BACKGROUND: Cefditoren is an advanced-generation, broad-spectrum cephalosporin antibiotic approved for the treatment of acute bacterial exacerbation of chronic bronchitis (AECB), group A beta-hemolytic streptococcal pharyngotonsillitis, and uncomplicated skin/skin structure infections in adult and adolescent patients. OBJECTIVE: This article briefly reviews the chemistry, antimicrobial activity, pharmacokinetics, efficacy, and safety of cefditoren. METHODS: Literature was identified by a MEDLINE search (January 1985 to October 2001) of the medical literature, review of the English-language literature, reference lists within these articles, as well as data presented at the 40th Interscience Conference on Antimicrobial Agents and Chemotherapy. RESULTS: Cefditoren has a broad spectrum of activity against many gram-negative and gram-positive aerobes, including Streptococcus pneumoniae, Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, and Moraxella catarrhalis. Cefditoren is stable to hydrolysis by many common beta-lactamases. Cefditoren is rapidly absorbed (time to peak plasma concentration, approximately 2-3 hours) from the gastrointestinal tract and is almost completely eliminated via renal clearance of unchanged drug. The terminal disposition half-life of the compound is approximately 0.8 to 1.3 hours. CONCLUSIONS: Cefditoren is effective in the management of AECB (in regimens of 400 mg twice daily for 10 days) and acute maxillary sinusitis, pharyngotonsillitis due to S pyogenes, and uncomplicated skin/skin structure infections (in regimens of 200 mg twice daily for 10 days). Cefditoren possesses broad activity against common pathogens of the respiratory tract and skin and is stable in the presence of numerous beta-lactamases. Its pharmacokinetic properties, in conjunction with in vitro susceptibility data, document the feasibility of twice-daily dosing.