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Ceftaroline fosamil, also referred to as TAK-599, is a cephalosporin antibacterial agent that was approved in the United States in October 2010 for the IV treatment of acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP). Ceftaroline fosamil is the water-soluble, N-phosphono prodrug of ceftaroline (T-91825), a broad-spectrum, bactericidal agent with potent activity against methicillin-resistant Staphylococcus aureus (MRSA) strains, multidrug resistant S. pneumonia, and common gram-negative organisms. Ceftaroline binds to PBP2a as well as other PBPs with high affinity and, as a result, retains potent activity. Ceftaroline exhibits activity against most gram-positive pathogens, including β-lactam-susceptible and -resistant S. aureus, vancomycin-resistant S. aureus, and resistant and susceptible forms of S. pneumoniae but has weak activity against Enterococcus sp. The gram-negative antibacterial activity of ceftaroline is limited mainly to respiratory pathogens such as Moraxella catarrhalis and Haemophilus influenzae.
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