01284nas a2200193 4500000000100000008004100001260001200042653001500054653001600069653002100085100001100106700001500117700001500132245005100147300001400198490000600212520085800218022001401076 1981 d c01/198110aMetabolism10aClofazimine10aLeprosy patients1 aFeng P1 aFenselau C1 aJacobson R00aMetabolism of clofazimine in leprosy patients. a521 - 5240 v93 a
We have identified two metabolites of clofazimine (B663; Lamprene; 3-(p-chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) in our initial investigation of its metabolism in leprosy patients. Based on mass, ultraviolet, and visible spectrometry, we characterized an unconjugated (metabolite I, 3-(p-hydroxyanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine ) and a conjugated (metabolite II, 3-(beta-D-glucopyranosiduronic acid)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) metabolite from the urine of patients. Both metabolites were red in color, similar to clofazimine; however, both were considerably more polar than the parent drug. We suggest that metabolite I was formed by a hydrolytic dehalogenation reaction, and metabolite II by hydrolytic deamination followed by glucuronidation.
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