Application of in vitro-in vivo extrapolation (IVIVE) and physiologically based pharmacokinetic (PBPK) modelling to investigate the impact of the CYP2C8 polymorphism on rosiglitazone exposure

European Journal of Clinical Pharmacology

Volumn 69, Issue 6, 2013, Pages 1311-1320

  Yeo, Karen Rowland ^a   Kenny, Jane R ^b   Rostami Hodjegan, Amin ^a,c  

^a CERTARA UK LIMITED   (United Kingdom)

^b GENENTECH INC   (United States)

^c UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

CYP2C8 polymorphism; Drug drug interaction; Genotype; Modelling

Indexed keywords

CYTOCHROME P450 1A2; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 3A4; ROSIGLITAZONE; TRIMETHOPRIM;

AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; DNA POLYMORPHISM; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG METABOLISM; GENE FREQUENCY; GENETIC VARIABILITY; GENOTYPE; HOMOZYGOSITY; HYDROXYLATION; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOLECULAR WEIGHT; PRIORITY JOURNAL; PROTEIN EXPRESSION; SINGLE DRUG DOSE; STEADY STATE;

ADOLESCENT; ADULT; AGED; ANALYSIS OF VARIANCE; AREA UNDER CURVE; ARYL HYDROCARBON HYDROXYLASES; CHILD; COMPUTER SIMULATION; DRUG INTERACTIONS; ENZYME INHIBITORS; FEMALE; GENE FREQUENCY; GENOTYPE; HUMANS; HYPOGLYCEMIC AGENTS; LINEAR MODELS; MALE; MICROSOMES, LIVER; MIDDLE AGED; MODELS, BIOLOGICAL; PHARMACOGENETICS; PHENOTYPE; POLYMORPHISM, GENETIC; REPRODUCIBILITY OF RESULTS; THIAZOLIDINEDIONES; TRIMETHOPRIM; YOUNG ADULT;

EID: 84878015548     PISSN: 00316970     EISSN: 14321041     Source Type: Journal    
DOI: 10.1007/s00228-012-1467-3     Document Type: Article

References (47)

1. Kirchheiner J, Thomas S, Bauer S, Tomalik-Scharte D, Hering U, Doroshyenko O, Jetter A, Stehle S, Tsahuridu M, Meineke I, Brockmoller J, Fuhr U (2006) Pharmacokinetics and pharmacodynamics of rosiglitazone in relation to CYP2C8 genotype. Clin Pharmacol Ther 80:657-667. doi: 10.1016/j.clpt.2006.09.008
2. Cox PJ, Ryan DA, Hollis FJ, Harris AM, Miller AK, Vousden M, Cowley H (2000) Absorption, disposition, and metabolism of rosiglitazone, a potent thiazolidinedione insulin sensitizer, in humans. Drug Metab Dispos 28:772-780
3. Baldwin SJ, Clarke SE, Chenery RJ (1999) Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of rosiglitazone. Br J Clin Pharmacol 48:424-432
4. Niemi M, Backman JT, Granfors M, Laitila J, Neuvonen M, Neuvonen PJ (2003) Gemfibrozil considerably increases the plasma concentrations of rosiglitazone. Diabetologia 46:1319-1323. doi: 10.1007/s00125-003-1181-x
5. Niemi M, Backman JT, Neuvonen PJ (2004) Effects of trimethoprim and rifampin on the pharmacokinetics of the cytochrome P450 2C8 substrate rosiglitazone. Clin Pharmacol Ther 76:239-249. doi: 10.1016/j.clpt.2004.05.001
6. Hruska MW, Amico JA, Langaee TY, Ferrell RE, Fitzgerald SM, Frye RF (2005) The effect of trimethoprim on CYP2C8 mediated rosiglitazone metabolism in human liver microsomes and healthy subjects. Br J Clin Pharmacol 59:70-79. doi: 10.1111/j.1365-2125.2005.02263.x
7. Dai D, Zeldin DC, Blaisdell JA, Chanas B, Coulter SJ, Ghanayem BI, Goldstein JA (2001) Polymorphisms in human CYP2C8 decrease metabolism of the anticancer drug paclitaxel and arachidonic acid. Pharmacogenetics 11:597-607
8. Kaspera R, Naraharisetti SB, Evangelista EA, Marciante KD, Psaty BM, Totah RA (2011) Drug metabolism by CYP2C8.3 is determined by substrate dependent interactions with cytochrome P450 reductase and cytochrome b5. Biochem Pharmacol 82:681-691. doi: 10.1016/j.bcp.2011.06.027
9. Daily EB, Aquilante CL (2009) Cytochrome P450 2C8 pharmacogenetics: a review of clinical studies. Pharmacogenomics 10:1489-1510. doi: 10.2217/pgs.09.82
10. Yasar U, Lundgren S, Eliasson E, Bennet A, Wiman B, de Faire U, Rane A (2002) Linkage between the CYP2C8 and CYP2C9 genetic polymorphisms. Biochem Biophys Res Commun 299:25-28
11. Bahadur N, Leathart JB, Mutch E, Steimel-Crespi D, Dunn SA, Gilissen R, Houdt JV, Hendrickx J, Mannens G, Bohets H, Williams FM, Armstrong M, Crespi CL, Daly AK (2002) CYP2C8 polymorphisms in Caucasians and their relationship with paclitaxel 6alpha-hydroxylase activity in human liver microsomes. Biochem Pharmacol 64:1579-1589
12. Naraharisetti SB, Lin YS, Rieder MJ, Marciante KD, Psaty BM, Thummel KE, Totah RA (2010) Human liver expression of CYP2C8: gender, age, and genotype effects. Drug Metab Dispos 38:889-893. doi: 10.1124/dmd.109.031542
13. Dickinson GL, Lennard MS, Tucker GT, Rostami-Hodjegan A (2007) The use of mechanistic DM-PK-PD modelling to assess the power of pharmacogenetic studies -CYP2C9 and warfarin as an example. Br J Clin Pharmacol 64:14-26. doi: 10.1111/j.1365-2125.2007.02850.x
14. Rowland Yeo K, Jamei M, Yang J, Tucker GT, Rostami-Hodjegan A (2010) Physiologically based mechanistic modelling to predict complex drug-drug interactions involving simultaneous competitive and time-dependent enzyme inhibition by parent compound and its metabolite in both liver and gut - the effect of diltiazem on the time-course of exposure to triazolam. Eur J Pharm Sci 39:298-309. doi: 10.1016/j.ejps.2009.12.002
15. Zhao P, Zhang L, Grillo JA, Liu Q, Bullock JM, Moon YJ, Song P, Brar SS, Madabushi R, Wu TC, Booth BP, Rahman NA, Reynolds KS, Gil Berglund E, Lesko LJ, Huang SM (2011) Applications of physiologically based pharmacokinetic (PBPK) modeling and simulation during regulatory review. Clin Pharmacol Ther 89:259-267. doi: 10.1038/clpt.2010.298
16. Howgate EM, Rowland Yeo K, Proctor NJ, Tucker GT, Rostami-Hodjegan A (2006) Prediction of in vivo drug clearance from in vitro data. I: impact of inter-individual variability. Xenobiotica 36:473-497. doi: 10.1080/ 00498250600683197
17. Jamei M, Marciniak S, Feng K, Barnett A, Tucker G, Rostami-Hodjegan A (2009) The Simcyp population-based ADME simulator. Expert Opin Drug Metab Toxicol 5:211-223. doi: 10.1517/17425250802691074
18. Rowland Yeo K, Rostami-Hodjegan A, Tucker GT (2004) Abundance of cytochromes P450 in human liver: a meta analysis. Br J Clin Pharmacol 57:687-688
19. Wilson ZE, Rostami-Hodjegan A, Burn JL, Tooley A, Boyle J, Ellis SW, Tucker GT (2003) Inter-individual variability in levels of human microsomal protein and hepatocellularity per gram of liver. Br J Clin Pharmacol 56:433-440
20. Johnson TN, Tucker GT, Tanner MS, Rostami-Hodjegan A (2005) Changes in liver volume from birth to adulthood: a meta-analysis. Liver Transpl 11:1481-1493. doi: 10.1002/lt.20519
21. Proctor NJ, Tucker GT, Rostami-Hodjegan A (2004) Predicting drug clearance from recombinantly expressed CYPs: intersystem extrapolation factors. Xenobiotica 34:151-178. doi: 10.1080/0049825031000164635346AHLL95GXWJ3T34
22. Austin RP, Barton P, Cockroft SL, Wenlock MC, Riley RJ (2002) The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties. Drug Metab Dispos 30:1497-1503
23. Turner DB, Rostami-Hodjegan A, Tucker GT, Rowland-Yeo K (2006) Prediction of non-specific hepatic microsomal binding from readily available physiochemical properties. 9th European ISSX Meeting, Manchester, UK, 4th-7th June 2006. In: Drug Metab Rev 38:162, A231
24. Leo MA, Lasker JM, Raucy JL, Kim CI, Black M, Lieber CS (1989) Metabolism of retinol and retinoic acid by human liver cytochrome P450IIC8. Arch Biochem Biophys 269:305-312
25. VandenBrink BM, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL (2011) Evaluation of CYP2C8 inhibition in vitro: utility of montelukast as a selective CYP2C8 probe substrate. Drug Metab Dispos 39:1546-1554. doi: 10.1124/dmd.111.039065
26. Tornio A, Niemi M, Neuvonen PJ, Backman JT (2008) Trimethoprim and the CYP2C8*3 allele have opposite effects on the pharmacokinetics of pioglitazone. Drug Metab Dispos 36:73-80. doi: 10.1124/dmd.107.018010
27. Miller AK, DiCicco RA, Freed MI (2002) The effect of ranitidine on the pharmacokinetics of rosiglitazone in healthy adult male volunteers. Clin Ther 24:1062-1071
28. Watson ID, Stewart MJ, Wiles A, McIntosh SJ (1983) Pharmacokinetics of two dosage levels of trimethoprim to 'steady-state' in normal volunteers. J Int Med Res 11:137-144
29. Dickinson GL, Rezaee S, Proctor NJ, Lennard MS, Tucker GT, Rostami-Hodjegan A (2007) Incorporating in vitro information on drug metabolism into clinical trial simulations to assess the effect of CYP2D6 polymorphism on pharmacokinetics and pharmacodynamics: dextromethorphan as a model application. J Clin Pharmacol 47:175-186. doi: 10.1177/0091270006294279
30. Kusama M, Maeda K, Chiba K, Aoyama A, Sugiyama Y (2009) Prediction of the effects of genetic polymorphism on the pharmacokinetics of CYP2C9 substrates from in vitro data. Pharm Res 26:822-835. doi: 10.1007/s11095-008-9781-2
31. Aquilante CL, Bushman LR, Knutsen SD, Burt LE, Rome LC, Kosmiski LA (2008) Influence of SLCO1B1 and CYP2C8 gene polymorphisms on rosiglitazone pharmacokinetics in healthy volunteers. Hum Genomics 3:7-16
32. Williams JA, Johnson K, Paulauskis J, Cook J (2006) So many studies, too few subjects: establishing functional relevance of genetic polymorphisms on pharmacokinetics. J Clin Pharmacol 46:258-264. doi: 10.1177/0091270005283463
33. Rostami-Hodjegan A, Tucker GT (2004) 'In silico' simulations to assess the 'in vivo' consequences of 'in vitro' metabolic drug-drug interactions. Drug Discov Today Technol 1:441-448
34. Collins C, Levy R, Ragueneau-Majlessi I, Hachad H (2006) Prediction of maximum exposure in poor metabolizers following inhibition of nonpolymorphic pathways. Curr Drug Metab 7:295-299
35. Pedersen RS, Damkier P, Brosen K (2006) The effects of human CYP2C8 genotype and fluvoxamine on the pharmacokinetics of rosiglitazone in healthy subjects. Br J Clin Pharmacol 62:682-689. doi: 10.1111/j.1365-2125.2006.02706.x
36. Gao Y, Liu D, Wang H, Zhu J, Chen C (2010) Functional characterization of five CYP2C8 variants and prediction of CYP2C8 genotype-dependent effects on in vitro and in vivo drug-drug interactions. Xenobiotica 40:467-475. doi: 10.3109/00498254.2010.487163
37. Rettie AE, Wienkers LC, Gonzalez FJ, Trager WF, Korzekwa KR (1994) Impaired (S)-warfarin metabolism catalysed by the R144C allelic variant of CYP2C9. Pharmacogenetics 4:39-42
38. Sullivan-Klose TH, Ghanayem BI, Bell DA, Zhang ZY, Kaminsky LS, Shenfield GM, Miners JO, Birkett DJ, Goldstein JA (1996) The role of the CYP2C9-Leu359 allelic variant in the tolbutamide polymorphism. Pharmacogenetics 6:341-349
39. Lee CR, Goldstein JA, Pieper JA (2002) Cytochrome P450 2C9 polymorphisms: a comprehensive review of the in-vitro and human data. Pharmacogenetics 12:251-263
40. Almond LM, Rowland-Yeo K, Howgate EM, Tucker GT, Rostami-Hodjegan A (2006) Prediction of the oral clearance of S-warfarin in CYP2C9 genotypes from in vitro enzyme kinetic data. 9th European ISSX Meeting, Manchester, UK, 4th-7th June. In: Drug Metab Rev 38: S92-93, A121 DOI 10.1080/03602530600742037
41. Committee for Medicinal Products for Human Use (2012) Guidance on the Investigation of Drug Interactions. European Medicines Agency. http://www.ema.europa.eu/doc/en-GB/document-library/Scientific-guideline/2012/ 07/WC500129606.pdf Accessed August 2012
42. Chapelsky MC, Thompson-Culkin K, Miller AK, Sack M, Blum R, Freed MI (2003) Pharmacokinetics of rosiglitazone in patients with varying degrees of renal insufficiency. J Clin Pharmacol 43:252-259
43. Yang J, Jamei M, Yeo KR, Tucker GT, Rostami-Hodjegan A (2007) Prediction of intestinal first-pass drug metabolism. Curr Drug Metab 8:676-684
44. Nowak A, Klimowicz A, Kadykow M (1985) Distribution of trimethoprim and sulphamethoxazole in blood during treatment with co-trimoxazole. Eur J Clin Pharmacol 29:231-234
45. Odlind B, Hartvig P, Fjellstrom KE, Lindstrom B, Bengtsson S (1984) Steady state pharmacokinetics of trimethoprim 300 mg once daily in healthy volunteers assessed by two independent methods. Eur J Clin Pharmacol 26:393-397
46. Klimowicz A, Nowak A, Kadykow M (1988) Plasma and skin blister fluid concentrations of trimethoprim following its oral administration. Eur J Clin Pharmacol 34:377-380
47. Watson ID, Cohen HN, Stewart MJ, McIntosh SJ, Shenkin A, Thomson JA (1982) Comparative pharmacokinetics of co-trifamole and co-trimoxazole to 'steady state' in normal subjects. Br J Clin Pharmacol 14:437-443