Gumbiner B, Musliner T, et al. Addition of ezetimibe to ongoing statin therapy: incremental reduction in low-dentisty lipoprotein cholesterol is independent of statin type [abstract no. 213]. Eur Heart J 2002 Aug 2; 23 (Abstr. Suppl.): 19
62. Simons L, Musliner T, Quinto K, et al. Ezetimibe added to on-going statin therapy for treatment of primary hypercholesterolemia: efficacy and safety in patients with Type 2 diabetes mellitus [abstract no. 1209]. Diabetologia 2002; 45 Suppl. 2 (Aug): A389
63. Lipka L, Kerzner B, Corbelli J, et al. Results of ezetimibe co-administered with lovastatin in 548 patients with primary hypercholesterolemia [abstract]. J Am Coll Cardiol 2002 May 1; 39 Suppl. B: 430B
64. Melani L, Mills R, Hassman D, et al. Ezetimibe co-administered with pravastatin in 538 patients with primary hypercholesterolemia [abstract]. J Am Coll Cardiol 2002 May 1; 39 Suppl. B: 134-135 (plus poster presented at the XIV World Congress of Cardiology, May 2002, Sydney)
65. Ballantyne C, Houri J, Notarbartolo A, et al. Ezetimibe co-administered with atorvastatin in 628 patients with primary hypercholesterolemia [abstract]. J Am Coll Cardiol 2002 May 1; 39 Suppl. B: 135-136 (plus poster presented at the XIV World Congress of Cardiology, May 2002, Sydney)
66. Lipka L, Melani L, LeBeaut S, et al. Consistency of LDL-C lowering effect across subgroups of ezetimibe co-administered with statins [abstract no. 214]. Eur Heart J 2002 Aug; 23 Abstr. Suppl.: 19
67. Poole RM. Ezetimibe enhances efficacy of statins in hypercholesterolaemia. Inpharma 2002; 1341: 7-9
68. Salen G, von Bergmann K, Kwiterovich P, et al. Ezetimbe is an effective treatment for homozygous sitosterolemia [abstract no. 929]. American Heart Association 75th Scientific Sessions 2002 Nov 17-20, Orlando, Florida