Drug-induced effects on cholesterol catabolism and bile acids

Current Opinion in Investigational Drugs

Volumn 7, Issue 3, 2006, Pages 214-218

  Gylling, Helena ^a   Miettinen, Tatu A ^b  

^a UNIVERSITY OF EASTERN FINLAND   (Finland)

^b UNIVERSITY OF HELSINKI   (Finland)

Author keywords

Bile acid synthesis; Cholesterol; Cholesterol absorption; Cholesterol synthesis; Colestimide; Colesvelam; Ezetimibe; Fiber; Fibrates

Indexed keywords

2 METHYLPROPANETHIOIC ACID S [2 [1 (2 ETHYLBUTYL)CYCLOHEXYLCARBOXAMIDO]PHENYL] ESTER; BILE ACID; BILE ACID SEQUESTRANT; CHOLESTEROL; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; CHOLESTEROL ESTER TRANSFER PROTEIN INHIBITOR; CHOLESTEROL ESTERASE; COLESEVELAM; COLESTILAN; COLESTIPOL; COLESTYRAMINE; EZETIMIBE; FIBRIC ACID DERIVATIVE; GEMFIBROZIL; GW 610742; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; HYPOCHOLESTEROLEMIC AGENT; ISPAGULA; MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN INHIBITOR; N (2,2,2 TRIFLUOROETHYL) N [4 [2,2,2 TRIFLUORO 1 HYDROXY 1 (TRIFLUOROMETHOXY)ETHYL]PHENYL]BENZENESULFONAMIDE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PLACEBO; RESIN; ROSUVASTATIN; SOYBEAN PROTEIN; STANOL ESTER; STEROL; TORCETRAPIB; UNCLASSIFIED DRUG; UNINDEXED DRUG;

BILE ACID METABOLISM; BILE ACID SYNTHESIS; BLOATING; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL METABOLISM; CHOLESTEROL SYNTHESIS; CLINICAL TRIAL; CONSTIPATION; DISEASE SEVERITY; DRUG FORMULATION; DRUG STRUCTURE; DRUG TARGETING; DYSPEPSIA; FAMILIAL HYPERCHOLESTEROLEMIA; FLATULENCE; GASTROINTESTINAL TOXICITY; HEARTBURN; HUMAN; INTESTINE CELL; LIPID ABSORPTION; LIPOLYSIS; NAUSEA; NONHUMAN; PROTEIN FUNCTION; REVIEW; STRUCTURE ACTIVITY RELATION; SYSTEMATIC REVIEW;

ALLYLAMINE; ANTICHOLESTEREMIC AGENTS; AZETIDINES; BILE ACIDS AND SALTS; CHOLESTEROL; EPICHLOROHYDRIN; HUMANS; IMIDAZOLES; RESINS, SYNTHETIC;

EID: 33644955931     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (41)

1. Gagne C, Bays HE, Weiss SR, Mata P, Quinto K, Melino M, Cho M, Musliner TA, Gumbiner B, Ezetimibe Study Group: Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia. Am J Cardiol (2002) 90(10):1084-1091
2. Dujovne CA, Ettinger MP, McNeer JF, Lipka LJ, LeBeaut AP, Suresh R, Yang B, Veltri EP, Ezetimibe Study Group: Efficacy and safety of a potent new selective cholesterol absorption inhibitor, ezetimibe, in patients with primary hypercholesterolemia. Am J Caidiol (2002) 90(10):1092-1097.
3. Sudhop T, Lutjohann D, Kodal A, Igel M, Tribble DL, Shah S, Perevozskaya I, von Bergmann K: Inhibition of intestinal cholesterol absorption by ezetimibe in humans. Circulation (2002) 106(15):1943-1948.
4. Salen G, von Bergmann K, Lütjohann D, Kwiterovich P, Kane J, Patel SB, Musliner T, Stein P, Musser B, Multicenter Sitosterolemia Study Group: Ezetimibe effectively reduces plasma plant sterols in patients with sitosterolemia. Circulation (2004) 109(8):966-971.
5. Berge KE, Tian H, Graf GA, Yu L, Grishin NV, Schultz J, Kwiterovich P, Shan B, Barnes R, Hobbs HH: Accumulation of dietary cholesterol in sitosterolemia caused by mutations in adjacent ABC transporters. Science (2000) 290(5497): 1771-1775.
6. Lee MH, Lu K, Hazard S, Yu H, Shulenin S, Hidaka H, Kojima H, Allikmets R, Sakuma N, Pegoraro R, Srivastava AK et al: Identification of a gene, ABCG5, important in the regulation of dietary cholesterol absorption. Nat Genet (2001) 27(1):79-83.
7. Björkhem I, Boberg KM, Leitersdorf E: Inborn errors in bile acid biosynthesis and storage of sterols other than cholesterol. In: The Metabolic and Molecular Bases of Inherited Disease. Scriver CS, Beaudet AL, Sly WS, Valle D (Eds), McGraw-Hill, New York, USA (2001):2961-2988.
8. Repa JJ, Turley SD, Quan G, Dietschy JM: Delineation of molecular changes in intrahepatic cholesterol metabolism resulting from diminished cholesterol absorption. J Lipid Res (2005) 46(4):779-789.
9. Altmann SW, Davis HR Jr, Zhu LJ, Yao X, Hoos LM, Tetzloff G, Iyer SPN, Maguire M, Golovko A, Zeng M, Wang L et al: Niemann-Plck C1 Like 1 protein is critical for intestinal cholesterol absorption. Science (2004) 303(5661):1201-1204.
10. Davies JP, Scott C, Oishi K, Liapis A, Ioannou YA: Inactivation of NPC1L1 causes multiple lipid transport defects and protects against diet-induced hypercholesterolemia. J Biol Chem (2005) 280(13):12710-12720.
11. Kramer W, Girbig F, Corsiero D, Pfenninger A, Frick W, Jähne G, Rhein M, Wendler W, Lottspeich F, Hochleitner EO, Orsó E, Schmitz G: Aminopeptidase N (CD13) is a molecular target of the cholesterol absorption inhibitor ezetimibe in the enterocyte brush border membrane. J Biol Chem (2005) 280(2):1306-1320.
12. Kramer W, Girbig F, Corsiero D, Burger K, Fahrenholz F, Jung C, Müller G: Intestinal cholesterol absorption: Identification of different binding proteins for cholesterol and cholesterol absorption inhibitors in the enterocyte brush border membrane. Biochim Biophys Acta (2003) 1633(1):13-26.
13. Berge KE: Sitosterolemia: A gateway to new knowledge about cholesterol metabolism. Ann Med (2003) 35(7):502-511.
14. Yu L, Li-Hawkins J, Hammer RE, Berge KE, Horton JD, Cohen JC, Hobbs HH: Overexpression of ABCG5 and ABCG8 promotes biliary cholesterol secretion and reduces fractional absorption of dietary cholesterol. J Clin Invest (2002) 110(5):671-680.
15. Yu L, Hammer RE, Li-Hawkins J, von Bergmann K, Lutjohann D, Cohen JC, Hobbs HH: Disruption of Abcg5 and Abcg8 in mice reveals their crucial role in biliary cholesterol secretion. Proc Natl Acad Sci USA (2002) 99(25):16237-16242.
16. Yu L, York J, von Bergmann K, Lutjohann D, Cohen JC, Hobbs HH: Stimulation of cholesterol excretion by the liver X receptor agonist requires ATP-binding cassette transporters G5 and G8. J Biol Chem (2003) 278(18):15565-15570.
17. Miettinen TA: Phytosterolaemia, xanthomatosis and premature atherosclerotic arterial disease: A case with high plant sterol absorption, impaired sterol elimination and low cholesterol synthesis. Eur J Clin Invest (1980) 10(1):27-35.
18. Post SM, Duez H, Gervois PP, Staels B, Kuipers F, Princen HMG: Fibrates suppress bile acid synthesis via peroxisome proliferator-activated receptor-α-mediated downregulation of cholesterol 7α-hydroxylase and sterol 27-hydroxylase expression. Arterioscler Thromb Vasc Biol (2001) 21(11):1840-1845.
19. Vanhanen HT, Miettinen TA: Cholesterol absorption and synthesis during pravastatin, gemfibrozil and their combination. Atherosclerosis (1995) 115(2):135-146.
20. van der Veen JN, Kruit JK, Havinga R, Baller JFW, Chimini G, Lestavel S, Staels B, Groot PHE, Groen AK, Kuipers F: Reduced cholesterol absorption upon PPARδ activation coincides with decreased intestinal expression of NPC1L1. J Lipid Res (2005) 46(3):526-534.
21. Inazu A, Brown ML, Hesler CB, Agellon LB, Koizumi J, Takata K, Maruhama Y, Mabuchi H, Tall AR: Increased high-density lipoprotein levels caused by a common cholesteryl-ester transfer protein gene mutation. N Engl J Med (1990) 323(18):1234-1238.
22. Koizumi J, Mabuchi H, Yoshimura A, Michishita I, Takeda M, Itoh H, Sakai Y, Sakai T, Ueda K, Takeda R: Deficiency of serum cholesteryl-ester transfer activity in patients with familial hyperalphalipoproteinaemia. Atherosclerosis (1985) 58(1-3): 175-186.
23. Yamashita S, Matsuzawa Y, Okazaki M, Kako H, Yasugi T, Akioka H, Hirano K, Tarui S: Small polydisperse low density lipoproteins in familial hyperalphalipoproteinemia with complete deficiency of cholesteryl ester transfer activity. Atherosclerosis (1988) 70(1-2):7-12.
24. de Grooth GJ, Klerkx AHEM, Stroes ESG, Stalenhoef AFH, Kastelein JJP, Kuivenhoven JA: A review of CETP and its relation to atherosclerosis. J Lipid Res (2004) 45(11):1967-1974.
25. de Grooth GJ, Kuivenhoven JA, Stalenhoef AF, de Graaf J, Zwinderman AH, Posma JL, van Tol A, Kastelein JJ: Efficacy and safety of a novel cholesteryl ester transfer protein inhibitor, JTT-705, in humans: A randomized phase II dose-response study. Circulation (2002) 105(18):2159-2165.
26. Clark RW, Sutfin TA, Ruggeri RB, Willauer AT, Sugarman ED, Magnus-Aryitey G, Cosgrove PG, Sand TM, Wester RT, Williams JA, Perlman ME, Bamberger MJ: Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: An initial multidose study of torcetrapib. Arterioscler Thromb Vasc Biol (2004) 24(3):490-497.
27. Brousseau ME, Diffenderfer MR, Millar JS, Nartsupha C, Asztalos BF, Welty FK, Wolfe ML, Rudling M, Bjorkhem I, Angelin B, Mancuso JP et al: Effects of cholesteryl ester transfer protein inhibition on high-density lipoprotein subspecies, apolipoprotein A-I metabolism, and fecal sterol excretion. Arterioscler Thromb Vasc Biol (2005) 25(5):1057-1064.
28. Miettinen TA, Lempinen M: Cholestyramine and ileal by-pass in the treatment of familial hypercholesterolaemia. Eur J Clin Invest (1977) 7(6):509-514.
29. Miettinen TA: Quantitation and metabolism of bile acids in hyperlipoproteinemias. In: Liver, Nutrition and Bile Acids. Galli G, Bosisio E (Eds), Plenum Press, New York, NY, USA, and London, UK (1985):87-100.
30. Buchwald H, Varco RL, Matts JP, Long JM, Fitch LL, Campbell GS, Pearce MB, Yellin AE, Edmiston WA, Smink RD Jr et al: Effect of partial ileal bypass surgery on mortality and morbidity from coronary heart disease in patients with hypercholesterolemia. Report of the Program on the Surgical Control of the Hyperlipidemias (POSCH). N Engl J Med (1990) 323(14):946-955.
31. The Lipid Research Clinics Coronary Primary Prevention Trial Results. I. Reduction in incidence of coronary heart disease. J Am Med Assoc (1984) 251(3):351-364; 365-374.
32. Melian EB, Plosker GL: Colesvelam. Am J Cardiovasc Drugs (2001) 1(2):141-146.
33. Homma Y, Kobayashi T, Yamaguchi H, Ozawa H, Sakane H, Nakamura H: Specific reduction of plasma large, light low-density lipoprotein by a bile acid sequestering resin, cholebine (MCI-196) in type II hyperlipoprotoeinemia. Atherosclerosis (1997) 129(2):241-248.
34. Kawashiri M, Higashikata T, Nohara A, Kobayashi J, Inazu A, Koizumi J, Mabuchi H: Efficacy of colestimide coadministred with atorvastatin in Japanese patients with heterozygous familial hypercholesterolemia (FH). Circ J (2005) 69(5):515-520.
35. Booker ML: S-8921 (Shionogi). Curr Opin Invest Drugs (2001) 2(3):393-395.
36. Uusitupa MIJ, Miettinen TA, Happonen P, Ebeling T, Turtola H, Voutilainen E, Pyörälä K: Lathosterol and other noncholesterol sterols during treatment of hypercholesterolemia with lovastatin alone and with cholestyramine or guar gum. Arterioscl Thromb (1992) 12(7):807-813.
37. Ballantyne CM, Miller E, Chitra R: Efficacy and safety of rosuvastatin alone and in combination with cholestyramine in patients with severe hypercholesterolemia: A randomized, open label, multicenter trial. Clin Ther (2004) 26(11):1855-1864.
38. Xydakis AM, Guyton JR, Chiou P, Stein JL, Jones PH, Ballantyne CM: Effectiveness and tolerability of ezetimibe add-on therapy to a bile acid resin-based regimen for hypercholesterolemia. Am J Cardiol (2004) 94(8):795-797.
39. Zema MJ: Colesevelam HCI and ezetimibe combination therapy provides effective lipid-lowering in difficult-to-treat patients with hypercholesterolemia. Am J Ther (2005) 12(4):306-310.
40. Gylling H, Miettinen TA: LDL cholesterol lowering by bile acid malabsorption during inhibited synthesis and absorption of cholesterol in hypercholesterolemic coronary subjects. Nutr Metab Cardiovas Dis (2002) 12(1):19-23.
41. Jenkins DJ, Kendall CW, Marchie A, Faulkner DA, Wong JM, de Souza R, Emam A, Parker TL, Vidgren E, Trautwein EA, Lapsley KG et al: Direct comparison of a dietary portfolio of cholesterol-lowering foods with a statin in hypercholesterolemic participants. Am J Clin Nutr (2005) 81(2):380-387.