@article{18366, keywords = {Administration, Oral, Animals, Disease Models, Animal, Dose-Response Relationship, Drug, Female, Leprostatic Agents, leprosy, Mice, Mice, Inbred BALB C, Mice, Nude, Mycobacterium leprae, Rifampin, Rifamycins}, author = {Tomioka H and Saito H}, title = {In vivo antileprosy activity of the newly synthesized benzoxazinorifamycin, KRM-1648.}, abstract = {
The in vivo anti-Mycobacterium leprae activity of the newly synthesized benzoxazinorifamycin, KRM-1648, was studied. KRM-1648 was given orally to athymic nude mice, infected subcutaneously with M. leprae in the hindfoot pad, at doses between 0.001 and 0.01 mg of the drug/mouse/day six times per week, from day 31 to day 80. KRM-1648 administration markedly suppressed bacterial growth in the foot pads for 360 days. KRM-1648 given daily at the dose of 0.01 mg/mouse elicited a 2-4-log decrease in the number of acid-fast bacilli. The therapeutic effects of KRM-1648 were significantly higher than that of rifampin when both drugs were given in the same dosage. Moreover, when mice were fed a KRM-1648-containing diet (0.00004%-0.0004%), the drug displayed an even higher efficacy against M. leprae infection, causing an almost 4-log decrease in the number of leprosy bacilli in the infected foot pad compared to untreated controls.
}, year = {1993}, journal = {International journal of leprosy and other mycobacterial diseases : official organ of the International Leprosy Association}, volume = {61}, pages = {255-8}, month = {1993 Jun}, issn = {0148-916X}, url = {http://ila.ilsl.br/pdfs/v61n2a11.pdf}, language = {eng}, }