Sitafloxacin, a fourth-generation fluoroquinolone antibacterial agent, exerts potent antibacterial activity against gram-negative and gram-positive bacteria, atypical pathogens and anaerobic bacteria. It also remains effective against fluoroquinolone-resistant strains, methicillin-resistant Staphylococcus aureus, penicillin-insensitive Streptococcus pneumoniae and Enterococcus. It is widely used clinically for treating infectious diseases such as upper and lower respiratory tract infections, genitourinary infections, oral infections and otitis media. Sitafloxacin shows linear pharmacokinetic characteristics within the dose range of 50-200 mg. It is rapidly absorbed after oral administration, widely distributed in various tissues and organs throughout the body, and mainly excreted in the urine as unchanged form. Commonly reported adverse events include diarrhea, nausea and abnormal liver function. In recent years, studies have found that sitafloxacin is also effective against multidrug-resistant pathogens causing ventilator-associated pneumonia, hospital-acquired pneumonia, tuberculosis, Mycoplasma genitalium infections in men, Mycobacterium abscessus infection periodontal infection, Helicobacter pylori infections and refractory Mycobacterium skin infections. However, further clinical studies are still needed to evaluate its efficacy and safety, and pharmacokinetic studies should be conducted in special populations such as the elderly and those with hepatic impairment. This article systematically reviews the pharmacological mechanism, antibacterial activity, pharmacokinetic/pharmacodynamic characteristics and recent advances in clinical research of sitafloxacin, aiming to provide a reference basis for the safe and effective clinical use of sitafloxacin.