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More recently, the discovery and development of ezetimibe (1,2) a novel, selective, and potent inhibitor that effectively blocks intestinal absorption of dietary and biliary cholesterol by blocking the NPC1L1, opens a new door to the treatment of hypercholesterolemia. In clinical studies ezetimibe lowers plasma LDLcholesterol by 15% to 20% and has demonstrated antiatherosclerotic activity in experimental and clinical hypercholesterolemia (3)... (cytuje sama siebie
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Ref.
1: S.B. Rosenblum, T. Huynh, A. Afonso, H.R. Davis Jr, N. Yumibe, J.W. Clader and D.A.
Burnett, Discovery of 1(4fluorophenyl)(3R)[3(4fluorophenyl)(3Shydroxypropyl](4S)(4hydroxyphenyl)2azetidinone(SCH 58235) a designed, potent, orally active inhibitor of cholesterol absorption, J Med Chem 41 (1998), pp. 973–980.
2: D.A. Burnett, M.A. Caplen, H.R. Davis Jr, R.E. Burrier and J.W. Clader, 2Azetidinones as inhibitors of cholesterol absorption, J Med Chem 37 (1994), pp. 1733–1736.
3: C.A. Dujovne, M.P. Ettinger, J.F. McNeer, L.J. Lipka, A.P. LeBeaut, R. Suresh, B. Yang, E.P. Veltri and Ezetimbe Study Group, Efficacy and safety of a potent new selective cholesterol absorption inhibitor, ezetimibe, in patients with primary hypercholesterolemia, Am J Cardiol 90(2002), pp. 1092–1097.
Macie jakies dane na temat stosowania ezetimibe w Polsce? Jest zarejestrowany, sa jakies dane kliniczne?
Zmieniony przez - Martucca w dniu 2007-10-31 11:36:16