Ezetimibe: A proven cholesterol absorption inhibitor drug

Indian Drugs

Volumn 46, Issue 2, 2009, Pages 91-103

  Kathiravan, M K ^a   Munde, M K ^a   Jain, D P ^a   Jain, K S ^a  

^a NONE

Author keywords

Cholesterol absorption inhibitors; Ezetimibe; Hyperlipidemia

Indexed keywords

ATORVASTATIN; CHOLESTEROL; EZETIMIBE; LOW DENSITY LIPOPROTEIN CHOLESTEROL; SIMVASTATIN;

ARTICLE; ATHEROSCLEROSIS; HEART INFARCTION; HUMAN; HYPERLIPIDEMIA; ISCHEMIC HEART DISEASE; MONOTHERAPY; RISK FACTOR;

EID: 77955784591     PISSN: 0019462X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (36)

1. Kawecka-Jaszcz K., Jankowski P and Pajak A., Determinants of appropriate lipid management in patients with ischaemic heart disease. Cracovian Program for Secondary Prevention of Ischaemic Heart Disease, Int. J. Cardiol., 2003, 91, 15-23. (Pubitemid 37101095)
2. Van Heek M and Davis H., Pharmacology of ezetimibe, European Heart Journal Supplements., 2002, 4, J5-J8.
3. Bays H., Ezetimibe, Exepert Opin Investig Drugs., 2002, 11, 1587-1604.
4. Altmann S. W., Davis H. R., Zhu L. J., Yao X. R., Hoos L. M., Tetzloff J., Iyer S. P. N., Maguire M., Golovko A., Zene M., Wang, L. Q., Murgolo N and Graziano M. P., Niemann-Pick C1 Like 1 protein is critical for intestinal cholesterol absorption, Science., 2004, 303, 1201-1204.
5. Yamagishi, S.; Nakamura, K.; Matsui, T. ; Sato, T. ; Takeuchi, M. Med Hypotheses, 2006, 66, 84.
6. Sudhop T., Lutjohann D and Kodal A., Inhibition of Intestinal Cholesterol Absorption by Ezetimibe in Humans, Circulation., 2002, 106, 1943-1948. (Pubitemid 35176299)
7. Kosoglou T., Statkevich P., Johnson-Leconas A. O., Paolini J. F., Bergman A. J and Atlon K. B., Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions, Clin. Pharmacokinet., 2005, 44, 467-494.
8. Easson L. H and Stedman E., Studies on the relationship between chemical constitution and physiological action, Biochem J., 1933, 27 (4), 1257-1266.
9. Scheinin M., Kallio A., Koulu M., Viikari J and Scheinin H., Sedative and cardiovascular effects of medetomidine, a novel selective alpha 2-adrenoceptor agonist, in healthy volunteers, Br. J. Clin. Pharmacol., 1987, 24(4), 443-451.
10. Kallio A., Scheinin M., Koulu M., Ponkilainen R and Schenin M., Effects of dexmedetomidine, a selective alpha 2-adrenoceptor agonist, on hemodynamic control mechanisms, Clin. Pharmacol. Ther., 1989, 46, 33-42.
11. Burrnett D.A., Caplen M. A., Davis H. R. Jr., Burrier R. E. and Clader J. W., 2-Azetidinones as Inhibitors of Cholesterol Absorption, J. Med. Chem., 1994, 37, 1733-1736.
12. Duga S., Clader J. W., Chan T. M and Jr. Davis H., Substituted 2-Azaspiro[5,3]nonan-1-ones as Potent Cholesterol Absorption Inhibitors: Defining a Binding Conformation for SCH 48461, J. Med. Chem., 1995, 38, 4875-4877.
13. Dugar S., Kirkup M. P., Clader J. W., Lin S. I., Rizvi R., Snow M. E., Davis H. R Jr and McCombie S. W., Gamma-lactams and Related Compounds as Cholesterol Absorption Inhibitors: Homologs of The Beta-Lactum Cholesterol Absorption Inhibitor SCH 484611, Bioorg. Med. Chem. Lett., 1995, 5, 2947-2952.
14. Clader J. H., Burnett D. A., Caplen M. A., Domalski M. S., Dugar S., Vaccaro W., Sher R., Browne M. E., Zhao H., Burrier R. E., Salisbury B and Davis H. R. Jr., 2-Azetidinone Cholesterol Absorption Inhibitors: Structure-Activity Relationships on the Heterocyclic Nucleous, J. Med. Chem., 1996, 39, 3684-3693.
15. Rosenblum S. B., Huynh T., Afonso A., Davis H. R. Jr., Yumibe N., Clader J. W and Burnett D. A., Discovery of 1-(4-Flurophenyl)-(3R)-[3-(4-flurophenyl)- (3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active Inhibitor of Cholesterol Absorption, J. Med. Chem., 1998, 41, 973-980.
16. Clader, J. W. J. Med. Chem., 2004, 47, 1.
17. Davis, H. R.; Zhu, L.; Hoss, L. M.; Tetzloff, G.; Maguire, M.;Liu, J.; Yao, X.; Iyer, S. P. N.; Lam, M. H.; Lund, E. G.; Detman, P. A.; Graziano, M. P.; Altmann, S.W. Niemann, J. Biol. Chem., 2004, 297, 33586.
18. Kvaerno L., Werder M., Hauser H and Erick M. C., Synthesis and in Vitro Evaluation of Inhibitors of Intestinal Cholesterol Absorption, J. Med. Chem., 2005, 48, 6035-6053.
19. The Merck Index, Marydele J. O'Neil, Ann Smith, Patricia E Heckelman, 13th edition, Merck & Co., INC, White house station, NJ, 2001, 3949.
20. Zetia, TM (ezetimibe) package insert. Kenilworth, NJ: Merck/Schering plough, October 2002.
21. Altman S. W. ,Davis H. R. Jr., Yao. X., Laverty M., Compton D. S., Zhu L. J., Crona J. H., Tetzloff G., Priestley T., Burnett D. A., Strader C. D and Graziano M. P., The identification of intestinal scavenger receptor class B, type I (SR-BI) by expression cloning and its role in cholesterol absorption, Biochem. Biophy. Acta, 2002, 1580, 77-93.
22. Repa, J. J and Dietschy J. M., Inhibition of cholesterol absorption by SCH 58053 in the mouse is not mediated via changes in the expression of mRNA for ABCA1, ABCG5, or ABCG8 in the enterocyte, J. Lipid Res., 2002, 43, 1864-1874.
23. Van Heek M., Farley C., Compton D. S., Hoos L., Davis H. R., Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function, Br. J. Pharmacol., 2001, 134, 409-417. (Pubitemid 32989139)
24. Davis H. R. Jr., Pula K. K., Alton K. B., Burrier R. E and Watkins R. W., 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.
25. Van Heek M., Farley C., Compton D. S., 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.
26. Patrick J. E., Kosoglou T., Stauber K. L., et al., Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects, Drug Metab. Dispos., 2002, 30, 430-437. (Pubitemid 34263828)
27. Keung A., Kosoglou T and Statkevich P., Ezetimibe does not affect the pharmacokinetics of oral contraceptives, Clin. Pharmacol. Ther., 2001, 69, 55.
28. Bauer K., Kosoglou T and Statkevich P., Ezetimibe does not affect the pharmacokinetics or pharmacodynamics of warfarin, Clin. Pharmacol. Ther., 2001, 69, 5.
29. Kosoglou T., Statkevich P., Bauer K., et al. Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of digoxin. AAPS PharmSci 2001 Annual Meeting Supplement2001:3(3). http://www.aapspharmaceutica.com/search/abstract- view.asp?id=290.
30. Reyderman L, Kosoglou T, Maxwell S. Lack of pharmacokinetic interaction between ezetimibe and fenofibrate. AAPS PharmSci 2001 Annual Meeting Supplement 2001:3(3). http://www.aapspharmaceutica.com/search/abstract-view.asp?id=366.
31. Reyderman L., Kosoglou T and Statkevich P., Assessment of a multipledose drug interaction between ezetimibe and gemfibrozil. Presented at the XIVth International Symposium on Drugs Affecting Lipid Metabolism, New York, NY, 10-13 September 2001.
32. Reyderman L., Kosoglou T and Statkevich P., No pharmacokinetic drug interaction between ezetimibe and lovastatin, Clin. Pharmacol. Ther., 2001, 69, 67.
33. Reyderman L, Statkevich P, Kosoglou T. No pharmacokinetic interaction between ezetimibe and either cerivastatin or fluvastatin. AAPS PharmSci 2001 Annual Meeting Supplement 2001:3(3). Available from http://www. aapspharmaceutica.com/search/abstract-view.asp?id=371.
34. Statkevich P., Reyderman L and Kosoglou T., Ezetimibe does not affect the pharmacokinetics and pharmacodynamics of glipizide, Clin. Pharmacol. Ther., 2001, 69, 68.
35. Zhu Y., Statkevich P and Kosoglou T., Lack of a pharmacokinetic interaction between ezetimibe and atorvastatin, Clin. Pharmacol. Ther., 2001, 69, 68.
36. Kosoglou T., Meyer I., Veltri E., et al. Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor, ezetimibe, and simvastatin, Br. J. Clin. Pharmacol., 2002, 54, 309-319.