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. 1992 Jun;33(6):661–664. doi: 10.1111/j.1365-2125.1992.tb04098.x

Cyclosporin metabolism by human gastrointestinal mucosal microsomes.

I R Webber 1, W H Peters 1, D J Back 1
PMCID: PMC1381361  PMID: 1389941

Abstract

The in vitro metabolism of the immunosuppressant cyclosporin (CsA) by human gastrointestinal mucosal microsomes has been studied. Macroscopically normal intestinal (n = 4) and liver (n = 2) tissue was obtained from kidney transplant donors, and microsomes prepared. Intestinal metabolism was most extensive with duodenal protein (15% conversion to metabolites M1/M17 after 2 h incubation at 37 degrees C; metabolite measurement by h.p.l.c). Western blotting confirmed the presence of P-4503A (enzyme subfamily responsible for CsA metabolism) in duodenum and ileum tissue, but not in colon tissue. The results of this study indicate that the gut wall may play a role in the first-pass metabolism of CsA, and could therefore be a contributory factor to the highly variable oral bioavailability of CsA.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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