Moxalactam was administered intravenously or intramuscularly or both in doses of 1 to 12 g/day to 45 patients with clinically significant infections (17 soft tissue or bone, 9 pleuropulmonary, 9 septicemic, 6 urinary tract, and 4 intraabdominal infections). Mean 0.5-h postinfusion levels were 105 micrograms/ml for a 4.0-g dose, 44.7 micrograms/ml for a 2.0-g dose, and 18 micrograms/ml for a 1.0-g dose. We identified 28 isolates of Enterobacteriaceae, 10 Pseudomonas aeruginosa isolates, 9 Staphylococcus aureus isolates, and 15 anaerobic bacterial isolates. A total of 15 patients were clinically cured, 8 patients improved, 13 patients improved initially but suffered subsequent relapses or superinfections, and 10 patients failed therapy. Toxicity was generally minimal (reversible eosinophilia, and mild liver function abnormalities, and elevated prothrombin time). The selection or emergence of resistant organisms in 17 patients during treatment (particularly Pseudomonas, enterococci, and Candida) was a disturbing feature of therapy. Our results were generally favorable, considering the complicated underlying medical problems of this group of patients.