A semisynthetic cephalosporin formulated as the water-soluble
fosamil acetate prodrug for intravenous administration.
Its properties are similar to those of ceftobiprole, with
which it shares an enhanced affinity for penicillin-binding
protein 2′ (2a) of methicillin-resistant Staph. aureus.
It is hydrolyzed by extended-spectrum β-lactamases and is not active against Amp-C derepressed strains of Gram-negative
bacilli.
Pharmacokinetics
Cmax 600 mg intravenous (1-h infusion): 19 mg/L end infusion
Plasma half-life: 2.6 h
Volume of distribution: 0.37 L/kg
Plasma protein binding :<20%
Like ceftobiprole, ceftaroline fosamil is rapidly hydrolyzed in
plasma after intravenous infusion and excreted principally in urine.
In preliminary clinical studies it appears to be well tolerated.
