PT - JOURNAL ARTICLE AU - Shu L. Lu AU - Itsaraet Gosriwatana AU - Ding Y. Liu AU - Zu D. Liu AU - Anthony I. Mallet AU - Robert C. Hider TI - Biliary and Urinary Metabolic Profiles of 1,2-Diethyl-3-hydroxypyridin-4-one (CP94) in the Rat DP - 2000 Aug 01 TA - Drug Metabolism and Disposition PG - 873--879 VI - 28 IP - 8 4099 - http://dmd.aspetjournals.org/content/28/8/873.short 4100 - http://dmd.aspetjournals.org/content/28/8/873.full SO - Drug Metab Dispos2000 Aug 01; 28 AB - This study compares the biliary and urinary metabolic profiles of 1,2-diethyl-3-hydroxypyridin-4-one (CP94), an orally active iron chelator, in the normal rat. Surprisingly, CP94 was found to form two phase II metabolites, the 3-O- and 4-O-glucuronides. These glucuronides accounted for 38 and 28% of the administered CP94 dose, in bile and urine, respectively. Unchanged CP94 accounted for 5% of the CP94 dose in both bile and urine. The 2-(1′-hydroxy) metabolite of CP94 was found to be the dominant metabolite in urine. In addition, an unstable metabolite was detected in the bile although its structure remains unknown at the present stage. The excretion of iron in bile, after administration of CP94, was found to parallel the biliary elimination of CP94 together with its hydroxylated derivatives, indicating the importance of metabolites in iron excretion. The American Society for Pharmacology and Experimental Therapeutics