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Xenobiotica
the fate of foreign compounds in biological systems
Volume 38, 2008 - Issue 2
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Research Article

Metabolism of OR-1896, a metabolite of levosimendan, in rats and humans

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Pages 156-170 | Received 07 Sep 2007, Accepted 12 Oct 2007, Published online: 22 Sep 2008
 

Abstract

OR-1896 is a pharmacologically active, long-lived metabolite of levosimendan. In the current study, the metabolism of 14C-labelled OR-1896 was investigated in six healthy men after intravenous infusion over 10 min and in male rats after an intravenous bolus dose. In human plasma, the only 14C-compounds detected were 14C-OR-1896 and its deacetylated form, 14C-OR-1855, in varying proportions in different subjects. In rat plasma >93% of radioactivity was associated with OR-1896. Radioactivity was mainly excreted to urine in both rats (about 69% of the dose) and humans (about 87% of the dose). OR-1896 was a major urinary compound in both humans and rats. Another major human metabolite was hypothesized as N-conjugated OR-1855. Other human and rat urinary biotransformation products were characterized as N-hydroxylated OR-1896 and N-hydroxylated OR-1855, as well as glucuronide or sulphate conjugates of N-hydroxyl OR-1896. The main difference between rat and human metabolism was a lower amount of OR-1855-related metabolites in the rats. In human faecal homogenates, only OR-1896 and OR-1855 were detected, whereas rat faecal metabolite profile was similar to that in urine.

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