A randomized, open-label, two-period, crossover bioavailability study of two oral formulations of tacrolimus in healthy Korean adults

Clinical Therapeutics

Volumn 29, Issue 1, 2007, Pages 154-162

  Park, Kyungsoo ^a   Kim, Yu Seun ^a   Kwon, Kwang il ^b   Park, Min Soo ^a   Lee, Yoon Jung ^a   Kim, Kyung Hwan ^a  

^a Yonsei University College of Medicine   (South Korea)

^b Chungnam National University   (South Korea)

Author keywords

bioequivalence; oral formulation; pharmacokinetics; tacrolimus

Indexed keywords

TACROLIMUS;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; BLOOD SAMPLING; CLINICAL PRACTICE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; COUGHING; CROSSOVER PROCEDURE; DIARRHEA; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG EXPOSURE; DRUG FORMULATION; DRUG HALF LIFE; DRUG TOLERABILITY; FATIGUE; FEMALE; HEADACHE; HUMAN; HUMAN EXPERIMENT; INDIGESTION; KOREA; MALE; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CAPSULES; CHROMATOGRAPHY, LIQUID; CIRCADIAN RHYTHM; CROSS-OVER STUDIES; FEMALE; HALF-LIFE; HUMANS; IMMUNOSUPPRESSIVE AGENTS; KOREA; MIDDLE AGED; REPRODUCIBILITY OF RESULTS; TACROLIMUS; TANDEM MASS SPECTROMETRY; THERAPEUTIC EQUIVALENCY;

EID: 33947166897     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2007.01.016     Document Type: Article

References (34)

1. First M.R., and Fitzsimmons W.E. Modified released tacrolimus. Yonsei Med J 45 (2004) 1127-1131
2. Spencer C.M., Goa K.L., and Gillis J.C. Tacrolimus: An update of its pharmacology and clinical efficacy in the management of organ transplantation. Drugs 54 (1997) 925-975
3. Calne R.Y. Cyclosporine and liver transplantation. Mt Sinai J Med 54 (1987) 465-466
4. Gordon R.D., Shaw Jr. B.W., Iwatsuki S., et al. Indications for liver transplantation in the cyclosporine era. Surg Clin North Am 66 (1986) 541-556
5. Scott L.J., McKeage K., Keam S.J., and Plosker G.L. Tacrolimus: A further update of its use in the management of organ transplantation. Drugs 63 (2003) 1247-1297
6. Felipe C.R., Silva H.T., Machado P.G., et al. The impact of ethnic miscegenation on tacrolimus clinical pharmacokinetics and therapeutic drug monitoring. Clin Transplant 16 (2002) 262-272
7. Bekersky I., Dressler D., Alak A., et al. Comparative tacrolimus pharmacokinetics: Normal versus mildly hepatically impaired subjects. J Clin Pharmacol 41 (2001) 628-635
8. Karamperis N., Povlsen J.V., Hojskov C., et al. Comparison of the pharmacokinetics of tacrolimus and cyclosporine at equivalent molecular doses. Transplant Proc 35 (2003) 1314-1318
9. Bekersky I., Dressler D., Boswell G.W., et al. Bioequivalence of a new strength tacrolimus capsule under development. Transplant Proc 30 (1998) 1457-1459
10. 14C-labeled tacrolimus after intravenous and oral administration in healthy human subjects. Drug Metab Dispos 27 (1999) 633-636
11. Bekersky I., Dressler D., and Mekki Q.A. Dose linearity after oral administration of tacrolimus 1-mg capsules at doses of 3, 7, and 10 mg. Clin Ther 21 (1999) 2058-2064
12. Korea Food and Drug Administration. Korea Good Clinical Practice (2000), KFDA, Seoul, Korea
13. Available at:. World Medical Association Declaration of Helsinki. Accessed. Ethical Principles for Medical Research Involving Human Subjects (November 14, 2005). http://www.wma.net/e/policy/b3.htm
14. Available at:. Electronic Medicines Compendium. Accessed. Astellas Pharma Ltd. Prograf 0.5mg, 1 mg, 5mg hard capsules (November 14, 2005). http://www.emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?DocumentlD=11102#POSOLOGY
15. Zhang Q., Simpson J., and Aboleneen H.I. A specific method for the measurement of tacrolimus in human whole blood by liquid chromatography/tandem mass spectrometry. Ther Drug Monit 19 (1997) 470-476
16. Guidance for Industry. Bioavailability and bioequivalence studies for orally administered drug products-general considerations (July 2002), US Dept of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research, Rockville, Md
17. Guidance for Industry. Bioavailability and bioequivalence studies for orally administered drug products-general considerations. BP Revision 1 (March 2003), US Dept of Health, Food and Drug Administration, Center for Drug Evaluation and Research, Rockville, Md
18. Jusko W.J., Piekoszewski W., Klintmalm G.B., et al. Pharmacokinetics of tacrolimus in liver transplant patients. Clin Pharmacol Ther 57 (1995) 281-290
19. Jain A.B., Todo S., Fung J.J., et al. Correlation of rejection episodes with FK 506 dosage, FK 506 level, and steroids following primary orthotopic liver transplant. Transplant Proc 23 (1991) 3023-3025
20. Backman L., Nicar M., Levy M., et al. FK506 trough levels in whole blood and plasma in liver transplant recipi ents: Correlation with clinical events and side effects. Transplantation 57 (1994) 519-525
21. Schwartz M., Holst B., Facklam D., and Buell D. FK 506 in liver transplantation: Correlation of whole blood lev els with efficacy and toxicity. The US Multicenter FK 506 Dose Optimization. Transplant Proc 27 (1995) 1107
22. Undre N.A., van Hooff J., Christiaans M., et al. Low systemic exposure to tacrolimus correlates with acute rejection. Transplant Proc 31 (1999) 296-298
23. Milanian I., Ghods A.J., Mahmoudian M., et al. Study of circadian variation of cyclosporine pharmacokinetics. Transplant Proc 29 (1997) 2930-2931
24. Iwahori T., Takeuchi H., Matsuno N., et al. Pharmacokinetic differences between morning and evening administration of cyclosporine and tacrolimus therapy. Transplant Proc 37 (2005) 1739-1740
25. Kovarik J.M., Mueller E.A., van Bree J.B., et al. Within-day consistency in cyclosporine pharmacokinetics from a microemulsion formulation in renal transplant patients. Ther Drug Monit 16 (1994) 232-237
26. Bekersky I., Dressier D., and Mekki Q. Effect of time of meal consumption on bioavailability of a single oral 5 mg tacrolimus dose. J Clin Pharmacol 41 (2001) 289-297
27. Bekersky I., Dressler D., and Mekki Q.A. Effect of low- and high-fat meals on tacrolimus absorption following 5 mg single oral doses to healthy human subjects. J Clin Pharmacol 41 (2001) 176-182
28. Hardinger K.L., Park J.M., Schnitzler M.A., et al. Pharmacokinetics of tacrolimus in kidney transplant recipients: Twice daily versus once daily dosing. Am J Transplant 4 (2004) 621-625
29. Mancinelli L.M., Frassetto L., Floren L.C., et al. The pharmacokinetics and metabolic disposition of tacrolimus: A comparison across ethnic groups. Clin Pharmacol Ther 69 (2001) 24-31
30. Dirks N.L., Huth B., Yates C.R., and Meibohm B. Pharmacokinetics of immunosuppressants: A perspec tive on ethnic differences. Int J Clin Pharmacol Ther 42 (2004) 701-718
31. Fitzsimmons W.E., Bekersky I., Dressier D., et al. Demographic considerations in tacrolimus pharmaco kinetics. Transplant Proc 30 (1998) 1359-1364
32. Thervet E., Anglicheau D., King B., et al. Impact of cytochrome p450 3A5 genetic polymorphism on tacrolimus doses and concentration-to-dose ratio in renal transplant recipients. Transplantation 76 (2003) 1233-1235
33. Hesselink D.A., van Schaik R.H., van der Heiden I.P., 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
34. Macphee I.A., Fredericks S., Mohamed M., et al. Tacrolimus pharmacogenetics: The CYP3A5*1 allele predicts low dose-normalized tacrolimus blood concentrations in whites and South Asians. Transplantation 79 (2005) 499-502