Ezetimibe: A selective inhibitor of cholesterol absorption

European Heart Journal, Supplement

Volumn 3, Issue SUPPL.5, 2001, Pages

  Catapano, A L ^a  

^a UNIVERSITY OF MILAN   (Italy)

Author keywords

Atherosclerosis; Cholesterol absorption inhibitor; Ezetimibe; Hypercholesterolaemia; Pre clinical studies; Statins

Indexed keywords

EID: 0002138183     PISSN: 1520765X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1520-765X(01)90106-3     Document Type: Article

References (19)

1. 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: 157-63.
2. 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: 1748-54.
3. van Heek M, Farley C, Compton D, Hoos L, Davis H. The novel cholesterol absorption inhibitor, ezetimibe, selectively inhibits the intestinal absorption of free cholesterol in the presence and absence of exocrine pancreatic function (Abstr). Atherosclerosis 2000; 151: 155.
4. Guerciolini R. Mode of action of orlistat. Int J Obes Relat Metab Disord 1997; 21 (Suppl 3): S12-23.
5. Toplak H, Marhardt K. Reduction of obesity and improvement in metabolic parameters by inhibition of intestinal lipases: current results with orlistat. Acta Med Austriaca 1998; 25: 142-5.
6. Heck AM, Yanovski JA, Calis KA. Orlistat, a new lipase inhibitor for the management of obesity. Pharmacotherapy 2000; 20: 270-9.
7. West RJ, Lloyd JK. The effect of cholestyramine on intestinal absorption. Gut 1975; 16: 93-8.
8. Matsui MS, Rozovski SJ. Drug-nutrient interaction. Clin Ther 1982; 4: 423-40.
9. Zbaida S, Alton K, Shannon D et al. In vitro metabolism of SCH 58235, 1-(4-fluorophenyl)-3R-[3-(4-fluorophenyl)-3S-hydroxypropyl]-4S-(4-hydroxyphenyl) -2-azetidinone, by liver and kidney slices (Abstr). 12th International Symposium on Microsomes and Drug Oxidations (ISMDO), Montpellier, France, July 20-24, 1998.
10. van Heek M, Compton DS, Davis HR. The cholesterol absorption inhibitor, ezetimibe, decreases diet-induced hypercholesterolemia in monkeys. Eur J Pharmacol 2001; 415: 79-84
11. Davis HR, Compton DS, Hoos L, Tetzloff G. The cholesterol inhibitor ezetimibe inhibits the development of atherosclerosis in apo E knockout ( - / - ) mice fed low fat and western diets (Abstr). Atherosclerosis 2000; 151: 133.
12. Davis HR, Watkins RW, Compton DS et al. The cholesterol absorption inhibitor ezetimibe (SCH 58235) and lovastatin synergistically lower plasma cholesterol and inhibit the development of atherosclerosis. Metabolism; in press.
13. Zilversmit DB. Atherogenic nature of triglycerides, postprandial lipemia, and triglyceride-rich remnant lipoproteins. Clin Chem 1995; 41: 153-8.
14. Cohn JS. Postprandial lipemia: emerging evidence for atherogenicity of remnant lipoproteins. Can J Cardiol 1998; 14 (Suppl B): 18B-27B.
15. Mamo JC, Proctor SD, Smith D. Retention of chylomicron remnants by arterial tissue; importance of an efficient clearance mechanism from plasma. Atherosclerosis 1998; 141 (Suppl 1): S63-9.
16. Havel RJ. Remnant lipoproteins as therapeutic targets. Curr Opin Lipidol 2000; 11: 615-20.
17. Davis HR, van Heek M, Watkins RW et al. The hypocholesterolemic activity of the potent cholesterol absorption inhibitor SCH58235 alone and in combination with HMG CoA reductase inhibitors (Abstr). Drugs Affecting Lipid Metabolism (DALM); Houston, TX; November 1995.
18. Knopp RH. Drug treatment of lipid disorders. N Engl J Med 1999; 341: 498-511.
19. Zhu Y, Statkevich P, Kosoglou T et al. Effect of ezetimibe (SCH 58235) on the activity of drug metabolizing enzymes in vivo (Abstr). Clin Pharmacol Ther 2000; 67: 152.