An up-date review on individualized dosage adjustment of calcineurin inhibitors in organ transplant patients

Pharmacology and Therapeutics

Volumn 112, Issue 1, 2006, Pages 184-198

  Masuda, Satohiro ^a   Inui, Ken ichi ^a  

^a KYOTO UNIVERSITY HOSPITAL   (Japan)

Author keywords

Cyclosporine; Immunosuppressant; P glycoprotein; Pharmacogenomics; Tacrolimus; Transplantation

Indexed keywords

ABC TRANSPORTER A1; AZATHIOPRINE; CALCINEURIN INHIBITOR; CELL NUCLEUS RECEPTOR; CYCLOSPORIN A; CYTOCHROME P450 3A; CYTOCHROME P450 3A4; CYTOCHROME P450 3A5; DIGOXIN; DRUG METABOLIZING ENZYME; GLYCOPROTEIN P; IMMUNOSUPPRESSIVE AGENT; MESSENGER RNA; MULTIDRUG RESISTANCE PROTEIN; PHENOBARBITAL; RIFAMPICIN; STEROID; TACROLIMUS; TALINOLOL;

AREA UNDER THE CURVE; CLINICAL PRACTICE; CLINICAL TRIAL; DOSE CALCULATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG CONTRAINDICATION; DRUG DETERMINATION; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG METABOLISM; DRUG MONITORING; DRUG SAFETY; DRUG TOLERABILITY; DRUG USE; ENZYME SUBSTRATE; GENE EXPRESSION; GENOTYPE; GRAFT REJECTION; HUMAN; HYPERGLYCEMIA; IMMUNOREGULATION; IMMUNOSUPPRESSIVE TREATMENT; INTESTINE; LIVER GRAFT; LIVER METABOLISM; LIVING DONOR; MICROEMULSION; NEPHROTOXICITY; NEUROTOXICITY; NONHUMAN; ORGAN TRANSPLANTATION; PHARMACOGENOMICS; POPULATION RESEARCH; POSTOPERATIVE PERIOD; PRIORITY JOURNAL; PROTEIN EXPRESSION; REVIEW; SINGLE NUCLEOTIDE POLYMORPHISM; TREATMENT OUTCOME;

ANIMALS; CALCINEURIN; CYCLOSPORINE; DRUG MONITORING; HUMANS; IMMUNOSUPPRESSIVE AGENTS; ORGAN TRANSPLANTATION; PHARMACOGENETICS; TACROLIMUS;

EID: 33748057835     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2006.04.006     Document Type: Review

References (145)

1. Akbas S.H., Yavuz A., Tuncer M., Yurdakonar E., Akcit F., Gurkan A., et al. Evaluation of the new EMIT tacrolimus assay in kidney and liver transplant recipients. Transplant Proc 36 (2004) 86-88
2. Akbas S.H., Ozdem S., Caglar S., Tuncer M., Gurkan A., Yucetin L., et al. Effects of some hematological parameters on whole blood tacrolimus concentration measured by two immunoassay-based analytical methods. Clin Biochem 38 (2005) 552-557
3. Andrews P.A., Sen M., and Chang R.W. Racial variation in dosage requirements of tacrolimus. Lancet 348 (1996) 1446
4. Anglicheau D., Verstuyft C., Laurent-Puig P., Becquemont L., Schlageter M.H., Cassinat B., et al. Association of the multidrug resistance-1 gene single-nucleotide polymorphisms with the tacrolimus dose requirements in renal transplant recipients. J Am Soc Nephrol 14 (2003) 1889-1896
5. Anglicheau D., Thervet E., Etienne I., Hurault De Ligny B., Le Meur Y., Touchard G., et al. CYP3A5 and MDR1 genetic polymorphisms and cyclosporine pharmacokinetics after renal transplantation. Clin Pharmacol Ther 75 (2004) 422-433
6. Armendariz Y., Garcia S., Lopez R.M., and Pou L. Hematocrit influences immunoassay performance for the measurement of tacrolimus in whole blood. Ther Drug Monit 27 (2005) 766-769
7. Armstrong V.W., and Oellerich M. New developments in the immunosuppressive drug monitoring of cyclosporine, tacrolimus, and azathioprine. Clin Biochem 34 (2001) 9-16
8. Balram C., Sharma A., Sivathasan C., and Lee E.J. Frequency of C3435T single nucleotide MDR1 genetic polymorphism in an Asian population: phenotypic-genotypic correlates. Br J Clin Pharmacol 56 (2003) 78-83
9. Belitsky P., Dunn S., Johnston A., and Levy G. Impact of absorption profiling on efficacy and safety of cyclosporin therapy in transplant recipients. Clin Pharmacokinet 39 (2000) 117-125
10. Benet L.Z., Izumi T., Zhang Y., Silverman J.A., and Wacher V.J. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J Control Release 62 (1999) 25-31
11. Bonhomme-Faivre L., Devocelle A., Saliba F., Chatled S., Maccario J., Farinotti R., et al. MDR-1 C3435T polymorphism influences cyclosporine a dose requirement in liver-transplant recipients. Transplantation 78 (2004) 21-25
12. Burckart G.J., Jain A., Diven W., Venkataramanan R., and Starzl T.E. Cyclosporine measurement by FPIA, PC-RIA, and HPLC following liver transplantation. Transplant Proc 22 (1990) 1319-1322
13. Busuttil R.W., and Holt C.D. Tacrolimus (FK506) is superior to cyclosporine in liver transplantation. Transplant Proc 29 (1997) 534-538
14. Busuttil R.W., Klintmalm G.B., Lake J.R., Miller C.M., and Porayko M. General guidelines for the use of tacrolimus in adult liver transplant patients. Transplantation 61 (1996) 845-847
15. Charpiat B., Falconi I., Breant V., Jelliffe R.W., Sab J.M., Ducerf C., et al. A population pharmacokinetic model of cyclosporine in the early postoperative phase in patients with liver transplants, and its predictive performance with Bayesian fitting. Ther Drug Monit 20 (1998) 158-164
16. Chenhsu R.Y., Loong C.C., Chou M.H., Lin M.F., and Yang W.C. Renal allograft dysfunction associated with rifampin-tacrolimus interaction. Ann Pharmacother 34 (2000) 27-31
17. Chowbay B., Li H., David M., Bun C.Y., and Lee E.J. Meta-analysis of the influence of MDR1 C3435T polymorphism on digoxin pharmacokinetics and MDR1 gene expression. Br J Clin Pharmacol 60 (2005) 159-171
18. Chowbay B., Zhou S., and Lee E.J. An interethnic comparison of polymorphisms of the genes encoding drug-metabolizing enzymes and drug transporters: experience in Singapore. Drug Metab Rev 37 (2005) 327-378
19. Cogill J.L., Taylor P.J., Westley I.S., Morris R.G., Lynch S.V., and Johnson A.G. Evaluation of the tacrolimus II microparticle enzyme immunoassay (MEIA II) in liver and renal transplant recipients. Clin Chem 44 (1998) 1942-1946
20. Cooney G.F., Habucky K., and Hoppu K. Cyclosporin pharmacokinetics in paediatric transplant recipients. Clin Pharmacokinet 32 (1997) 481-495
21. de Wildt S., Kearns G.L., Leeder J.S., and van den Anker J.N. Cytochrome P450 3A: ontogeny and drug disposition. Clin Pharmacokinet 37 (1999) 485-505
22. Demetris A., Adams D., Bellamy C., Blakolmer K., Clouston A., Dhillon A.P., et al. Update of the International Banff Schema for Liver Allograft Rejection: working recommendations for the histopathologic staging and reporting of chronic rejection. An International Panel. Hepatology 31 (2000) 792-799
23. Dousset B., Conti F., Cherruau B., Louvel A., Soubrane O., Houssin D., et al. Is acute rejection deleterious to long-term liver allograft function?. J Hepatol 29 (1998) 660-668
24. Frezza E.E., Tzakis A., Fung J.J., and Van Thiel D.H. Small bowel transplantation: current progress and clinical application. Hepatogastroenterology 43 (1996) 363-376
25. Friman S., and Backman L. A new microemulsion formulation of cyclosporin: pharmacokinetic and clinical features. Clin Pharmacokinet 30 (1996) 181-193
26. Fromm M.F. P-glycoprotein: a defense mechanism limiting oral bioavailability and CNS accumulation of drugs. Int J Clin Pharmacol Ther 38 (2000) 69-74
27. Fukatsu S., Yano I., Igarashi T., Hashida T., Takayanagi K., Saito H., et al. Population pharmacokinetics of tacrolimus in adult recipients receiving living-donor liver transplantation. Eur J Clin Pharmacol 57 (2001) 479-484
28. Fukudo M., Yano I., Fukatsu S., Saito H., Uemoto S., Kiuchi T., et al. Forecasting of blood tacrolimus concentrations based on the Bayesian method in adult patients receiving living-donor liver transplantation. Clin Pharmacokinet 42 (2003) 1161-1178
29. Fukudo M., Yano I., Masuda S., Fukatsu S., Katsura T., Ogura Y., et al. Pharmacodynamic analysis of tacrolimus and cyclosporine in living-donor liver transplant patients. Clin Pharmacol Ther 78 (2005) 168-181
30. Fukudo M., Yano I., Masuda S., Okuda M., and Inui K. Distinct inhibitory effects of tacrolimus and cyclosporin A on calcineurin phosphatase activity. J Pharmacol Exp Ther 312 (2005) 816-825
31. Fukudo M., Yano I., Masuda S., Katsura T., Ogura Y., Oike F., et al. Cyclosporine exposure and calcineurin phosphatase activity in living-donor liver transplant patients: twice daily versus once daily dosing. Liver Transpl 12 (2006) 292-300
32. Garcia G.M., Pera M.C., Bernardos R.A., Gomez G.M., Herrero J.I., Mir P.J., et al. An open, randomized, multicenter clinical trial of oral tacrolimus in liver allograft transplantation: a comparison of dual vs. triple drug therapy. Liver Transpl 11 (2005) 515-524
33. Geick A., Eichelbaum M., and Burk O. Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem 276 (2001) 14581-14587
34. Gordon R.D., Shaw Jr. B.W., Iwatsuki S., Esquivel C.O., and Starzl T.E. Indications for liver transplantation in the cyclosporine era. Surg Clin North Am 66 (1986) 541-556
35. Goto M., Masuda S., Saito H., Uemoto S., Kiuchi T., Tanaka K., et al. C3435T polymorphism in the MDR1 gene affects the enterocyte expression level of CYP3A4 rather than Pgp in recipients of living-donor liver transplantation. Pharmacogenetics 12 (2002) 451-457
36. Goto M., Masuda S., Saito H., and Inui K. Decreased expression of P-glycoprotein during differentiation in the human intestinal cell line Caco-2. Biochem Pharmacol 66 (2003) 163-170
37. *1-carrying graft liver reduces the concentration/oral dose ratio of tacrolimus in recipients of living-donor liver transplantation. Pharmacogenetics 14 (2004) 471-478
38. Gottesman M.M., Fojo T., and Bates S.E. Multidrug resistance in cancer: role of ATP-dependent transporters. Nat Rev Cancer 2 (2002) 48-58
39. Greiner B., Eichelbaum M., Fritz P., Kreichgauer H.P., von Richter O., Zundler J., et al. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest 104 (1999) 147-153
40. Grevel J. Area-under-the-curve versus trough level monitoring of cyclosporine concentration: critical assessment of dosage adjustment practices and measurement of clinical outcome. Ther Drug Monit 15 (1993) 488-491
41. Grevel J., Post B.K., and Kahan B.D. Michaelis-Menten kinetics determine cyclosporine steady-state concentrations: a population analysis in kidney transplant patients. Clin Pharmacol Ther 53 (1993) 651-660
42. Halloran P.F., Helms L.M., Kung L., and Noujaim J. The temporal profile of calcineurin inhibition by cyclosporine in vivo. Transplantation 68 (1999) 1356-1361
43. Hashida T., Masuda S., Uemoto S., Saito H., Tanaka K., and Inui K. Pharmacokinetic and prognostic significance of intestinal MDR1 expression in recipients of living-donor liver transplantation. Clin Pharmacol Ther 69 (2001) 308-316
44. Hashimoto Y., Sasa H., Shimomura M., and Inui K. Effects of intestinal and hepatic metabolism on the bioavailability of tacrolimus in rats. Pharm Res 15 (1998) 1609-1613
45. Haufroid V., Mourad M., Van Kerckhove V., Wawrzyniak J., De Meyer M., Eddour D.C., et al. The effect of CYP3A5 and MDR1 (ABCB1) polymorphisms on cyclosporine and tacrolimus dose requirements and trough blood levels in stable renal transplant patients. Pharmacogenetics 14 (2004) 147-154
46. Hauser I.A., Schaeffeler E., Gauer S., Scheuermann E.H., Wegner B., Gossmann J., et al. ABCB1 genotype of the donor but not of the recipient is a major risk factor for cyclosporine-related nephrotoxicity after renal transplantation. J Am Soc Nephrol 16 (2005) 1501-1511
47. He P., Court M.H., Greenblatt D.J., and Von Moltke L.L. Genotype-phenotype associations of cytochrome P450 3A4 and 3A5 polymorphism with midazolam clearance in vivo. Clin Pharmacol Ther 77 (2005) 373-387
48. Hebert M.F. Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Adv Drug Deliv Rev 27 (1997) 201-214
49. Hebert M.F., Fisher R.M., Marsh C.L., Dressler D., and Bekersky I. Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers. J Clin Pharmacol 39 (1999) 91-96
50. Hesselink D.A., van Schaik R.H., van der Heiden I.P., van der Werf M., Gregoor P.J., Lindemans J., et al. Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus. Clin Pharmacol Ther 74 (2003) 245-254
51. Hesselink D.A., van Gelder T., van Schaik R.H., Balk A.H., van der Heiden I.P., van Dam T., et al. Population pharmacokinetics of cyclosporine in kidney and heart transplant recipients and the influence of ethnicity and genetic polymorphisms in the MDR-1, CYP3A4, and CYP3A5 genes. Clin Pharmacol Ther 76 (2004) 545-556
52. Hoffmeyer S., Burk O., von Richter O., Arnold H.P., Brockmoller J., Johne A., et al. Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo. Proc Natl Acad Sci USA 97 (2000) 3473-3478
53. Homma M., Tomita T., Yuzawa K., Takada Y., and Kohda Y. False positive blood tacrolimus concentration in microparticle enzyme immunoassay. Biol Pharm Bull 25 (2002) 1119-1120
54. Hustert E., Haberl M., Burk O., Wolbold R., He Y.Q., Klein K., et al. The genetic determinants of the CYP3A5 polymorphism. Pharmacogenetics 11 (2001) 773-779
55. Inomata Y., Kiuchi T., Kim I., Uemoto S., Egawa H., Asonuma K., et al. Auxiliary partial orthotopic living donor liver transplantation as an aid for small-for-size grafts in larger recipients. Transplantation 67 (1999) 1314-1319
56. Inui K., Masuda S., and Saito H. Cellular and molecular aspects of drug transport in the kidney. Kidney Int 58 (2000) 944-958
57. Ishikawa T., Tsuji A., Inui K., Sai Y., Anzai N., Wada M., et al. The genetic polymorphism of drug transporters: functional analysis approaches. Pharmacogenomics 5 (2004) 67-99
58. Jusko W.J. Analysis of tacrolimus (FK 506) in relation to therapeutic drug monitoring. Ther Drug Monit 17 (1995) 596-601
59. Jusko W.J., Piekoszewski W., Klintmalm G.B., Shaefer M.S., Hebert M.F., Piergies A.A., et al. Pharmacokinetics of tacrolimus in liver transplant patients. Clin Pharmacol Ther 57 (1995) 281-290
60. Kamdem L.K., Streit F., Zanger U.M., Brockmoller J., Oellerich M., Armstrong V.W., et al. Contribution of CYP3A5 to the in vitro hepatic clearance of tacrolimus. Clin Chem 51 (2005) 1374-1381
61. Kaplan B., Lown K., Craig R., Abecassis M., Kaufman D., Leventhal J., et al. Low bioavailability of cyclosporine microemulsion and tacrolimus in a small bowel transplant recipient: possible relationship to intestinal P-glycoprotein activity. Transplantation 67 (1999) 333-335
62. Kawasaki S., Makuuchi M., Ishizone S., Matsunami H., Terada M., and Kawarazaki H. Liver regeneration in recipients and donors after transplantation. Lancet 339 (1992) 580-581
63. Kelly D., Jara P., Rodeck B., Lykavieris P., Burdelski M., Becker M., et al. Tacrolimus and steroids versus ciclosporin microemulsion, steroids, and azathioprine in children undergoing liver transplantation: randomised European multicentre trial. Lancet 364 (2004) 1054-1061
64. Kershner R.P., and Fitzsimmons W.E. Relationship of FK506 whole blood concentrations and efficacy and toxicity after liver and kidney transplantation. Transplantation 62 (1996) 920-926
65. Kim R.B., Leake B.F., Choo E.F., Dresser G.K., Kubba S.V., Schwarz U.I., et al. Identification of functionally variant MDR1 alleles among European Americans and African Americans. Clin Pharmacol Ther 70 (2001) 189-199
66. Kimchi-Sarfaty C., Gribar J.J., and Gottesman M.M. Functional characterization of coding polymorphisms in the human MDR1 gene using a vaccinia virus expression system. Mol Pharmacol 62 (2002) 1-6
67. Kiuchi T., Inomata Y., Uemoto S., Satomura K., Egawa H., Okajima H., et al. A hepatic graft tuberculosis transmitted from a living-related donor. Transplantation 63 (1997) 905-907
68. Kivisto K.T., Niemi M., and Fromm M.F. Functional interaction of intestinal CYP3A4 and P-glycoprotein. Fundam Clin Pharmacol 18 (2004) 621-626
69. Kokado Y., Takahara S., Kyo M., Ichimaru N., Toki K., Wang J.D., et al. Low-dose tacrolimus (FK 506)-based immunosuppressive protocol in living donor renal transplantation. Transplant Proc 31 (1999) 1151-1154
70. Kuehl P., Zhang J., Lin Y., Lamba J., Assem M., Schuetz J., et al. Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression. Nat Genet 27 (2001) 383-391
71. Kurokawa N., Kadobayashi M., Yamamoto K., Arakawa Y., Sawada M., Takahara S., et al. In-vivo distribution and erythrocyte binding characteristics of cyclosporin in renal transplant patients. J Pharm Pharmacol 48 (1996) 553-559
72. Lazzaro C., McKechnie T., and McKenna M. Tacrolimus versus cyclosporin in renal transplantation in Italy: cost-minimisation and cost-effectiveness analyses. J Nephrol 15 (2002) 580-588
73. Levy G. Neoral/cyclosporine-based immunosuppression. Liver Transpl Surg 5 (1999) S37-S47
74. Levy G. C2 monitoring strategy for optimising cyclosporin immunosuppression from the Neoral formulation. BioDrugs 15 (2001) 279-290
75. 0 monitoring in de novo liver transplantation. Transplantation 77 (2004) 1632-1638
76. Li A.P., Kaminski D.L., and Rasmussen A. Substrates of human hepatic cytochrome P450 3A4. Toxicology 104 (1995) 1-8
77. Lin J.H., and Yamazaki M. Role of P-glycoprotein in pharmacokinetics: clinical implications. Clin Pharmacokinet 42 (2003) 59-98
78. Lopez-Montes A., Gallego E., Lopez E., Perez J., Lorenzo I., Llamas F., et al. Treatment of tuberculosis with rifabutin in a renal transplant recipient. Am J Kidney Dis 44 (2004) e59-e63
79. Lown K.S., Mayo R.R., Leichtman A.B., Hsiao H.L., Turgeon D.K., Schmiedlin-Ren P., et al. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther 62 (1997) 248-260
80. Macphee I.A., Fredericks S., Tai T., Syrris P., Carter N.D., Johnston A., et al. Tacrolimus pharmacogenetics: polymorphisms associated with expression of cytochrome p4503A5 and P-glycoprotein correlate with dose requirement. Transplantation 74 (2002) 1486-1489
81. MacPhee I.A., Fredericks S., Tai T., Syrris P., Carter N.D., Johnston A., et al. The influence of pharmacogenetics on the time to achieve target tacrolimus concentrations after kidney transplantation. Am J Transplant 4 (2004) 914-919
82. *1 allele predicts low dose-normalized tacrolimus blood concentrations in whites and South Asians. Transplantation 79 (2005) 499-502
83. Maglich J.M., Stoltz C.M., Goodwin B., Hawkins-Brown D., Moore J.T., and Kliewer S.A. Nuclear pregnane x receptor and constitutive androstane receptor regulate overlapping but distinct sets of genes involved in xenobiotic detoxification. Mol Pharmacol 62 (2002) 638-646
84. Margreiter R. Efficacy and safety of tacrolimus compared with ciclosporin microemulsion in renal transplantation: a randomised multicentre study. Lancet 359 (2002) 741-746
85. Martin S.R., Atkison P., Anand R., and Lindblad A.S. Studies of pediatric liver transplantation 2002: patient and graft survival and rejection in pediatric recipients of a first liver transplant in the United States and Canada. Pediatr Transplant 8 (2004) 273-283
86. Masuda S., Uemoto S., Hashida T., Inomata Y., Tanaka K., and Inui K. Effect of intestinal P-glycoprotein on daily tacrolimus trough level in a living-donor small bowel recipient. Clin Pharmacol Ther 68 (2000) 98-103
87. Masuda S., Goto M., Kiuchi T., Uemoto S., Kodawara T., Saito H., et al. Enhanced expression of enterocyte P-glycoprotein depresses cyclosporine bioavailability in a recipient of living donor liver transplantation. Liver Transpl 9 (2003) 1108-1113
88. Masuda S., Uemoto S., Goto M., Fujimoto Y., Tanaka K., and Inui K. Tacrolimus therapy according to mucosal MDR1 levels in small-bowel transplant recipients. Clin Pharmacol Ther 75 (2004) 352-361
89. Masuda S., Goto M., Okuda M., Ogura Y., Oike F., Kiuchi T., et al. Initial dosage adjustment for oral administration of tacrolimus using the intestinal MDR1 level in living-donor liver transplant recipients. Transplant Proc 37 (2005) 1728-1729
90. Masuda S., Goto M., Fukatsu S., Uesugi M., Ogura Y., Oike F., et al. Intestinal, M.D.R1/ABCB1 level at surgery as a risk factor of acute cellular rejection in living-donor liver transplant patients. Clin Pharmacol Ther 79 (2006) 90-102
91. McBride J.H., Kim S.S., Rodgerson D.O., Reyes A.F., and Ota M.K. Measurement of cyclosporine by liquid chromatography and three immunoassays in blood from liver, cardiac, and renal transplant recipients. Clin Chem 38 (1992) 2300-2306
92. McDiarmid S.V., Busuttil R.W., Ascher N.L., Burdick J., D'Alessandro A.M., Esquivel C., et al. FK506 (tacrolimus) compared with cyclosporine for primary immunosuppression after pediatric liver transplantation. Results from the U.S. Multicenter Trial. Transplantation 59 (1995) 530-536
93. McMaster P. Patient and graft survival in the European Multicentre Liver Study-FK 506 vs. cyclosporin A. Transpl Int 7 Suppl 1 (1994) S32-S36
94. Min D.I., and Ellingrod V.L. C3435T mutation in exon 26 of the human MDR1 gene and cyclosporine pharmacokinetics in healthy subjects. Ther Drug Monit 24 (2002) 400-404
95. Morris R.G., Russ G.R., Cervelli M.J., Juneja R., McDonald S.P., and Mathew T.H. Comparison of trough, 2-hour, and limited AUC blood sampling for monitoring cyclosporin (Neoral) at day 7 post-renal transplantation and incidence of rejection in the first month. Ther Drug Monit 24 (2002) 479-486
96. Morita N., Yasumori T., and Nakayama K. Human MDR1 polymorphism: G2677T/A and C3435T have no effect on MDR1 transport activities. Biochem Pharmacol 65 (2003) 1843-1852
97. Mourad M., Mourad G., Wallemacq P., Garrigue V., Van Bellingen C., Van Kerckhove V., et al. Sirolimus and tacrolimus trough concentrations and dose requirements after kidney transplantation in relation to CYP3A5 and MDR1 polymorphisms and steroids. Transplantation 80 (2005) 977-984
98. Nagase K., Iwasaki K., Nozaki K., and Noda K. Distribution and protein binding of FK506, a potent immunosuppressive macrolide lactone, in human blood and its uptake by erythrocytes. J Pharm Pharmacol 46 (1994) 113-117
99. Nakamura T., Sakaeda T., Horinouchi M., Tamura T., Aoyama N., Shirakawa T., et al. Effect of the mutation (C3435T) at exon 26 of the MDR1 gene on expression level of MDR1 messenger ribonucleic acid in duodenal enterocytes of healthy Japanese subjects. Clin Pharmacol Ther 71 (2002) 297-303
100. Nashan B., Bock A., Bosmans J.L., Budde K., Fijter H., Jaques B., et al. Use of Neoral C monitoring: a European consensus. Transpl Int 18 (2005) 768-778
101. O'Grady J.G., Burroughs A., Hardy P., Elbourne D., and Truesdale A. Tacrolimus versus microemulsified ciclosporin in liver transplantation: the TMC randomised controlled trial. Lancet 360 (2002) 1119-1125
102. Omae T., Goto M., Shimomura M., Masuda S.K.I., Okuda M., and Inui K. Transient up-regulation of P-glycoprotein reduces tacrolimus absorption after ischemia-reperfusion injury in rat ileum. Biochem Pharmacol 69 (2005) 560-567
103. Ormonde D.G., de Boer W.B., Kierath A., Bell R., Shilkin K.B., House A.K., et al. Banff schema for grading liver allograft rejection: utility in clinical practice. Liver Transpl Surg 5 (1999) 261-268
104. Otte J.B. History of pediatric liver transplantation. Where are we coming from? Where do we stand?. Pediatr Transplant 6 (2002) 378-387
105. Pascussi J.M., Drocourt L., Gerbal-Chaloin S., Fabre J.M., Maurel P., and Vilarem M.J. Dual effect of dexamethasone on CYP3A4 gene expression in human hepatocytes. Sequential role of glucocorticoid receptor and pregnane X receptor. Eur J Biochem 268 (2001) 6346-6358
106. Pascussi J.M., Gerbal-Chaloin S., Drocourt L., Maurel P., and Vilarem M.J. The expression of CYP2B6, CYP2C9 and CYP3A4 genes: a tangle of networks of nuclear and steroid receptors. Biochim Biophys Acta 1619 (2003) 243-253
107. Ptachcinski R.J., Venkataramanan R., and Burckart G.J. Clinical pharmacokinetics of cyclosporin. Clin Pharmacokinet 11 (1986) 107-132
108. Rousseau A., Leger F., Le Meur Y., Saint-Marcoux F., Paintaud G., Buchler M., et al. Population pharmacokinetic modeling of oral cyclosporin using NONMEM: comparison of absorption pharmacokinetic models and design of a Bayesian estimator. Ther Drug Monit 26 (2004) 23-30
109. Schinkel A.H. P-Glycoprotein, a gatekeeper in the blood-brain barrier. Adv Drug Deliv Rev 36 (1999) 179-194
110. Schinkel A.H., and Jonker J.W. Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview. Adv Drug Deliv Rev 55 (2003) 3-29
111. Scholten E.M., Cremers S.C., Schoemaker R.C., Rowshani A.T., van Kan E.J., den Hartigh J., et al. AUC-guided dosing of tacrolimus prevents progressive systemic overexposure in renal transplant recipients. Kidney Int 67 (2005) 2440-2447
112. Shimomura M., Masuda S., Saito H., Sakamoto S., Uemoto S., Tanaka K., et al. Roles of the jejunum and ileum in the first-pass effect as absorptive barriers for orally administered tacrolimus. J Surg Res 103 (2002) 215-222
113. Siegsmund M., Brinkmann U., Schaffeler E., Weirich G., Schwab M., Eichelbaum M., et al. Association of the P-glycoprotein transporter MDR1(C3435T) polymorphism with the susceptibility to renal epithelial tumors. J Am Soc Nephrol 13 (2002) 1847-1854
114. Singh D., Alexander J., Owen A., Rustom R., Bone M., Hammad A., et al. Whole-blood cultures from renal-transplant patients stimulated ex vivo show that the effects of cyclosporine on lymphocyte proliferation are related to P-glycoprotein expression. Transplantation 77 (2004) 557-561
115. Staatz C.E., Taylor P.J., Lynch S.V., Willis C., Charles B.G., and Tett S.E. Population pharmacokinetics of tacrolimus in children who receive cut-down or full liver transplants. Transplantation 72 (2001) 1056-1061
116. Staatz C.E., Willis C., Taylor P.J., and Tett S.E. Population pharmacokinetics of tacrolimus in adult kidney transplant recipients. Clin Pharmacol Ther 72 (2002) 660-669
117. Starzl T.E., Iwatsuki S., Van Thiel D.H., Gartner J.C., Zitelli B.J., Malatack J.J., et al. Evolution of liver transplantation. Hepatology 2 (1982) 614-636
118. Stefoni S., Midtved K., Cole E., Thervet E., Cockfield S., Buchler M., et al. Efficacy and safety outcomes among de novo renal transplant recipients managed by C2 monitoring of cyclosporine a microemulsion: results of a 12-month, randomized, multicenter study. Transplantation 79 (2005) 577-583
119. Takano M., Yumoto R., and Murakami T. Expression and function of efflux drug transporters in the intestine. Pharmacol Ther 109 (2006) 137-161
120. Tanabe M., Ieiri I., Nagata N., Inoue K., Ito S., Kanamori Y., et al. Expression of P-glycoprotein in human placenta: relation to genetic polymorphism of the multidrug resistance (MDR)-1 gene. J Pharmacol Exp Ther 297 (2001) 1137-1143
121. Tanaka K., Uemoto S., Tokunaga Y., Fujita S., Sano K., Yamamoto E., et al. Living related liver transplantation in children. Am J Surg 168 (1994) 41-48
122. Tanaka K., Lake J., Villamil F., Levy G., Marotta P., Mies S., et al. Comparison of cyclosporine microemulsion and tacrolimus in 39 recipients of living donor liver transplantation. Liver Transpl 11 (2005) 1395-1402
123. Thervet E., Pfeffer P., Scolari M.P., Toselli L., Pallardo L.M., Chadban S., et al. Clinical outcomes during the first three months posttransplant in renal allograft recipients managed by C2 monitoring of cyclosporine microemulsion. Transplantation 76 (2003) 903-908
124. Thervet E., Legendre C., Beaune P., and Anglicheau D. Cytochrome P450 3A polymorphisms and immunosuppressive drugs. Pharmacogenomics 6 (2005) 37-47
125. Todo S., Tzakis A., Reyes J., Abu-Elmagd K., Casavilla A., Nour B.M., et al. Clinical small bowel or small bowel plus liver transplantation under FK 506. Transplant Proc 23 (1991) 3093-3095
126. Todo S., Tzakis A.G., Abu-Elmagd K., Reyes J., Nakamura K., Casavilla A., et al. Intestinal transplantation in composite visceral grafts or alone. Ann Surg 216 (1992) 223-233
127. Tsuchiya N., Satoh S., Tada H., Li Z., Ohyama C., Sato K., et al. Influence of CYP3A5 and MDR1 (ABCB1) polymorphisms on the pharmacokinetics of tacrolimus in renal transplant recipients. Transplantation 78 (2004) 1182-1187
128. Tzakis A., Todo S., and Starzl T. Intestinal transplantation. Annu Rev Med 45 (1994) 79-91
129. Uesugi M., Masuda S., Katsura T., Oike F., Takada Y., and Inui K. Effect of intestinal CYP3A5 on postoperative tacrolimus trough levels in living-donor liver transplant recipients. Pharmacogenet Genomics 16 (2006) 119-127
130. Uwai Y., Masuda S., Goto M., Motohashi H., Saito H., Okuda M., et al. Common single nucleotide polymorphisms of the MDR1 gene have no influence on its mRNA expression level of normal kidney cortex and renal cell carcinoma in Japanese nephrectomized patients. J Hum Genet 49 (2004) 40-45
131. Venkataramanan R., Jain A., Warty V.W., Abu E.K., Furakawa H., Imventarza O., et al. Pharmacokinetics of FK 506 following oral administration: a comparison of FK 506 and cyclosporine. Transplant Proc 23 (1991) 931-933
132. Venkataramanan R., Swaminathan A., Prasad T., Jain A., Zuckerman S., Warty V., et al. Clinical pharmacokinetics of tacrolimus. Clin Pharmacokinet 29 (1995) 404-430
133. von Ahsen N., Richter M., Grupp C., Ringe B., Oellerich M., and Armstrong V.W. No influence of the MDR-1 C3435T polymorphism or a CYP3A4 promoter polymorphism (CYP3A4-V allele) on dose-adjusted cyclosporin A trough concentrations or rejection incidence in stable renal transplant recipients. Clin Chem 47 (2001) 1048-1052
134. Wasik M., Stepien-Sopniewska B., Lagodzinski Z., and Gorski A. Effect of FK-506 and cyclosporine on human T and B lymphoproliferative responses. Immunopharmacology 20 (1990) 57-61
135. Westphal K., Weinbrenner A., Zschiesche M., Franke G., Knoke M., Oertel R., et al. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Clin Pharmacol Ther 68 (2000) 345-355
136. Wiederrecht G., Lam E., Hung S., Martin M., and Sigal N. The mechanism of action of FK-506 and cyclosporin A. Ann N Y Acad Sci 696 (1993) 9-19
137. Williams J.A., Ring B.J., Cantrell V.E., Jones D.R., Eckstein J., Ruterbories K., et al. Comparative metabolic capabilities of CYP3A4, CYP3A5, and CYP3A7. Drug Metab Dispos 30 (2002) 883-891
138. Williams J.A., Cook J., and Hurst S.I. A significant drug-metabolizing role for CYP3A5?. Drug Metab Dispos 31 (2003) 1526-1530
139. Xu X., Su B., Barndt R.J., Chen H., Xin H., Yan G., et al. FKBP12 is the only FK506 binding protein mediating T-cell inhibition by the immunosuppressant FK506. Transplantation 73 (2002) 1835-1838
140. Yasuhara M., Hashida T., Toraguchi M., Hashimoto Y., Kimura M., Inui K., et al. Pharmacokinetics and pharmacodynamics of FK 506 in pediatric patients receiving living-related donor liver transplantations. Transplant Proc 27 (1995) 1108-1110
141. Zhang Y., and Benet L.Z. The gut as a barrier to drug absorption: combined role of cytochrome P450 3A and P-glycoprotein. Clin Pharmacokinet 40 (2001) 159-168
142. Zhang X., Liu Z.H., Zheng J.M., Chen Z.H., Tang Z., Chen J.S., et al. Influence of CYP3A5 and MDR1 polymorphisms on tacrolimus concentration in the early stage after renal transplantation. Clin Transplant 19 (2005) 638-643
143. Zhao J.Y., Ikeguchi M., Eckersberg T., and Kuo M.T. Modulation of multidrug resistance gene expression by dexamethasone in cultured hepatoma cells. Endocrinology 133 (1993) 521-528
144. Zheng H., Webber S., Zeevi A., Schuetz E., Zhang J., Bowman P., et al. Tacrolimus dosing in pediatric heart transplant patients is related to CYP3A5 and MDR1 gene polymorphisms. Am J Transplant 3 (2003) 477-483
145. Zucchelli G.C., Pilo A., Chiesa M.R., Scarlattini M., and Bizollon C.A. Progress report of an external quality assessment scheme for cyclosporine assay. Ther Drug Monit 18 (1996) 273-279