PT  - JOURNAL ARTICLE
AU  - P C Feng
AU  - C C Fenselau
AU  - R R Jacobson
TI  - Metabolism of clofazimine in leprosy patients.
DP  - 1981 Nov 01
TA  - Drug Metabolism and Disposition
PG  - 521--524
VI  - 9
IP  - 6
4099  - http://dmd.aspetjournals.org/content/9/6/521.short
4100  - http://dmd.aspetjournals.org/content/9/6/521.full
SO  - Drug Metab Dispos1981 Nov 01; 9
AB  - 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.