A randomized, crossover pharmacokinetic study comparing generic tacrolimus vs. the reference formulation in subpopulations of kidney transplant patients

Clinical Transplantation

Volumn 27, Issue 6, 2013, Pages

  Bloom, R D ^a   Trofe Clark, J ^a,b   Wiland, A ^c   Alloway, R R ^d  

^a UNIVERSITY OF PENNSYLVANIA   (United States)

^b HOSPITAL OF THE UNIVERSITY OF PENNSYLVANIA   (United States)

^c NOVARTIS PHARMA AG   (Switzerland)

^d UNIVERSITY OF CINCINNATI   (United States)

Author keywords

African American; Bioequivalence; Diabetes; Generic; Hecoria; Pharmacokinetic; Prograf; Sandoz; Tacrolimus

Indexed keywords

GENERIC DRUG; MYCOPHENOLIC ACID; STEROID; TACROLIMUS;

ADULT; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG FORMULATION; FEMALE; HUMAN; KIDNEY GRAFT REJECTION; KIDNEY TRANSPLANTATION; MAJOR CLINICAL STUDY; MALE; MULTICENTER STUDY; POST HOC ANALYSIS; PRIORITY JOURNAL; PROSPECTIVE STUDY; RANDOMIZED CONTROLLED TRIAL; REFERENCE VALUE;

AFRICAN AMERICAN; BIOEQUIVALENCE; DIABETES; GENERIC; HECORIA; PHARMACOKINETIC; PROGRAF; SANDOZ; TACROLIMUS;

AREA UNDER CURVE; CROSS-OVER STUDIES; DRUGS, GENERIC; FEMALE; FOLLOW-UP STUDIES; HUMANS; IMMUNOSUPPRESSIVE AGENTS; KIDNEY; KIDNEY TRANSPLANTATION; MALE; MIDDLE AGED; PROGNOSIS; PROSPECTIVE STUDIES; TACROLIMUS; THERAPEUTIC EQUIVALENCY; TISSUE DISTRIBUTION;

EID: 84889099740     PISSN: 09020063     EISSN: 13990012     Source Type: Journal    
DOI: 10.1111/ctr.12256     Document Type: Article

References (45)

1. Wallemacq P, Armstrong VW, Brunet M et al. Opportunities to optimize tacrolimus therapy in solid organ transplantation: report of the European consensus conference. Ther Drug Monit 2009: 31: 139.
2. Staatz CE, Tett SE. Clinical pharmacokinetics and pharmacodynamics of tacrolimus in solid organ transplantation. Clin Pharmacokinet 2004: 43: 623.
3. Bekersky I, Dressler D, Mekki QA. Effect of low- and high-fat meals on tacrolimus absorption following 5 mg single oral doses to healthy human subjects. J Clin Pharmacol 2001: 41: 176.
4. Lainesse A, Hussain S, Monif T et al. Bioequivalence studies of tacrolimus capsule under fasting and fed conditions in healthy male and female subjects. Arzneimittelforschung 2008: 58: 242.
5. Lemahieu W, Maes B, Verbeke K, Rutgeerts P, Geboes K, Vanrenterghem Y. Cytochrome P450 3A4 and P-glycoprotein activity and assimilation of tacrolimus in transplant patients with persistent diarrhea. Am J Transplant 2005: 5: 1383.
6. Kuypers DR, Claes K, Evenepoel P et al. Time-related clinical determinants of long-term tacrolimus pharmacokinetics in combination therapy with mycophenolic acid and corticosteroids: a prospective study in one hundred de novo renal transplant recipients. Clin Pharmacokinet 2004: 43: 741.
7. Undre NA, Schäfer A. Factors affecting the pharmacokinetics of tacrolimus in the first year after renal transplantation. European Tacrolimus Multicentre Renal Study Group. Transplant Proc 1998: 30: 1261.
8. Park SI, Felipe CR, Pinheiro-Machado PG et al. Tacrolimus pharmacokinetic drug interactions: effect of prednisone, mycophenolic acid or sirolimus. Fundam Clin Pharmacol 2009: 23: 137.
9. Bekersky I, Dressler D, Alak A, Boswell GW, Mekki QA. Comparative tacrolimus pharmacokinetics: normal versus mildly hepatically impaired subjects. J Clin Pharmacol 2001: 41: 628.
10. Macphee IA, Fredericks S, Tai T et al. Tacrolimus pharmacogenetics: polymorphisms associated with expression of cytochrome p4503A5 and P-glycoprotein correlate with dose requirement. Transplantation 2002: 74: 1486.
11. Santoro AB, Struchiner CJ, Felipe CR, Tedesco-Silva H, Medina-Pestana JO, Suarez-Kurtz G. CYP3A5 genotype, but not CYP3A4*1b, CYP3A4*22, or hematocrit, predicts tacrolimus dose requirements in Brazilian renal transplant patients. Clin Pharmacol Ther 2013: 94: 201.
12. Yoon SH, Cho JH, Kwon O et al. CYP3A and ABCB1 genetic polymorphisms on the pharmacokinetics and pharmacodynamics of tacrolimus and its metabolites (M-I and M-III). Transplantation 2013: 95: 828.
13. Felipe CR, Silva HT, Machado PG, Garcia R, Da Silva Moreira SR, Pestana JO. The impact of ethnic miscegenation on tacrolimus clinical pharmacokinetics and therapeutic drug monitoring. Clin Transplant 2002: 16: 262.
14. Neylan JF. Racial differences in renal transplantation after immunosuppression with tacrolimus versus cyclosporine. FK506 Kidney Transplant Study Group. Transplantation 1998: 65: 515.
15. Mancinelli LM, Frassetto L, Floren LC et al. The pharmacokinetics and metabolic disposition of tacrolimus: a comparison across ethnic groups. Clin Pharmacol Ther 2001: 69: 24.
16. Mendonza AE, Zahir H, Gohh RY, Akhlaghi F. Tacrolimus in diabetic kidney transplant recipients: pharmacokinetics and application of a limited sampling strategy. Ther Drug Monit 2007: 29: 391.
17. Hu RH, Lee PH, Tsai MK. Clinical influencing factors for daily dose, trough level, and relative clearance of tacrolimus in renal transplant recipients. Transplant Proc 2000: 32: 1689.
18. Velicković-Radovanović R, Mikov M, Paunović G et al. Gender differences in pharmacokinetics of tacrolimus and their clinical significance in kidney transplant recipients. Gend Med 2011: 8: 23.
19. Van Duijnhoven EM, Boots JM, Christiaans MH, Stolk LM, Undre NA, Van Hooff JP. Increase in tacrolimus trough levels after steroid withdrawal. Transpl Int 2003: 16: 721.
20. Van Gelder T. Drug interactions with tacrolimus. Drug Saf 2002: 25: 707.
21. Antignac M, Barrou B, Farinotti R, Lechat P, Urien S. Population pharmacokinetics and bioavailability of tacrolimus in kidney transplant patients. Br J Clin Pharmacol 2007: 64: 750.
22. Kim JS, Aviles DH, Silverstein DM, Leblanc PL, Matti Vehaskari V. Effect of age, ethnicity, and glucocorticoid use on tacrolimus pharmacokinetics in pediatric renal transplant patients. Pediatr Transplant 2005: 9: 162.
23. Pascual J, Del Castillo D, Cabello M et al. Interaction between everolimus and tacrolimus in renal transplant recipients: a pharmacokinetic controlled trial. Transplantation 2010: 89: 994.
24. Kershner RP, Fitzsimmons WE. Relationship of FK506 whole blood concentrations and efficacy and toxicity after liver and kidney transplantation. Transplantation 1996: 62: 920.
25. Mathew P, Mandal J, Patel K et al. Bioequivalence of two tacrolimus formulations under fasting conditions in healthy male subjects. Clin Ther 2011: 33: 1105.
26. Park K, Kim YS, Kwon KI, Park MS, Lee YJ, Kim KH. A randomized, open-label, two-period, crossover bioavailability study of two oral formulations of tacrolimus in healthy Korean adults. Clin Ther 2007: 29: 154.
27. Food and Drug Administration (FDA). Bioavailability and bioequivalence requirements. Fed Regist 1992: 57: 17997.
28. European Medicines Agency. Guideline on the Investigation of Bioequivalence. CPMP/EWP/QWP/1401/98 Rev. 1/Corr, January 20, 2010. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf (Accessed December 2011).
29. Trofe-Clark J, Gabardi S, Mcdevitt-Potter L, Alloway RR. Immunosuppression, generic drugs and the FDA. Am J Transplant 2012: 12: 792.
30. ®): Prescribing Information. Deerfield, IL, USA: Astellas Pharma US, Inc. Revised September 2011. Available at: http://www.astellas.us/docs/prograf.pdf
31. Anglicheau D, Flamant M, Schlageter MH et al. Pharmacokinetic interaction between corticosteroids and tacrolimus after renal transplantation. Nephrol Dial Transplant 2003: 18: 2409.
32. Baldan N, Rigotti P, Furian L et al. Co-administration of sirolimus alters tacrolimus pharmacokinetics in a dose-dependent manner in adult renal transplant recipients. Pharmacol Res 2006: 54: 181.
33. Alloway RA, Isaacs R, Lake K et al. Report of the American Society of Transplantation Conference on immunosuppressive drugs and the use of generic immunosuppressants. Am J Transplant 2003: 3: 1211.
34. Alloway RR, Sadaka B, Trofe-Clark J, Wiland A, Bloom RD. A randomized pharmacokinetic study of generic tacrolimus versus reference tacrolimus in kidney transplant recipients. Am J Transplant 2012: 12: 2825.
35. Poggio ED, Wang X, Weinstein DM et al. Assessing glomerular filtration rate by estimation equations in kidney transplant recipients. Am J Transplant 2006: 6: 100.
36. Venkataramanan R, Swaminathan A, Prasad T et al. Clinical pharmacokinetics of tacrolimus. Clin Pharmacokinet 1995: 29: 404.
37. Wong KM, Shek CC, Chau KF, Li CS. Abbreviated tacrolimus area-under-the-curve monitoring for renal transplant recipients. Am J Kidney Dis 2000: 35: 660.
38. Ihara H, Shinkuma D, Ichikawa Y, Nojima M, Nagano S, Ikoma F. Intra- and inter-individual variation in the pharmacokinetics of tacrolimus (FK506) in kidney transplant recipients-importance of trough level as a practical indicator. Int J Urol 1995: 2: 151.
39. Fitzsimmons WE, Bekersky I, Dressler D, Raye K, Hodosh E, Mekki Q. Demographic considerations in tacrolimus pharmacokinetics. Transplant Proc 1998: 30: 1359.
40. Renton KW, Crocker JF, Mclellan H, Acott PD. A comparison of the pharmacokinetics of tacrolimus and microemulsified cyclosporin in paediatric renal transplant recipients. Eur J Clin Pharmacol 2004: 60: 421.
41. Shihab FS, Lee ST, Smith LD et al. Effect of corticosteroid withdrawal on tacrolimus and mycophenolate mofetil exposure in a randomized multicenter study. Am J Transplant 2013: 13: 474.
42. Horowitz M, Su YC, Rayner CK, Jones KL. Gastroparesis: prevalence, clinical significance and treatment. Can J Gastroenterol 2001: 15: 805.
43. Anger GJ, Cressman AM, Piquette-Miller M. Expression of ABC efflux transporters in placenta for women with insulin-managed diabetes. PLoS ONE 2012: 7: e35027.
44. Jacobson PA, Oetting WS, Brearley AM, et al. DeKAF Investigators. Novel polymorphisms associated with tacrolimus trough concentrations: results from a multicenter kidney transplant consortium. Transplantation 2011: 91: 300.
45. Park SI, Felipe CR, Pinheiro-Machado PG, Garcia R, Tedesco-Silva HJR, Medina-Pestana JO. Circadian and time-dependent variability in tacrolimus pharmacokinetics. Fundam Clin Pharmacol 2007: 21: 191.