Literature DB >> 1714802

Isolation of an immunosuppressive metabolite of FK506 generated by human microsome preparations.

U Christians1, H H Radeke, R Kownatzki, H M Schiebel, R Schottmann, K F Sewing.   

Abstract

Metabolism of FK506, a 23 member macrolide under clinical investigation as immunosuppressant after transplantation, was studied using human liver microsomes. Two fractions isolated by semi-preparative HPLC were identified by negative fast atom bombardment mass spectrometry as FK506 metabolites with mass peaks at m/z = 790 indicating demethylation of the mother compound. The immunosuppressive activity of one metabolite was evaluated in a ConA-stimulated peripheral rat lymphocyte assay. FK506 had an IC50 of 0.186 nmol/L and the metabolite tested of 1.89 nmol/L.

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Year:  1991        PMID： 1714802     DOI： 10.1016/0009-9120(91)80019-y

Source DB:  PubMed          Journal:  Clin Biochem        ISSN： 0009-9120            Impact factor:   3.281


  6 in total

1.  Effects of cyclosporin and FK-506 on glomerular mesangial cells. Evidence for direct inhibition of thromboxane synthase by low cyclosporin concentrations.

Authors:  H H Radeke; S Kuster; V Kaever; K Resch
Journal:  Eur J Clin Pharmacol       Date:  1993       Impact factor: 2.953

2.  Tacrolimus (FK 506) biotransformation in primary rat hepatocytes depends on extracellular matrix geometry.

Authors:  A Bader; E Knop; K H Böker; O Crome; N Frühauf; A K Gonschior; U Christians; H Esselmann; R Pichlmayr; K F Sewing
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1996-03       Impact factor: 3.000

Review 3.  Clinical pharmacokinetics and pharmacodynamics of tacrolimus in solid organ transplantation.

Authors:  Christine E Staatz; Susan E Tett
Journal:  Clin Pharmacokinet       Date:  2004       Impact factor: 6.447

4.  Pharmacokinetics of tacrolimus during pregnancy.

Authors:  Songmao Zheng; Thomas R Easterling; Jason G Umans; Menachem Miodovnik; Justina C Calamia; Kenneth E Thummel; Danny D Shen; Connie L Davis; Mary F Hebert
Journal:  Ther Drug Monit       Date:  2012-12       Impact factor: 3.681

Review 5.  Clinical pharmacokinetics of tacrolimus.

Authors:  R Venkataramanan; A Swaminathan; T Prasad; A Jain; S Zuckerman; V Warty; J McMichael; J Lever; G Burckart; T Starzl
Journal:  Clin Pharmacokinet       Date:  1995-12       Impact factor: 6.447

Review 6.  Mechanisms of clinically relevant drug interactions associated with tacrolimus.

Authors:  Uwe Christians; Wolfgang Jacobsen; Leslie Z Benet; Alfonso Lampen
Journal:  Clin Pharmacokinet       Date:  2002       Impact factor: 6.447
  6 in total

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