@article{103522, keywords = {Metabolism, Clofazimine, Leprosy patients}, author = {Feng P and Fenselau C and Jacobson R}, title = {Metabolism of clofazimine in leprosy patients.}, abstract = {
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.
}, year = {1981}, journal = {Drug metabolism and disposition: the biological fate of chemicals}, volume = {9}, pages = {521 - 524}, month = {01/1981}, issn = {0090-9556}, language = {ENG}, }