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The rat biliary and urinary metabolism of the N6-methylated derivative of elliptinium acetate, and antitumor agent.

The rat biliary and urinary metabolism of N2,N6-dimethyl-9-hydroxyellipticinium (an N6-methyl derivative of elliptinium acetate, an antitumor agent) is reported. Two main metabolites have been identified: the glucuronide and sulfate derivatives by conjugation of the hydroxy group at position 9. Excretion profiles in bile and urine are also given. It has to be noted that no metabolite corresponding to a demethylation at the indolic nitrogen has been identified. However, the evidence for an increased concentration of the oxidized form of glutathione in bile during the drug excretion supports the hypothesis of an oxidative metabolism of this drug in rat liver.