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Chemical Compound Review

ezetimib     (3R,4S)-1-(4-fluorophenyl)-3- [(3S)-3-(4...

Synonyms: Ezetimibe, Ezetrol, Ezedoc, Zetia, Zient, ...
 
 
 
 Thornberry,  Weinstock,  Detmers,  Mazzone,  Edwards,  Lipka,  Suresh,  Bettis,  Shevell,  Garcia-Calvo,  Mukhopadhyay,  Patrick,  Orsó,  Yuan,  Chowdhury, Stefan Oswald, Jörg König, Dieter Lütjohann, Thomas Giessmann, Heyo K. Kroemer, Christian Rimmbach, Dieter Rosskopf, Martin F. Fromm, Werner Siegmund,  Tang, Anna Bonjoch, Bonaventura Clotet,  Braun,  Pahan,  Veltri,  Lipetz,  Sun,  Farley,  Rhein,  Zbaida, Asunción Blanco,  Starc,  Kosoglou,  Simon,  Bull,  Iyer,  Davis,  Achanfuo-Yeboah,  Tomassini,  Melani,  Hughes,  Corsiero,  Ogawa,  LeBeaut,  Wendler,  Lisnock,  Pfenninger,  Moser,  Altmann,  O'neill,  Graziano,  Hassman,  LeBeaut,  During,  Dawson,  Sachs,  Altmann,  Hawes,  Crona,  Dean,  Johnson-Levonas,  Graziano, José Moltó,  Alton,  Palmisano,  Staprans,  Veltri,  Davies,  Paolini,  Lottspeich,  Hawes,  Devlin,  Chapman,  Schmitz,  Plump,  Ujjainwalla,  Hochleitner,  Qiu,  Pan, Denise Cinquegrana,  Ghosal,  Davis,  Salen,  Alton, Núria Pérez-Alvarez,  Goldberg,  Smith,  Lipka,  Kramer,  Cook,  Cook,  Sisk,  Frick,  Crona,  Jähne,  Guyton,  Austin,  Polis,  Mills, Celestino Rey-Joly,  Yao,  Davis,  Bayne,  Arreaza,  McGarry,  Deutsch,  Girbig,  Statkevich, Raquel López-Blázquez,  Karnoub,  Harrison,  Tetzloff,  Tershakovec,  Melani,  Alemao,  van Heek,  Bergman,  Iannucci, Eugenia Negredo,  Macintyre,  Burnett,  Davidson,  O'neill,  Makarewicz,  Rapp,  Monks,  Severino,  Veltri,  Suresh,  Schadt,  Erbey,  Feingold,  Patel,  Hapangama, Jordi Puig,  
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Disease relevance of Ezedoc

 

Psychiatry related information on Ezedoc

  • The objective of this analysis was to estimate the additional CHD risk reduction that could potentially be provided by co-administration of ezetimibe with statin therapy [4].
 

High impact information on Ezedoc

 

Chemical compound and disease context of Ezedoc

 

Biological context of Ezedoc

 

Anatomical context of Ezedoc

 

Associations of Ezedoc with other chemical compounds

 

Gene context of Ezedoc

 

Analytical, diagnostic and therapeutic context of Ezedoc

References

  1. New insights into the genetic regulation of intestinal cholesterol absorption. Lammert, F., Wang, D.Q. Gastroenterology (2005) [Pubmed]
  2. Intestinal cholesterol absorption inhibitor ezetimibe added to cholestyramine for sitosterolemia and xanthomatosis. Salen, G., Starc, T., Sisk, C.M., Patel, S.B. Gastroenterology (2006) [Pubmed]
  3. Ezetimibe, a potent cholesterol absorption inhibitor, normalizes combined dyslipidemia in obese hyperinsulinemic hamsters. van Heek, M., Austin, T.M., Farley, C., Cook, J.A., Tetzloff, G.G., Davis, H.R. Diabetes (2001) [Pubmed]
  4. Projected coronary heart disease risk benefit with ezetimibe. Davies, G.M., Cook, J.R., Erbey, J., Alemao, E., Veltri, E.P. Atherosclerosis (2005) [Pubmed]
  5. Disruption of cholesterol homeostasis by plant sterols. Yang, C., Yu, L., Li, W., Xu, F., Cohen, J.C., Hobbs, H.H. J. Clin. Invest. (2004) [Pubmed]
  6. The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1). Garcia-Calvo, M., Lisnock, J., Bull, H.G., Hawes, B.E., Burnett, D.A., Braun, M.P., Crona, J.H., Davis, H.R., Dean, D.C., Detmers, P.A., Graziano, M.P., Hughes, M., Macintyre, D.E., Ogawa, A., O'neill, K.A., Iyer, S.P., Shevell, D.E., Smith, M.M., Tang, Y.S., Makarewicz, A.M., Ujjainwalla, F., Altmann, S.W., Chapman, K.T., Thornberry, N.A. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  7. Efficacy of simvastatin and ezetimibe in treating hypercholesterolemia. Davidson, M.H. J. Am. Coll. Cardiol. (2003) [Pubmed]
  8. Efficacy and safety of ezetimibe coadministered with pravastatin in patients with primary hypercholesterolemia: a prospective, randomized, double-blind trial. Melani, L., Mills, R., Hassman, D., Lipetz, R., Lipka, L., LeBeaut, A., Suresh, R., Mukhopadhyay, P., Veltri, E. Eur. Heart J. (2003) [Pubmed]
  9. Efficacy and safety of ezetimibe co-administered with simvastatin compared with atorvastatin in adults with hypercholesterolemia. Ballantyne, C.M., Blazing, M.A., King, T.R., Brady, W.E., Palmisano, J. Am. J. Cardiol. (2004) [Pubmed]
  10. Efficacy and safety of ezetimibe coadministered with lovastatin in primary hypercholesterolemia. Kerzner, B., Corbelli, J., Sharp, S., Lipka, L.J., Melani, L., LeBeaut, A., Suresh, R., Mukhopadhyay, P., Veltri, E.P. Am. J. Cardiol. (2003) [Pubmed]
  11. Rhabdomyolysis associated with pomegranate juice consumption. Sorokin, A.V., Duncan, B., Panetta, R., Thompson, P.D. Am. J. Cardiol. (2006) [Pubmed]
  12. Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, an inhibitor of multidrug transport proteins. Oswald, S., Giessmann, T., Luetjohann, D., Wegner, D., Rosskopf, D., Weitschies, W., Siegmund, W. Clin. Pharmacol. Ther. (2006) [Pubmed]
  13. In Vivo Responsiveness to Ezetimibe Correlates with Niemann-Pick C1 Like-1 (NPC1L1) Binding Affinity: Comparison of Multiple Species NPC1L1 Orthologs. Hawes, B.E., O'neill, K.A., Yao, X., Crona, J.H., Davis, H.R., Graziano, M.P., Altmann, S.W. Mol. Pharmacol. (2007) [Pubmed]
  14. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Kosoglou, T., Statkevich, P., Johnson-Levonas, A.O., Paolini, J.F., Bergman, A.J., Alton, K.B. Clinical pharmacokinetics. (2005) [Pubmed]
  15. Ezetimibe inhibits the incorporation of dietary oxidized cholesterol into lipoproteins. Staprans, I., Pan, X.M., Rapp, J.H., Moser, A.H., Feingold, K.R. J. Lipid Res. (2006) [Pubmed]
  16. Aminopeptidase N (CD13) is a molecular target of the cholesterol absorption inhibitor ezetimibe in the enterocyte brush border membrane. Kramer, W., Girbig, F., Corsiero, D., Pfenninger, A., Frick, W., Jähne, G., Rhein, M., Wendler, W., Lottspeich, F., Hochleitner, E.O., Orsó, E., Schmitz, G. J. Biol. Chem. (2005) [Pubmed]
  17. Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia). Ghosal, A., Hapangama, N., Yuan, Y., Achanfuo-Yeboah, J., Iannucci, R., Chowdhury, S., Alton, K., Patrick, J.E., Zbaida, S. Drug Metab. Dispos. (2004) [Pubmed]
  18. Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia. Davidson, M.H., McGarry, T., Bettis, R., Melani, L., Lipka, L.J., LeBeaut, A.P., Suresh, R., Sun, S., Veltri, E.P. J. Am. Coll. Cardiol. (2002) [Pubmed]
  19. Lipid-lowering drugs. Pahan, K. Cell. Mol. Life Sci. (2006) [Pubmed]
  20. Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. During, A., Dawson, H.D., Harrison, E.H. J. Nutr. (2005) [Pubmed]
  21. Ezetimibe, a promising lipid-lowering agent for the treatment of dyslipidaemia in HIV-infected patients with poor response to statins. Negredo, E., Moltó, J., Puig, J., Cinquegrana, D., Bonjoch, A., Pérez-Alvarez, N., López-Blázquez, R., Blanco, A., Clotet, B., Rey-Joly, C. AIDS (2006) [Pubmed]
  22. Intestinal expression of P-glycoprotein (ABCB1), multidrug resistance associated protein 2 (ABCC2), and uridine diphosphate-glucuronosyltransferase 1A1 predicts the disposition and modulates the effects of the cholesterol absorption inhibitor ezetimibe in humans. Oswald, S., Haenisch, S., Fricke, C., Sudhop, T., Remmler, C., Giessmann, T., Jedlitschky, G., Adam, U., Dazert, E., Warzok, R., Wacke, W., Cascorbi, I., Kroemer, H.K., Weitschies, W., von Bergmann, K., Siegmund, W. Clin. Pharmacol. Ther. (2006) [Pubmed]
  23. Annexin 2-caveolin 1 complex is a target of ezetimibe and regulates intestinal cholesterol transport. Smart, E.J., De Rose, R.A., Farber, S.A. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  24. Caveolin-1 is not required for murine intestinal cholesterol transport. Valasek, M.A., Weng, J., Shaul, P.W., Anderson, R.G., Repa, J.J. J. Biol. Chem. (2005) [Pubmed]
  25. Ezetimibe normalizes metabolic defects in mice lacking ABCG5 and ABCG8. Yu, L., von Bergmann, K., Lütjohann, D., Hobbs, H.H., Cohen, J.C. J. Lipid Res. (2005) [Pubmed]
  26. Disposition of ezetimibe is influenced by polymorphisms of the hepatic uptake carrier OATP1B1. Oswald, S., König, J., Lütjohann, D., Giessmann, T., Kroemer, H.K., Rimmbach, C., Rosskopf, D., Fromm, M.F., Siegmund, W. Pharmacogenet. Genomics (2008) [Pubmed]
  27. Therapy and clinical trials: ezetimibe. Jialal, I., Kappagoda, T. Curr. Opin. Lipidol. (2003) [Pubmed]
  28. Sequence variation in NPC1L1 and association with improved LDL-cholesterol lowering in response to ezetimibe treatment. Simon, J.S., Karnoub, M.C., Devlin, D.J., Arreaza, M.G., Qiu, P., Monks, S.A., Severino, M.E., Deutsch, P., Palmisano, J., Sachs, A.B., Bayne, M.L., Plump, A.S., Schadt, E.E. Genomics (2005) [Pubmed]
  29. Autosomal recessive hypercholesterolaemia: normalization of plasma LDL cholesterol by ezetimibe in combination with statin treatment. Lind, S., Olsson, A.G., Eriksson, M., Rudling, M., Eggertsen, G., Angelin, B. J. Intern. Med. (2004) [Pubmed]
  30. Ezetimibe/simvastatin vs atorvastatin in patients with type 2 diabetes mellitus and hypercholesterolemia: the VYTAL study. Goldberg, R.B., Guyton, J.R., Mazzone, T., Weinstock, R.S., Polis, A., Edwards, P., Tomassini, J.E., Tershakovec, A.M. Mayo Clin. Proc. (2006) [Pubmed]
 
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