Orally active, 4th generation fluoroquinolone broad-spectrum antibiotic with dual DNA gyrase and topoisomerase IV inhibitory activity.
Sitafloxacin (DU-6859 or DU-6859a) is an orally active, fourth generation fluoroquinolone that exhibits broad-spectrum antibiotic activity against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, via dual inhibitory activity against bacterial DNA gyrase and topoisomerase IV (IC50 = 1.16 and 1.88 μg/mL against S. pneumoniae gyrA/B and parC/E, respectively). Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin also exhibits activity against clinical isolates of Klebsiella pneumoniae, Enterobacter cloacae, Pseudomonas aeruginosa as well as some activity against quinolone-resistant strains and Acinetobacter baumannii. Sitafloxacin in vitro activity against anaerobes is comparable to imipenem and metronidazole.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Certificates of Analysis (COA)
Lot/Batch Number
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Antimicrobial agents and chemotherapy, 36(7), 1491-1498 (1992-07-01)
DU-6859, (-)-7-[(7S)-amino-5-azaspiro(2,4)heptan-5-yl]-8-chloro-6- fluoro-1-[(1R,2R)-cis-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxoquinol one-3- carboxylic acid, is a new fluoroquinolone with antibacterial activity which is significantly better than those of currently available quinolones. The MICs for 90% of methicillin-susceptible and -resistant Staphylococcus aureus and Staphylococcus epidermidis clinical isolates (MIC90s) were
Antimicrobial agents and chemotherapy, 42(5), 1284-1287 (1998-05-21)
The in vitro inhibitory effects of sitafloxacin (DU-6859a) and its three stereoisomers on bacterial DNA gyrase from Escherichia coli, topoisomerase IV from Staphylococcus aureus, and topoisomerase II from human placenta were compared. No correlation was observed between the inhibitory activities
Drugs of today (Barcelona, Spain : 1998), 44(7), 489-501 (2008-09-23)
Sitafloxacin hydrate (DU-6859a, Gracevit), a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract
Diagnostic microbiology and infectious disease, 20(1), 45-47 (1994-09-01)
The activity of DU-6859a, a new fluoroquinolone antimicrobial agent, was compared with that of ciprofloxacin by agar dilution susceptibility testing against enteric pathogens and multiresistant Escherichia coli. The results indicate that DU-6859a inhibits most of these organisms at concentrations similar
Antimicrobial agents and chemotherapy, 37(12), 2747-2753 (1993-12-01)
DU-6859a was tested against 844 recent clinical isolates (most from bacteremias) by using reference MIC determination procedures. The activity of DU-6859a against members of the family Enterobacteriaceae was comparable to that of ciprofloxacin (range of MICs for 90% of isolates
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