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Overview
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Ceftaroline Dihydrochloride is a fifth-generation cephalosporin, a broad-spectrum β-lactam active against Gram-positive organisms including methicillin-resistant Staphylococcus aureus (MRSA) and drug-resistant Streptococcus pneumoniae, as well as non-beta-lactamase-producing Gram-negative organisms. Ceftaroline was developed by Forest Laboratories under a license from Takeda. In vitro studies show a similar spectrum to ceftobiprole, the only other 5th generation cephalosporin to date. Analytical methods of ceftaroline quantification for biological samples is scarce. Ceftaroline exhibits time-dependent bactericidal activity.
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Background
Ceftaroline 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 has a high affinity for modified PBPs like PBP2a in S. aureus and PBP2x in S. pneumoniae, leading to high activity against Gram-positive cocci.
Ceftaroline Dihydrochloride is a prodrug that is converted in vivo to its active metabolite Ceftaroline by plasma phosphatases.
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- Properties
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Overview