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Seven cyclosporin G metabolites were isolated by high-performance liquid chromatography from the urine of normal subjects receiving the drug. The structure and purity of the metabolites were assessed by fast atom bombardment/mass spectroscopy, by proton nuclear magnetic resonance (NMR), and by 13C-NMR. The structural modifications of the cyclosporin G metabolites consisted primarily of hydroxylation and demethylation, as is the case for cyclosporin A metabolites. The immunosuppressive activities of the metabolites were tested in three separate in vitro systems: a primary and secondary mixed lymphocyte system, as well as a mitogen stimulated system. In general, the metabolites have immunosuppressive activity of less than 10% of cyclosporin G. The significance of these findings in relation to the therapeutic monitoring of cyclosporin G is discussed.
K R Copeland, and
R W Yatscoff
June 1993,
Clinical chemistry,
K R Copeland, and
R W Yatscoff
April 1986,
Clinical chemistry,
K R Copeland, and
R W Yatscoff
October 1992,
Therapeutic drug monitoring,
K R Copeland, and
R W Yatscoff
February 1993,
Clinical chemistry,
K R Copeland, and
R W Yatscoff
July 1987,
Clinical chemistry,
K R Copeland, and
R W Yatscoff
October 1987,
Transplantation proceedings,
K R Copeland, and
R W Yatscoff
February 1989,
Transplantation proceedings,
K R Copeland, and
R W Yatscoff
July 1987,
Transplantation,
K R Copeland, and
R W Yatscoff
August 1989,
Lancet (London, England),
K R Copeland, and
R W Yatscoff
April 1989,
Lancet (London, England),
