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Research ArticleArticle

The Disposition of 14C-Labeled Tacrolimus after Intravenous and Oral Administration in Healthy Human Subjects

A. Möller, K. Iwasaki, A. Kawamura, Y. Teramura, T. Shiraga, T. Hata, A. Schäfer and N. A. Undre
Drug Metabolism and Disposition June 1999, 27 (6) 633-636;
A. Möller
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K. Iwasaki
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A. Kawamura
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Y. Teramura
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T. Shiraga
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T. Hata
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A. Schäfer
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N. A. Undre
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Abstract

Tacrolimus is a macrolide lactone with potent immunosuppressive properties. It has been shown in clinical studies to prevent allograft rejection. The pharmacokinetics of tacrolimus in healthy subjects and transplant patients has been described in earlier studies using immunoassay methods; however, detailed information on the absorption, distribution, metabolism, and excretion of tacrolimus using a radiolabeled drug is lacking. The objective of the present study was to characterize the disposition of tacrolimus after single i.v. (0.01 mg/kg) and oral (0.05 mg/kg) administration of 14C-labeled drug in six healthy subjects. Tacrolimus was absorbed rapidly after oral dosing with a mean Cmax andTmax of 42 ng/ml and 1 h, respectively. The oral bioavailability was about 20%. After i.v. and oral dosing, most of the administered dose was recovered in feces, suggesting that bile is the principal route of elimination. Urinary excretion accounted for less than 3% of total administered dose. In systemic circulation, unchanged parent compound accounted for nearly all the radioactivity; however, less than 0.5% of unchanged drug was detectable in feces and urine. The excretion of the metabolites was formation-rate-limited. The mean total body clearance at 37.5 ml/min was equivalent to about 3% of the liver blood flow. Renal clearance was less than 1% of the total body clearance. The mean elimination half-life was 44 h.

Footnotes

  • Send reprint requests to: Dr. N. A. Undre, Fujisawa GmbH, Levelingstrasse 12, D-81606, Munich, Germany. E-mail:Nas.Undre{at}Fujisawa.DE

  • This study was supported by Fujisawa GmbH, Munich.

  • Abbreviations used are::
    LSC
    liquid scintillation counting
    ELISA
    enzyme-linked immunosorbent assay
    AUC
    area under the concentration–time profile
    • Received May 8, 1998.
    • Accepted September 28, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 27 (6)
Drug Metabolism and Disposition
Vol. 27, Issue 6
1 Jun 1999
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Research ArticleArticle

The Disposition of 14C-Labeled Tacrolimus after Intravenous and Oral Administration in Healthy Human Subjects

A. Möller, K. Iwasaki, A. Kawamura, Y. Teramura, T. Shiraga, T. Hata, A. Schäfer and N. A. Undre
Drug Metabolism and Disposition June 1, 1999, 27 (6) 633-636;

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Research ArticleArticle

The Disposition of 14C-Labeled Tacrolimus after Intravenous and Oral Administration in Healthy Human Subjects

A. Möller, K. Iwasaki, A. Kawamura, Y. Teramura, T. Shiraga, T. Hata, A. Schäfer and N. A. Undre
Drug Metabolism and Disposition June 1, 1999, 27 (6) 633-636;
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