Ceftibuten is an orally active third generation cephalosporin which has a broad spectrum of in vitro antibacterial activity, encompassing the majority of Gram-negative pathogens and streptococci, and which shows greater stability than several other cephalosporins against bacteria producing extended-spectrum beta-lactamases. In clinical studies, ceftibuten (generally 400 mg/day in adults or 9 mg/kg/day in children, administered once daily) was effective in the treatment of acute uncomplicated or complicated urinary tract infections, demonstrating an efficacy similar to that of cefaclor (1500 mg/day), and similar or superior to that of cotrimoxazole (trimethoprim/sulfamethoxazole; 8/40 mg/kg/day) in children. The majority of patients with acute or chronic lower respiratory tract infections responded to treatment with ceftibuten, and response rates were similar to those achieved with cefaclor (750 or 1500 mg/day). Ceftibuten 9 mg/kg/day was at least as effective as cefaclor and as effective as amoxicillin/clavulanic acid (both 40 mg/kg/day) in children with acute otitis media, and was superior to phenoxymethylpenicillin (penicillin V; 25 mg/kg/day) in children and adolescents with streptococcal pharyngitis or scarlet fever caused by Group A beta-haemolytic streptococci. Ceftibuten was well tolerated in most patients, with adverse events (mostly mild to moderate gastrointestinal disturbances) generally occurring in 5 to 10% of patients. Thus, ceftibuten, with a once- or twice-daily oral dosage regimen, good tolerability profile and activity against a wide range of bacterial organisms, offers a promising alternative to other agents (including cefaclor, cotrimoxazole, amoxicillin/clavulanic acid, bacampicillin and phenoxymethylpenicillin) for the treatment of patients with urogenital and respiratory tract infections. Its place in therapy will be more clearly defined following further large comparative trials, in which it is likely to prove most useful in patients with infections caused by beta-lactamase-producing pathogens.