Patent Review of Manufacturing Routes to Fifth-Generation Cephalosporin Drugs. Part 1, Ceftolozane

Over SO cephalosporin drugs have been approved over the past five decades, nearly half of all approved antibacterial drugs. Three new cephalosporins, classified as fifth generation for the treatment of serious Gram-negative bacterial infections including methicillin-resistant Staphylococcus aureus (MRSA), were recently approved. The current article summarizes the current status of antibacterial R&D and government actions to incentivize antibacterial research, provides a brief history of the development of cephalosporin antibacterials, and reviews the patent literature on synthetic routes and final forms of ceftolozane, a cephalosporin drug that was approved in the U.S. in Dec 2014.