Biliary concentrations of a new cephalosporin, ceftizoxime, were measured in bile collected in 8 cholecystectomized patients provided with T-tube drainage and in 14 patients where bile was obtained by puncture of the gall bladder and choledochus during cholecystectomy. In patients with external biliary drainage, a mean biliary peak of 150.3 ± SEM 49.8 μg/ml has been observed 2 h after intravenous injection of 2 g of ceftizoxime; the antibiotic activity amounted still to 17.3 ± 6.0 μg/ml after 6 h. Assays performed during operation showed the following simultaneous concentrations 1 h after 2g of ceftizoxime given intravenously: serum: 85.3 ± 8.1 μg/ml; main duct bile: 279.8 ± 40.0 μg/ml; gallbladder bile: 119.9 ± 19.4 μg/ml. These findings were compared with the biliary excretion of 8 other cephalosporins studied previously under the same conditions. The results of the present study suggest that administration of ceftizoxime may be effective in the treatment of biliary tract infections.