Molecular mechanism of altered ezetimibe disposition in nonalcoholic steatohepatitis

Drug Metabolism and Disposition

Volumn 40, Issue 3, 2012, Pages 450-460

  Hardwick, Rhiannon N ^a   Fisher, Craig D ^a   Street, Stephanie M ^a   Canet, Mark J ^a   Cherrington, Nathan J ^a  

^a UNIVERSITY OF ARIZONA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ABC TRANSPORTER C2; ABC TRANSPORTER C3; CARRIER PROTEIN; CHOLINE; DRUG METABOLITE; E 975000; EZETIMIBE; EZETIMIBE GLUCURONIDE; METHIONINE; MULTIDRUG RESISTANCE PROTEIN 1; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CELLULAR DISTRIBUTION; CONTROLLED STUDY; DRUG BILE LEVEL; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG RETENTION; DRUG TRANSPORT; INTERNALIZATION; INTRAHEPATIC BILE DUCT; LIVER MEMBRANE; MALE; NONALCOHOLIC FATTY LIVER; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN INDUCTION; PROTEIN LOCALIZATION; RAT;

ANIMALS; ANTICHOLESTEREMIC AGENTS; AZETIDINES; BILE ACIDS AND SALTS; BILIARY TRACT; BIOLOGICAL TRANSPORT; CHOLINE DEFICIENCY; DIET; FATTY LIVER; GLUCURONOSYLTRANSFERASE; INTESTINES; LIVER; MALE; MEMBRANE TRANSPORT PROTEINS; METHIONINE; MULTIDRUG RESISTANCE-ASSOCIATED PROTEINS; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84857428305     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.041095     Document Type: Article

References (28)

1. Adams LA and Angulo P (2005) Recent concepts in non-alcoholic fatty liver disease. Diabetic Med 22:1129-1133. (Pubitemid 41224168)
2. Ali R and Cusi K (2009) New diagnostic and treatment approaches in non-alcoholic fatty liver disease (NAFLD). Ann Med 41:265-278.
3. Brady JM, Cherrington NJ, Hartley DP, Buist SC, Li N, and Klaassen CD (2002) Tissue distribution and chemical induction of multiple drug resistance genes in rats. Drug Metab Dispos 30:838-844. (Pubitemid 34671097)
4. Cherrington NJ, Hartley DP, Li N, Johnson DR, and Klaassen CD (2002) Organ distribution of multidrug resistance proteins 1, 2, and 3 (Mrp1, 2, and 3) mRNA and hepatic induction of Mrp3 by constitutive androstane receptor activators in rats. J Pharmacol Exp Ther 300:97-104. (Pubitemid 34028514)
5. Chu XY, Huskey SE, Braun MP, Sarkadi B, Evans DC, and Evers R (2004) Transport of ethinylestradiol glucuronide and ethinylestradiol sulfate by the multidrug resistance proteins MRP1, MRP2, and MRP3. J Pharmacol Exp Ther 309:156-164. (Pubitemid 38393126)
6. de Waart DR, Vlaming ML, Kunne C, Schinkel AH, and Oude Elferink RP (2009) Complex pharmacokinetic behavior of ezetimibe depends on Abcc2, Abcc3, and Abcg2. Drug Metab Dispos 37:1698-1702.
7. Fan JG (2008) Impact of non-alcoholic fatty liver disease on accelerated metabolic complications. J Dig Dis 9:63-67.
8. Fan JG and Qiao L (2009) Commonly used animal models of non-alcoholic steatohepatitis. Hepatobiliary Pancreat Dis Int 8:233-240.
9. Fisher CD, Lickteig AJ, Augustine LM, Oude Elferink RP, Besselsen DG, Erickson RP, and Cherrington NJ (2009a) Experimental non-alcoholic fatty liver disease results in decreased hepatic uptake transporter expression and function in rats. Eur J Pharmacol 613:119-127.
10. Fisher CD, Lickteig AJ, Augustine LM, Ranger-Moore J, Jackson JP, Ferguson SS, and Cherrington NJ (2009b) Hepatic cytochrome P450 enzyme alterations in humans with progressive stages of nonalcoholic fatty liver disease. Drug Metab Dispos 37:2087-2094.
11. Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, Crona JH, Davis HR Jr, Dean DC, Detmers PA, et al. (2005) The target of ezetimibe is Niemann-Pick C1-like 1 (NPC1L1). Proc Natl Acad Sci USA 102:8132-8137. (Pubitemid 40800055)
12. Hardwick RN, Fisher CD, Canet MJ, Lake AD, and Cherrington NJ (2010) Diversity in antioxidant response enzymes in progressive stages of human nonalcoholic fatty liver disease. Drug Metab Dispos 38:2293-2301.
13. Institute of Laboratory Animal Resources (1996) Guide for the Care and Use of Laboratory Animals, 7th ed, Institute of Laboratory Animal Resources, Commission on Life Sciences, National Research Council, Washington DC.
14. Kosoglou T, Statkevich P, Johnson-Levonas AO, Paolini JF, Bergman AJ, and Alton KB (2005) Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet 4:467-494. (Pubitemid 40733733)
15. Lickteig AJ, Fisher CD, Augustine LM, Aleksunes LM, Besselsen DG, Slitt AL, Manautou JE, and Cherrington NJ (2007) Efflux transporter expression and acetaminophen metabolite excretion are altered in rodent models of nonalcoholic fatty liver disease. Drug Metab Dispos 35:1970-1978. (Pubitemid 47481594)
16. Manautou JE, de Waart DR, Kunne C, Zelcer N, Goedken M, Borst P, and Elferink RO (2005) Altered disposition of acetaminophen in mice with a disruption of the Mrp3 gene. Hepatology 42:1091-1098. (Pubitemid 43112676)
17. Marchesini G, Bugianesi E, Forlani G, Cerrelli F, Lenzi M, Manini R, Natale S, Vanni E, Villanova N, Melchionda N, et al. (2003) Nonalcoholic fatty liver, steatohepatitis, and the metabolic syndrome. Hepatology 37:917-923. (Pubitemid 36397405)
18. Marra F, Gastaldelli A, Svegliati Baroni G, Tell G, and Tiribelli C (2008) Molecular basis and mechanisms of progression of non-alcoholic steatohepatitis. Trends Mol Med 14:72-81.
19. McCullough AJ (2006) Pathophysiology of nonalcoholic steatohepatitis. J Clin Gastroenterol 40:S17-S29.
20. Mottino AD, Cao J, Veggi LM, Crocenzi F, Roma MG, and Vore M (2002) Altered localization and activity of canalicular Mrp2 in estradiol-17β-D- glucuronide-induced cholestasis. Hepatology 35:1409-1419. (Pubitemid 34966895)
21. Mottino AD, Crocenzi FA, Pozzi EJ, Veggi LM, Roma MG, and Vore M (2005) Role of microtubules in estradiol-17β-D-glucuronide-induced alteration of canalicular Mrp2 localization and activity. Am J Physiol Gastrointest Liver Physiol 288:G327-G336. (Pubitemid 40129585)
22. Oswald S, Koll C, and Siegmund W (2007) Disposition of the cholesterol absorption inhibitor ezetimibe in mdr1a/b (-/-) mice. J Pharm Sci 96:3478-3484.
23. Oswald S, May K, Rosin J, Lütjohann D, and Siegmund W (2010) Synergistic influence of Abcb1 and Abcc2 on disposition and sterol lowering effects of ezetimibe in rats. J Pharm Sci 99:422-429.
24. Oswald S, Scheuch E, Cascorbi I, and Siegmund W (2006a) A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1. J Chromatogr B Analyt Technol Biomed Life Sci 830:143-150. (Pubitemid 41831400)
25. Oswald S, Westrup S, Grube M, Kroemer HK, Weitschies W, and Siegmund W (2006b) Disposition and sterol-lowering effect of ezetimibe in multidrug resistance-associated protein 2-deficient rats. J Pharmacol Exp Ther 318:1293-1299. (Pubitemid 44268338)
26. Schattenberg JM and Galle PR (2010) Animal models of non-alcoholic steatohepatitis: of mice and man. Dig Dis 28:247-254.
27. Vansell NR and Klaassen CD (2002) Increase in rat liver UDP-glucuronosyltransferase mRNA by microsomal enzyme inducers that enhance thyroid hormone glucuronidation. Drug Metab Dispos 30:240-246. (Pubitemid 34175013)
28. Zhang P, Tian X, Chandra P, and Brouwer KL (2005) Role of glycosylation in trafficking of Mrp2 in sandwich-cultured rat hepatocytes. Mol Pharmacol 67:1334-1341. (Pubitemid 40410434)