Journal article

METABOLISM AND ELIMINATION OF 5,6-DIMETHYLXANTHENONE-4-ACETIC ACID IN THE ISOLATED-PERFUSED RAT-LIVER

LK WEBSTER, AG ELLIS, P KESTELL, GW REWCASTLE

Drug Metabolism and Disposition | WILLIAMS & WILKINS | Published : 1995

Abstract

5,6-Dimethylxanthenone-4-acetic acid (DXAA) is a synthetic xanthenone derivative that is active against murine solid tumors and is being formulated for clinical trials. This study used the isolated perfused rat liver to compare the hepatic metabolism and biliary excretion of DXAA with flavone-8-acetic acid (FAA), a synthetic flavonoid undergoing clinical evaluation as an anticancer drug. Perfusate, bile, and liver samples were assayed for parent drug and metabolites by HPLC. Three FAA metabolites were present in bile, and one of these coeluted with FAA acyl glucuronide. Alkaline hydrolysis of high-dose DXAA bile samples resulted in the disappearance of 5 of 7 metabolite peaks. One biliary me..

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