title: In vivo susceptibility of Mycobacterium leprae to sitafloxacin (DU-6859a), either singly or in combination with rifampicin analogues.
abstract: The antimicrobial effects of sitafloxacin (DU-6859a) against Mycobacterium leprae, either singly or in combination with either rifampicin, rifabutin or KRM-1648, were studied using a mouse footpad assay technique and the results were compared with those obtained with ofloxacin. When used singly, the minimum concentrations of sitafloxacin and ofloxacin needed to inhibit completely the growth of M. leprae were 25 and 100 mg per kg body weight per day, respectively, and the effects were bactericidal. Both sitafloxacin and ofloxacin exhibited excellent synergistic effects when combined with either rifabutin or KRM-1648, but not with rifampicin. Thus, incorporation of sitafloxacin and rifabutin (or KRM-1648) in the multidrug regimen for treating leprosy patients is suggested.
authors.affiliation: Department of Biological Sciences, Florida Institute of Technology, 150 West University Boulevard, Melbourne, FL 32901-6975, USA. adhople@fit.edu
authors.forename: Arvind M
authors.initials: AM
authors.lastname: Dhople
authors.forename: Kenji
authors.initials: K
authors.lastname: Namba
mesh_terms: D000818:Animals; D024881:Drug Resistance, Bacterial; D004359:Drug Therapy, Combination; D005260:Female; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000494:pharmacology*; D007917:Leprostatic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D007918:Leprosy / Q000188:drug therapy* / Q000382:microbiology*; D051379:Mice; D008807:Mice, Inbred BALB C; D009166:Mycobacterium leprae / Q000187:drug effects* / Q000254:growth & development; D015242:Ofloxacin / Q000008:administration & dosage / Q000494:pharmacology; D012293:Rifampin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D024841:Fluoroquinolones; D007917:Leprostatic Agents; C076246:sitafloxacin; D015242:Ofloxacin; D012293:Rifampin