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Hepatic biotransformation of MLN8054 was studied in vitro applying human liver S9 fractions (Information on file, Millennium). Glucuronidation with the carboxylate moiety of MLN8054 to an acyl glucuronide was the predominant mechanism of biotransformation, Hydroxylation from the azepine moiety of MLN8054 was the main phase 1 biotransformation pathw