Cefozopran hydrochloride is a third-generation cephalosporin that was launched for the treatment of severe infections in immunocompromised patients caused by staphylococci and enterococci. While it shows a very broad antibacterial spectrum against Gram-positive and Gram-negative organisms, it is particularly potent against S. aureus, Enterococcus faecalis, P. aeruginosa, and Citrobacter freundii. It is resistant to hydrolysis by most chromosomal and plasmid mediated β-lactamases and is reported to be active against respiratory, urinary tract, obstetrical, gynecological, soft tissue, and surgical infections. Similar to β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases.