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Drug Metabolism Letters

Editor-in-Chief

ISSN (Print): 1872-3128
ISSN (Online): 1874-0758

In Vitro Metabolism of Leflunomide by Mouse and Human Liver Microsomes

Author(s): Eric C.Y. Chan and Lee-Sun New

Volume 1, Issue 4, 2007

Page: [299 - 305] Pages: 7

DOI: 10.2174/187231207783221402

Price: $65

Abstract

Leflunomide was found to be metabolized predominantly to A77-1726 and two novel hydroxylated metabolites, M1 and M2, in microsomes while A77-1726 was only biotransformed to M1. M1 and M2 were proposed to be the hydroxylated α-cyanoenol form of A77-1726 and the hydroxylated 5 methyl-isoxazole form of leflunomide, respectively.

Keywords: Leflunomide, A77-1726, microsomes, metabolic profiling, UPLC, QTOFMS


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