Ceftaroline Fosamil

Ceftaroline Fosamil is a fifth-generation cephalosporin, a broad-spectrum β-lactam active against MRSA and respiratory pathogens. It carries the trade name Teflaro (US) or Zinforo i(Europe). It can be used against the bacteria causing community-acquired pneumonia and complicated skin and skin structure infections. In vitro studies show a similar spectrum to ceftobiprole, the only other 5th generation cephalosporin to date.
Ceftaroline Fosamil is sparingly soluble in DMSO.

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Background

Ceftaroline Fosamil binds to penicillin-binding protein (PBP) which prevents the formation of the bacterial cell wall. MRSA strains have a mutated PBP2a which prohibits β-lactam antibiotics from accessing its active site. Ceftaroline has an ethyoxyimino side-chain mimicking a portion of a cell wall structure, which opens and facilitates access to the active site of PBP2a.
Ceftaroline Fosamil is a prodrug that is converted in vivo to its active metabolite Ceftaroline by plasma phosphatases.