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Chemical Compound Review:

Fk-506

Synonyms: AGN-PC-00BJ0S, SureCN385446, AC1L1K7H

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Associations of tacrolimus with other chemical compounds

Methylprednisolone aceponate was superior to tacrolimus for EASI, itch and sleep [1].
DIRECT (Diabetes Incidence after Renal Transplantation: Neoral C(2) Monitoring Versus Tacrolimus) was a 6-month, open-label, randomized, multicenter study which used American Diabetes Association/World Health Organization criteria to define glucose abnormalities [2].

Gene context of tacrolimus

CYP3A5 in the kidney may play a protective role in the development of tacrolimus-related nephrotoxicity [3].
In renal allograft recipients the CYP3A5*3/*1 genotype is associated with a reduced susceptibility for the inhibitory effects of fluconazole on tacrolimus metabolism, thereby identifying a genetic determinant of the clinical variability of CYP3A-mediated drug interactions [4].
We conclude that patients expressing CYP3A5 need more tacrolimus to reach target concentrations and have a lower tacrolimus exposure shortly after transplantation [5].

References

Efficacy and safety of methylprednisolone aceponate ointment 0.1% compared to tacrolimus 0.03% in children and adolescents with an acute flare of severe atopic dermatitis. Bieber, T., Vick, K., Fölster-Holst, R., Belloni-Fortina, A., Städtler, G., Worm, M., Arcangeli, F. Allergy (2007) [Pubmed]
Results of an international, randomized trial comparing glucose metabolism disorders and outcome with cyclosporine versus tacrolimus. Vincenti, F., Friman, S., Scheuermann, E., Rostaing, L., Jenssen, T., Campistol, J.M., Uchida, K., Pescovitz, M.D., Marchetti, P., Tuncer, M., Citterio, F., Wiecek, A., Chadban, S., El-Shahawy, M., Budde, K., Goto, N. Am. J. Transplant. (2007) [Pubmed]
Impact of MDR1 and CYP3A5 on the oral clearance of tacrolimus and tacrolimus-related renal dysfunction in adult living-donor liver transplant patients. Fukudo, M., Yano, I., Yoshimura, A., Masuda, S., Uesugi, M., Hosohata, K., Katsura, T., Ogura, Y., Oike, F., Takada, Y., Uemoto, S., Inui, K. Pharmacogenet. Genomics (2008) [Pubmed]
Effects of CYP3A5 and MDR1 single nucleotide polymorphisms on drug interactions between tacrolimus and fluconazole in renal allograft recipients. Kuypers, D.R., de Jonge, H., Naesens, M., Vanrenterghem, Y. Pharmacogenet. Genomics (2008) [Pubmed]
CYP3A5 genotype is not associated with a higher risk of acute rejection in tacrolimus-treated renal transplant recipients. Hesselink, D.A., van Schaik, R.H., van Agteren, M., de Fijter, J.W., Hartmann, A., Zeier, M., Budde, K., Kuypers, D.R., Pisarski, P., Le Meur, Y., Mamelok, R.D., van Gelder, T. Pharmacogenet. Genomics (2008) [Pubmed]

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