Ceftaroline Fosamil is a novel fifth-generation cephalosporin, a broad-spectrum β-lactam active against MRSA and respiratory pathogens. It goes by the name Teflaro in the US and Zinforo in Europe. It can be used for community-acquired pneumonia and complicated skin and skin structure infections. The compound is soluble in DMSO (30 mg/ml).
|Mechanism of Action|
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 active metabolite Ceftaroline by plasma phosphatases.
|Spectrum||Ceftaroline Fosamil is broad-spectrum against Gram-positive and Gram-negative bacteria. It is effective against methicillin-resistant Staphylococcus aureus (MRSA), and extensively-resistant strains such as vancomycin-resistant S. aureus (VRSA), vancomycin-intermediate S. aureus (VISA), and heteroresistant VISA (hVISA). It is also effective against respiratory pathogens like Streptococcus pneumoniae and Haemophilus influenzae.|
In vitro studies show a similar spectrum to ceftobiprole, the only other 5th generation cephalosporin to date.
Ceftaroline is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips). Medical microbiologists use AST results to recommend antibiotic treatment options for infected patients. Representative MIC values include:
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