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.
