Sitafloxacin (DU-6859a) is a new-generation oral fluoroquinolone with in vitro activity against a broad range of Gram-positive and -negative bacteria, including anaerobic bacteria, as well as against atypical bacterial pathogens. Particularly in Japan this antibiotic was approved in 2008 for treatment of a number of bacterial infections caused by Gram-positive cocci and Gram-negative cocci and rods, including anaerobia atypical bacterial pathogens. As compared to oral levofloxacin sitafloxacin was non-inferior in the treatment of community-acquired pneumonia and non-inferior in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, non-inferiority trials. Non-comparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, cervicitis in women and odontogenic infections. Most common adverse reactions were gastrointestinal disorders and laboratory abnormalities in patients receiving oral sitafloxacin; diarrhea and liver enzyme elevations were among the common. In the Japanese population sitafloxacin covers broad spectrum of bacteria as compared to carbapenems, whereas in the Caucasians its use is currently limited due to the potential for ultraviolet A phototoxicity. Sitafloxacin is a promising therapeutic agent which merits further investigation in randomized clinical trials of elderly patients.