Zinforo: first cephalosporin with activity against MRSA

3 December 2012

Ceftaroline fosamil is a fifth-generation cephalosporin licensed for the treatment of complicated skin and soft tissue infections (cSSTI) and community-acquired pneumonia (CAP).

Zinforo can be used at a lower dose in patients with mild to moderate renal impairment but is contraindicated if the impairment is severe

PHARMACOLOGY

Ceftaroline fosamil is a fifth-generation broad-spectrum cephalosporin prodrug that is converted to the active compound ceftaroline in vivo. It exhibits bactericidal activity through inhibition of cell wall synthesis. Importantly, it is active against methicillin-resistant Staphylococcus aureus (MRSA) and penicillin non-susceptible Streptococcus pneumoniae (PNSP) owing to an affinity for the altered penicillin-binding proteins found in these organisms.¹

CLINICAL STUDIES

Ceftaroline displayed efficacy in the treatment of cSSTI in two randomised double-blind phase III non-inferiority studies (CANVAS 1 and 2) in 1378 adults. In a pooled analysis, patients treated with ceftaroline monotherapy (600mg every 12 hours) had similar clinical cure rates to those treated with vancomycin plus aztreonam (1g of each every 12 hours) following 5–14 days of treatment (91.6% versus 92.7% in the clinically evaluable population [n=1202]).²

Efficacy in hospitalised patients with CAP was assessed in two randomised double-blind phase III non-inferiority trials (FOCUS 1 and 2, total n=1228). An integrated analysis of the results showed a non-inferior and numerically higher clinical cure rate following treatment with ceftaroline (600mg every 12 hours) compared with ceftriaxone (1g every 24 hours) both for 5–7 days: 82.6% vs 76.6% (difference 6%; 95% CI 1.4–10.7%, modified intention-to-treat efficacy population [n=1153]).³

Ceftaroline was well tolerated in clinical trials, with nausea, diarrhoea, headache and pruritus being the most commonly observed adverse events.¹

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