In vitro metabolism of leflunomide by mouse and human liver microsomes.
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 alpha-cyanoenol form of A77-1726 and the hydroxylated 5 methyl-isoxazole form of leflunomide, respectively.
Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543. phaccye@nus.edu.sg
Eric C Y
EC
Chan
Lee-Sun
LS
New
D000814:Aniline Compounds / Q000378:metabolism; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000378:metabolism*; D002853:Chromatography, Liquid / Q000379:methods; D003437:Crotonates; D006801:Humans; D006885:Hydroxybutyrates / Q000378:metabolism; D006900:Hydroxylation; D007555:Isoxazoles / Q000378:metabolism*; D000077339:Leflunomide; D008297:Male; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism*; D009570:Nitriles; D014052:Toluidines
D000814:Aniline Compounds; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003437:Crotonates; D006885:Hydroxybutyrates; D007555:Isoxazoles; D009570:Nitriles; D014052:Toluidines; C527525:teriflunomide; D000077339:Leflunomide