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  • Title: Isolation of two immunosuppressive metabolites after in vitro metabolism of rapamycin.
    Author: Christians U, Sattler M, Schiebel HM, Kruse C, Radeke HH, Linck A, Sewing KF.
    Journal: Drug Metab Dispos; 1992; 20(2):186-91. PubMed ID: 1352208.
    Abstract:
    Rapamycin was incubated with human liver microsomes and an NADPH regenerating system, the metabolites were purified by semipreparative HPLC, and their structures were elucidated by direct chemical ionization and FAB-MS. At least six fractions were isolated containing rapamycin metabolites, indicating that rapamycin is metabolized by the human liver cytochrome P-450 system. One of these metabolites was identified as 41-O-demethyl-rapamycin. A second metabolite was hydroxylated in a yet unknown position. These two metabolites retained immunosuppressive activity in a phytohemagglutinin-stimulated human lymphocyte assay with IC50S of 1 and 1.5 nmol/liter, respectively. Rapamycin was metabolized by rat small intestinal microsomes to at least two metabolites, indicating extra-hepatic metabolism of rapamycin.
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