Sitafloxacin is a fluoroquinolone antibacterial with in vitro activity against a broad range of Gram-positive and -negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. It is approved in Japan for use in a number of bacterial infections caused by sitafloxacin-susceptible strains of Staphylococcus spp., Streptococcus pneumoniae, other Streptococcus spp., Enterococcus spp., Moraxella catarrhalis, Escherichia coli, Citrobacter spp., Klebsiella spp., Enterobacter spp., Serratia spp., Proteus spp., Morganella morganii, Haemophilus influenzae, Pseudomonas aeruginosa, Legionella pneumophila, Peptostreptococcus spp., Prevotella spp., Porphyromonas spp., Fusobacterium spp., Chlamydia trachomatis, Chlamydophila pneumoniae and Mycoplasma pneumoniae. In terms of clinical efficacy, oral sitafloxacin was noninferior to oral levofloxacin in the treatment of community-acquired pneumonia or an infectious exacerbation of chronic respiratory tract disease, noninferior to oral tosufloxacin in the treatment of community-acquired pneumonia, and noninferior to oral levofloxacin in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, noninferiority trials. Noncomparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, C. trachomatis-associated cervicitis in women and odontogenic infections. Gastrointestinal disorders and laboratory abnormalities were the most commonly occurring adverse reactions in patients receiving oral sitafloxacin. Adverse reactions reported in sitafloxacin recipients in the active comparator trials were of mild to moderate severity.