Drug Metabolism Letters

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

DOI: 10.2174/187231207783221402

Cite As
In Vitro Metabolism of Leflunomide by Mouse and Human Liver Microsomes

Page: [299 - 305] Pages: 7

  • * (Excluding Mailing and Handling)

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