In vitro-in vivo correlation for low-clearance compounds using hepatocyte relay method

Drug Metabolism and Disposition

Volumn 41, Issue 12, 2013, Pages 2018-2023

  Di, Li ^a   Atkinson, Karen ^a   Orozco, Christine C ^a   Funk, Carrie ^a   Zhang, Hui ^a   McDonald, Thomas S ^a   Tan, Beijing ^a   Lin, Jian ^a   Chang, Cheng ^a   Obach, R Scott ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACEBUTOLOL; BOSENTAN; CAFFEINE; CIMETIDINE; FAMOTIDINE; FEXOFENADINE; FLUINDOSTATIN; KETOPROFEN; NAPROXEN; PHENAZONE; PRAZOSIN; RANITIDINE; TOLBUTAMIDE; WARFARIN;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CANINE MODEL; CELL ASSAY; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG CLEARANCE; HEPATOCYTE RELAY METHOD; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL; LIVER CLEARANCE; MALE; METABOLIC CLEARANCE RATE; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; RAT;

ANIMALS; DOGS; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; HEPATOCYTES; MALE; MEMBRANE TRANSPORT PROTEINS; METABOLIC CLEARANCE RATE; RATS; RATS, WISTAR;

EID: 84888631944     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.113.053322     Document Type: Article

References (44)

1. Andresen BD and Davis FT (1979) Metabolism of acebutolol-d6 in the rat correlates with the identification of a new metabolite in human urine. Drug Metab Dispos 7:360-365.
2. Ashforth EIL, Carlile DJ, Chenery R, and Houston JB (1995) Prediction of in vivo disposition from in vitro systems: clearance of phenytoin and tolbutamide using rat hepatic microsomal and hepatocyte data. J Pharmacol Exp Ther 274:761-766.
3. Balani SK, Zhu T, Yang TJ, Liu Z, He B, and Lee FW (2002) Effective dosing regimen of 1-aminobenzotriazole for inhibition of antipyrine clearance in rats, dogs, and monkeys. Drug Metab Dispos 30:1059-1062.
4. Bayliss MK and Cross DM (2000) The Hepatocyte Review, Springer, Dordrecht.
5. Belpaire FM, de Smet F, Vynckier LJ, Vermeulen AM, Rosseel MT, Bogaert MG, and Chauvelot-Moachon L (1990) Effect of aging on the pharmcokinetics of atenolol, metoprolol and propranolol in the rat. J Pharmacol Exp Ther 254:116-122.
6. Berry LM, Li C, and Zhao Z (2011) Species differences in distribution and prediction of human V (ss) from preclinical data. Drug Metab Dispos 39:2103-2116.
7. Brown HS, Griffin M, and Houston JB (2007) Evaluation of cryopreserved human hepatocytes as an alternative in vitro system to microsomes for the prediction of metabolic clearance. Drug Metab Dispos 35:293-301.
8. Di L, Kerns EH, Gao N, Li SQ, Huang Y, Bourassa JL, and Huryn DM (2004) Experimental design on single-time-point high-throughput microsomal stability assay. J Pharm Sci 93:1537-1544.
9. Di L, Trapa P, Obach RS, Atkinson K, Bi Y-A, Wolford AC, Tan B, McDonald TS, Lai Y, and Tremaine LM (2012) A novel relay method for determining low-clearance values. Drug Metab Dispos 40:1860-1865.
10. Eddershaw PJ, Chadwick AP, Higton DM, Fenwick SH, Linacre P, Jenner WN, Bell JA, and Manchee GR (1996) Absorption and disposition of ranitidine hydrochloride in rat and dog. Xenobiotica 26:947-956.
11. Granero GE and Amidon GL (2008) Possibility of enterohepatic recycling of ketoprofen in dogs. Int J Pharm 349:166-171.
12. Hallifax D, Foster JA, and Houston JB (2010) Prediction of human metabolic clearance from in vitro systems: retrospective analysis and prospective view. Pharm Res 27:2150-2161.
13. Hirate J, Zhu C, Horikoshi I, and Nagase S (1990) Disposition of warfarin in analbuminemic rats. Int J Pharm 65:149-157.
14. Hosea NA, Collard WT, Cole S, Maurer TS, Fang RX, Jones H, Kakar SM, Nakai Y, Smith BJ, and Webster R, et al. (2009) Prediction of human pharmacokinetics from preclinical information: comparative accuracy of quantitative prediction approaches. J Clin Pharmacol 49:513-533.
15. Huang L, Chen A, Roberts J, Janosky B, Be X, Berry L, and Lin M-HJ (2012) Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds. Xenobiotica 42:830-840.
16. Huntjens DRH, Spalding DJM, Danhof M, and Della Pasqua OE (2006) Correlation between in vitro and in vivo concentration-effect relationships of naproxen in rats and healthy volunteers. Br J Pharmacol 148:396-404.
17. Kilford PJ, Gertz M, Houston JB, and Galetin A (2008) Hepatocellular binding of drugs: correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data. Drug Metab Dispos 36:1194-1197.
18. Kilford PJ, Stringer R, Sohal B, Houston JB, and Galetin A (2009) Prediction of drug clearance by glucuronidation from in vitro data: use of combined cytochrome P450 and UDP-glucuronosyltransferase cofactors in alamethicin-activated human liver microsomes. Drug Metab Dispos 37:82-89.
19. Kimura K, Hirayama F, and Uekama K (1999) Characterization of tolbutamide polymorphs (Burger's forms II and IV) and polymorphic transition behavior. J Pharm Sci 88:385-391.
20. Kurata T, Muraki Y, Mizutani H, Iwamoto T, and Okuda M (2010) Elevated systemic elimination of cimetidine in rats with acute biliary obstruction: the role of renal organic cation transporter OCT2. Drug Metab Pharmacokinet 25:328-334.
21. Mandula H, Parepally JMR, Feng R, and Smith QR (2006) Role of site-specific binding to plasma albumin in drug availability to brain. J Pharmacol Exp Ther 317:667-675.
22. Matsuzaki T, Morisaki T, Sugimoto W, Yokoo K, Sato D, Nonoguchi H, Tomita K, Terada T, Inui K-i, and Hamada A, et al. (2008) Altered pharmacokinetics of cationic drugs caused by down-regulation of renal rat organic cation transporter 2 (Slc22a2) and rat multidrug and toxin extrusion 1 (Slc47a1) in ischemia/reperfusion-induced acute kidney injury. Drug Metab Dispos 36:649-654.
23. McPherson FJ and Lee RM (1977) Biliary excretion and metabolism of 14C cimetidine following oral administration to male and female rats. Experientia 33:1139-1140.
24. Morita N, Kusuhara H, Nozaki Y, Endou H, and Sugiyama Y (2005) Functional involvement of rat organic anion transporter 2 (Slc22a7) in the hepatic uptake of the nonsteroidal anti-inflammatory drug ketoprofen. Drug Metab Dispos 33:1151-1157.
25. Nakazawa K, Tanaka H, and Arima M (1985) The effect of caffeine ingestion on pharmacokinetics of caffeine and its metabolites after a single administration in pregnant rats. J Pharmacobiodyn 8:151-160.
26. Neirinckx E, Croubels S, De Boever S, Remon JP, Bosmans T, Daminet S, De Backer P, and Vervaet C (2011) Species comparison of enantioselective oral bioavailability and pharmacokinetics of ketoprofen. Res Vet Sci 91:415-421.
27. Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, and Guiral S, et al. (2011) Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem 54:5082-5096.
28. Ohkura T, Yamada S, Deguchi Y, and Kimura R (1999) Comparative study on pharmacokinetics and in vivo α1-adrenoceptor binding of [3H]tamsulosin and [3H]prazosin in rats. Biol Pharm Bull 22:412-417.
29. Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, and Tu M, et al. (2012) Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido) nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J Med Chem 55:1318-1333.
30. Piquette-Miller M and Jamali F (1997) Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats. Biopharm Drug Dispos 18:543-556.
31. Poirier A, Funk C, Scherrmann J-M, and Lavé T (2009) Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine. Mol Pharm 6:1716-1733.
32. Qin M, Nilsson M, and Oie S (1994) Decreased elimination of drug in the presence of alpha-1-acid glycoprotein is related to a reduced hepatocyte uptake. J Pharmacol Exp Ther 269:1176-1181.
33. Rangan S, Tahrani AA, Macleod AF, and Moulik PK (2007) Once weekly thyroxine treatment as a strategy to treat non-compliance. Postgrad Med J 83:e3.
34. Richmond W, Wogan M, Isbell J, and Gordon WP (2010) Interstrain differences of in vitro metabolic stability and impact on early drug discovery. J Pharm Sci 99:4463-4468.
35. Satterwhite JH and Boudinot FD (1992) Pharmacokinetics of ketoprofen in rats: effect of age and dose. Biopharm Drug Dispos 13:197-212.
36. Shitara Y, Horie T, and Sugiyama Y (2006) Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 27:425-446.
37. Suh H, Jun HW, Dzimianski MT, and Lu GW (1997) Pharmacokinetic and local tissue disposition studies of naproxen-following topical and systemic administration in dogs and rats. Biopharm Drug Dispos 18:623-633.
38. Tahara H, Kusuhara H, Fuse E, and Sugiyama Y (2005) P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. Drug Metab Dispos 33:963-968.
39. Terrier N, Benoit E, Senay C, Lapicque F, Radominska-Pandya A, Magdalou J, and Fournel-Gigleux S (1999) Human and rat liver UDP-glucuronosyltransferases are targets of ketoprofen acylglucuronide. Mol Pharmacol 56:226-234.
40. Watanabe T, Kusuhara H, Maeda K, Kanamaru H, Saito Y, Hu Z, and Sugiyama Y (2010a) Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans. Drug Metab Dispos 38:215-222.
41. Watanabe T, Kusuhara H, and Sugiyama Y (2010b) Application of physiologically based pharmacokinetic modeling and clearance concept to drugs showing transporter-mediated distribution and clearance in humans. J Pharmacokinet Pharmacodyn 37:575-590.
42. Wilby AJ, Maeda K, Courtney PF, Debori Y, Webborn PJH, Kitamura Y, Kusuhara H, Riley RJ, and Sugiyama Y (2011) Hepatic uptake in the dog: comparison of uptake in hepatocytes and human embryonic kidney cells expressing dog organic anion-transporting polypeptide 1B4. Drug Metab Dispos 39:2361-2369.
43. Yacobi A and Levy G (1977) Protein binding of warfarin enantiomers in serum of humans and rats. J Pharmacokinet Biopharm 5:123-131.
44. Yamazaki M, Suzuki H, and Sugiyama Y (1996) Recent advances in carrier-mediated hepatic uptake and biliary excretion of xenobiotics. Pharm Res 13:497-513.