An Acid Metabolite of Cyclosporine

Overview

Journal Biochem Biophys Res Commun

Publisher Elsevier

Specialty Biochemistry

Date 1985 Dec 31

PMID 4084311

Citations 11

Authors

N R Hartman

L A Trimble

J C Vederas

I Jardine

Affiliations

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Abstract

The primary biliary metabolite of cyclosporine has been isolated from rabbit and human bile. The material has been identified by mass spectrometry and by nuclear magnetic resonance spectrometry as an acidic metabolite of cyclosporine in which the eta-methyl group of the cyclosporine-specific nine carbon amino acid #1 has been oxidized to an alpha, beta unsaturated carboxylic acid functionality. This major cyclosporine metabolite is inactive in a phytohemagglutinin stimulated lymphocyte proliferation assay.

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Cyclosporin clinical pharmacokinetics.

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