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

✍ Scribed by Uwe Christians; Heinfried H. Radeke; Reinhard Kownatzki; H.M. Schiebel; Renate Schottmann; Karl-Fr. Sewing

Book ID: 103039198
Publisher: Elsevier Science
Year: 1991
Tongue: English
Weight: 378 KB
Volume: 24
Category: Article
ISSN: 0009-9120
DOI: 10.1016/0009-9120(91)80019-y

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✦ Synopsis

Metabolism of FK506, a 23 member macrolide under clinical investigation as immunosuppressant after transplantation, was studied using human liver microsomes. Two fractions isolated by semipreparative 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 ICso of 0.186 nmol/L and the metabolite tested of 1.89 nmol/L.

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