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Clin Biochem. 1991 Jun;24(3):271-5.

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

Author information

1
Institut für Allgemeine Pharmakologie, Medizinische Hochschule Hannover, Germany.

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.

PMID:
1714802
DOI:
10.1016/0009-9120(91)80019-y
[Indexed for MEDLINE]

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