In Vitro Metabolism of Leflunomide by Mouse and Human Liver Microsomes
Eric C.Y. Chan,
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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