Inhibition of intestinal cholesterol absorption by ezetimibe in humans

Circulation

Volumn 106, Issue 15, 2002, Pages 1943-1948

  Sudhop, Thomas ^a   Lutjohann, Dieter ^a   Kodal, Annette ^a   Tribble, Diane L ^b   Shah, Sukrut ^b   Perevozskaya, Inna ^b   Von Bergmann, Klaus ^a  

^a UNIVERSITY OF BONN   (Germany)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Cholesterol absorption; Cholesterol synthesis; Ezetimibe; Lathosterol; Plant sterols

Indexed keywords

BILE ACID; CAMPESTEROL; CHOLESTEROL; COPROSTEROL; DEUTERIUM; EZETIMIBE; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; LATHOSTEROL; LOW DENSITY LIPOPROTEIN CHOLESTEROL; PLACEBO; SITOSTANOL; SITOSTEROL; TRIACYLGLYCEROL;

ADULT; ARTICLE; BILE ACID SYNTHESIS; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL SYNTHESIS; CLINICAL ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOUBLE BLIND PROCEDURE; DRUG SAFETY; DRUG TOLERABILITY; FECES; GAS CHROMATOGRAPHY; HUMAN; HYPERCHOLESTEROLEMIA; INTESTINE ABSORPTION; MALE; MASS SPECTROMETRY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; STEROL EXCRETION;

ADULT; ANTICHOLESTEREMIC AGENTS; AZETIDINES; CHOLESTEROL; CROSS-OVER STUDIES; DOUBLE-BLIND METHOD; HUMANS; HYPERCHOLESTEROLEMIA; INTESTINAL ABSORPTION; LIPOPROTEINS; MALE; MIDDLE AGED; STEROLS;

EID: 0037044454     PISSN: 00097322     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1567-5688(02)80680-8     Document Type: Article

References (35)

1. 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;285:2486-2497. (See http://www.nhlbi.nih.gov/guidelines/cholesterol/for full report and references)
2. Clinical reality of coronary prevention guidelines: a comparison of EUROASPIRE I and II in nine countries. EUROASPIRE I and II Group. European Action on Secondary Prevention by Intervention to Reduce Events. Lancet. 2001;357:995-1001.
3. Igel M, Sudhop T, von Bergmann K. Metabolism and drug interactions of 3-hydroxy-3-metbylglutaryl coenzyme A-reductase inhibitors (statins). Eur J Clin Pharmacol. 2001;57:357-364.
4. Ros E. Intestinal absorption of triglyceride and cholesterol: dietary and pharmacological inhibition to reduce cardiovascular risk. Atherosclerosis. 2000;151:357-379.
5. van Heek M, Farley C, Compton DS, et al. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharmacol. 2001;134:409-417.
6. Davis HR, Compton DS, Hoos L, et al. Ezetimibe (SCH58235) localizes to the brush border of small intestinal enterocyte and inhibits enterocyte cholesterol uptake and absorption. Eur Heart J. 2000;21(suppl):636. Abstract.
7. 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;129:1748-1754.
8. Ezzet F, Wexler D, Statkevich P, et al. The plasma concentration and LDL-C relationship in patients receiving ezetimibe. J Clin Pharmacol. 2001;41:943-949.
9. 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. Atherosclerosis. 2001:2(suppl):38. Abstract.
10. Knopp RH, Gitter H, Truitt T, et al. Ezetimibe significantly lowers low-density cholesterol in subjects with primary hypercholesterolaemia. Eur Heart J. 2001;22:252. Abstract.
11. Lütjohann D, Meese CO, Crouse JR III, et al. Evaluation of deuterated cholesterol and deuterated sitostanol for measurement of cholesterol absorption in humans. J Lipid Res. 1993;34:1039-1046.
12. Czubayko F, Beumers B, Lammsfuss S, et al. A simplified micro-method for quantification of fecal excretion of neutral and acidic sterols for outpatient studies in humans. J Lipid Res. 1991;32:1861-1867.
13. Friedewald WT, Levy RI, Fredrickson DS. Estimation of the concentration of low-density lipoprotein cholesterol in plasma, without use of the preparative ultracentrifuge. Clin Chem. 1972;18:499-502.
14. Teunissen CE, Mulder M, de Vente J, et al. Concentrations of different sterols in the striatum and serum of 3- nitropropionic acid-treated Wistar and Lewis rats. Neurochem Res. 2001;26:1237-1244.
15. 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;283:157-163.
16. Samuel P. Treatment of hypercholesterolemia with neomycin: a time for reappraisal. N Engl J Med. 1979;301:595-597.
17. Gylling H, Miettinen TA. The effect of cholesterol absorption inhibition on low density lipoprotein cholesterol level. Atherosclerosis. 1995;117:305-308.
18. Hainer JW, Terry JG, Connell JM, et al. Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin Pharmacol Ther. 1994;56:65-74.
19. Kesäniemi YA, Grundy SM. Turnover of low density lipoproteins during inhibition of cholesterol absorption by neomycin. Arteriosclerosis. 1984;4:41-48.
20. Sedaghat A, Samuel P, Crouse JR, et al. Effects of neomycin on absorption, synthesis, and/or flux of cholesterol in man. J Clin Invest. 1975;55:12-21.
21. Lees RS, Lees AM. Effects of sitosterol therapy on plasma lipid and lipoprotein concentrations. In: Greten H, ed. Lipoprotein Metabolism. New York, NY: Springer-Verlag; 1976:117-124.
22. Grundy S, Mok H. Effects of low dose phytosterols on cholesterol absorption in man. In: Greten H, ed. Lipoprotein Metabolism. New York, NY: Springer-Verlag; 1976:112-118.
23. Heinemann T, Axtmann G, von Bergmann K. Comparison of intestinal absorption of cholesterol with different plant sterols in man. Eur J Clin Invest. 1993;23:827-831.
24. Boberg KM, Einarsson K, Björkhem I. Apparent lack of conversion of sitosterol into C24-bile acids in humans. J Lipid Res. 1990;31:1083-1088.
25. Björkhem I, Miettinen T, Reihner E, et al. Correlation between serum levels of some cholesterol precursors and activity of HMG-CoA reductase in human liver. J Lipid Res. 1987;28:1137-1143.
26. Kempen HJ, Glatz JF, Gevers Leuven JA, et al. Serum lathosterol concentration is an indicator of whole-body cholesterol synthesis in humans. J Lipid Res. 1988;29:1149-55.
27. Davis HR Jr, 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;50:1234-1241.
28. Kosoglou T, Meyer I, Musiol B, et al. Pharmacodynamic interaction between fluvastatin and ezetimibe has favorable clinical implications. Atherosclerosis. 2001;2(suppl):89. Abstract.
29. Kosoglou T, Seiberling M, Statkevich P, et al. Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and atorvastafin. J Am Coll Cardiol. 2001;37(suppl):229A. Abstract.
30. Kosoglou T, Meyer I, Cutler DL, et al. Pharmacodynamic interaction between the selective cholesterol absorption inhibitor ezetimibe and lovastatin. In: Program and Abstracts of the Third International Congress on Coronary Artery Disease: From Prevention to Intervention. Lyon, France; 2000:101. Abstract.
31. Kosoglou T, Meyer I, Musiol B, et al. Coadministration of simvastatin and ezetimibe leads to significant reduction in LDL-cholesterol. In: Program and Abstracts of the Third International Congress on Coronary Artery Disease: From Prevention to Intervention. Lyon. France; 2000:71. Abstract.
32. Kosoglou, T, Meyer I, Musiol B, et al. Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and simvastatin. Atherosclerosis. 2000;151:135. Abstract.
33. Ballantyne C, Houri J, Notarbartolo A, et al. Ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia. J Am Coll Cardiol. 2002;39(suppl.):227A. Abstract.
34. Davidson M, McGarry T, Bettis R, et al. Ezetimibe co-administered with simvastatin in 668 patients with primary hypercholesterolemia. J Am Coll Cardiol. 2002;39(suppl.):226A. Abstract.
35. Bays H, Weiss S, Gagne C, et al. Ezetimibe added to ongoing statin therapy for treatment of primary hypercholesterolemia. J Am Coll Cardiol. 2002;39(suppl.):245A. Abstract.