Pharmacokinetic interaction between ezetimibe and lovastatin in healthy volunteers*

References

• 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
   PubMed Web of Science ®Google Scholar
• 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
   PubMed Web of Science ®Google Scholar
• Altmann SW, Davis HR, Zhu LJ, et al. Niemann-Pick C1 Like 1 protein is critical for intestinal cholesterol absorption. Science 2004;303:1201–4
   PubMed Web of Science ®Google Scholar
• Sudhop T, Lütjohann D, Kodal A, et al. Inhibition of intestinal cholesterol absorption by ezetimibe in humans. Circulation 2002;106:1943–8
   PubMed Web of Science ®Google Scholar
• Patrick JE, Kosoglou T, Stauber KL, et al. Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects. Drug Metabol Dispos 2002;30:430–7
   PubMed Web of Science ®Google Scholar
• Ezzet F, Krishna G, Wexler D, Statkevich P, Kosoglou T, Batra V. A population pharmacokinetic model that describes multiple peaks due to enterohepatic recirculation of ezetimibe. Clin Ther 2001;23:871–85
   PubMed Web of Science ®Google Scholar
• Knopp RH, Gitter H, Truitt T, et al. Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia. Eur Heart J 2003;24:729–41
   PubMed Web of Science ®Google Scholar
• Bays HE, Moore PB, Drehobl MA, et al. Effectiveness and tolerability of ezetimibe in subjects with primary hypercholesterolemia: pooled analysis of two phase II studies. Clin Ther 2001;23:1209–30
   PubMed Web of Science ®Google Scholar
• 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;90:1092–7
   PubMed Web of Science ®Google Scholar
• Kerzner B, Corbelli J, Sharp S, et al. Efficacy and safety of ezetimibe coadministered with lovastatin in primary hypercholesterolemia. Am J Cardiol 2003;91:418–24
   PubMed Web of Science ®Google Scholar
• Davidson MH, McGarry T, Bettis R, et al. Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia. J Am Coll Cardiol 2002;40:2125–34
   PubMed Web of Science ®Google Scholar
• Ballantyne CM, Houri J, Notarbartolo A, et al. Effect of ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial. Circulation 2003;107:2409–15
   PubMed Web of Science ®Google Scholar
• Melani L, Mills R, Hassman D, et al. Efficacy and safety of ezetimibe coadministered with pravastatin in patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial. Eur Heart J 2003;24:717–28
   PubMed Web of Science ®Google Scholar
• Kosoglou T, Statkevich P, Fruchart J-C, et al. Pharmacodynamic and pharmacokinetic interaction between fenofibrate and ezetimibe. Curr Med Res Opin 2004;8:1197–207
   Google Scholar
• Downs JR, Clearfield M, Weis S, et al. Primary prevention of acute coronary events with lovastatin in men and women with average cholesterol levels: results of AFCAPS/TexCAPS. J Am Med Assoc 1998;279:1615–22
   PubMed Web of Science ®Google Scholar
• Bradford RH, Shear CL, Chremos AN, et al. Expanded Clinical Evaluation of Lovastatin (EXCEL) study results. I. Efficacy in modifying plasma lipoproteins and adverse event profile in 8245 patients with moderate hypercholesterolemia. Arch Intern Med 1991;151:43–9
   Google Scholar
• Bradford RH, Shear CL, Chremos AN, et al. Expanded Clinical Evaluation of Lovastatin (EXCEL) study results: two-year efficacy and safety follow-up. Am J Cardiol 1994;74:667–73
   PubMed Web of Science ®Google Scholar
• Kosoglou T, Statkevich P, Meyer I, et al. Effects of ezetimibe on the pharmacodynamics and pharmacokinetics of lovastatin. Curr Med Res Opin 2004;6:955–65
   Google Scholar
• Physicians’ Desk Reference. MEVACOR tablets (lovastatin) product information. Montvale (NJ): Medical Economics Company Inc.; 1999. p. 1834
   Google Scholar
• Kantola T, Kivistö KT, Neuvonen PJ. Grapefruit juice greatly increases serum concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1998;63:397–402
   PubMed Web of Science ®Google Scholar
• Data on file; Schering-Plough Research Institute, Kenilworth (NJ), USA
   Google Scholar
• Zhu Y, Statkevich P, Kosoglou T, et al. Effect of ezetimibe (SCH 58235) on the activity of drug metabolizing enzymes in vivo [abstract]. Clin Pharmacol Ther 2000;67:152
   Web of Science ®Google Scholar
• Kosoglou T, Seiberling M, Statkevich P, et al. Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and atorvastatin [abstract]. J Am Coll Cardiol 2001;37(2 Suppl A):229A
   Google Scholar
• Kosoglou T, Meyer I, Veltri EP, et al. Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and simvastatin. Br J Clin Pharmacol 2002;54:309–19
   PubMed Web of Science ®Google Scholar
• Gibaldi M, Perrier D. Pharmacokinetics, 2nd ed. New York: Marcel Dekker Inc; 1982. p. 409–17
   Google Scholar
• Stein E. Results of phase I/II clinical trials with ezetimibe, a novel selective cholesterol absorption inhibitor. Eur Heart J Suppl 2001;3(Suppl E):E11–E16
   Google Scholar
• Rogers JD, Zhao J, Liu L, et al. Grapefruit juice has minimal effects on plasma concentrations of lovastatin-derived 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Clin Pharmacol Ther 1999;66:358–66
   PubMed Web of Science ®Google Scholar