Ceftaroline Fosamil: A Broad-spectrum Cephalosporin With Methicillin-Resistant Staphylococcus aureus Activity

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Abstract

Ceftaroline fosamil is a cephalosporin prodrug, the active metabolite of which, ceftaroline, exhibits broad-spectrum bactericidal activity against gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and Streptococcus pneumoniae, as well as common gram-negative pathogens. It exerts its antimicrobial effects by binding to penicillin-binding proteins, causing bacterial cell death. Ceftaroline is primarily eliminated by renal excretion and exhibits plasma protein binding of ∼20% and an elimination half-life of 1.60 hours (single intravenous [IV] dose) to 2.66 hours (multiple doses). On the basis of the results of phase 3 clinical trials, ceftaroline fosamil was approved by the US Food and Drug Administration for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) and community-acquired bacterial pneumonia caused by designated susceptible bacteria. In these trials, patients with ABSSSI treated with ceftaroline fosamil 600 mg IV every 12 hours for 5 to 14 days had a clinical cure rate of 91.6% (559/610) compared with 92.7% (549/592) for patients treated with vancomycin 1 g IV plus aztreonam 1 g IV every 12 hours. Patients with community-acquired bacterial pneumonia treated with ceftaroline fosamil 600 mg IV every 12 hours for 5 to 7 days had a clinical cure rate of 84.3% (387/459), and those who received ceftriaxone 1 g IV every 24 hours had a clinical cure rate of 77.7% (349/449). No off-label uses for ceftaroline fosamil have been studied. The most common treatment-emergent adverse effects reported in clinical trials were diarrhea, nausea, and headache. The benefits of ceftaroline fosamil include broad-spectrum antimicrobial activity, including activity against MRSA, and a safety profile typical of the cephalosporin class.

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