Drug Metabolism Letters

Zhiyang Zhao
Amgen
Cambridge, MA
USA

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In Vitro Metabolism of Leflunomide by Mouse and Human Liver Microsomes

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

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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Article Details

VOLUME: 1
ISSUE: 4
Year: 2007
Page: [299 - 305]
Pages: 7
DOI: 10.2174/187231207783221402
Price: $58