Ceftaroline fosamil

TAK-599 is a prodrug of T-91825, a cephalosporin antibiotic.¹ In vitro, TAK-599 inhibits growth of S. pneumoniae, S. aureus, methicillin-resistant S. aureus (MRSA), E. coli, and K. pneumoniae (MICs = 0.008-2 mg/L).² It is rapidly converted to T-91825 in rats and monkeys.¹ TAK-599 has bacteriostatic effects in mice infected with S. pneumoniae, S. aureus, MRSA, E. coli, or K. pneumoniae when administered at doses ranging from 0.2-234 mg/kg per day and also decreases the number of CFUs in a mouse model of thigh infection.² It exhibits a protective effect against systemic infection by clinical MRSA isolates in mice (ED₅₀s = 1.08-4.81 mg/kg).³

1.Ishikawa, T., Matsunaga, N., Tawada, H., et al.TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: Synthesis, physicochemical and pharmacological propertiesBioorg. Med. Chem.11(11)2427-2437(2003) 2.Andes, D., and Craig, W.A.Pharmacodynamics of a new cephalosporin, PPI-0903 (TAK-599), active against methicillin-resistant Staphylococcus aureus in murine thigh and lung infection models: Identification of an in vivo pharmacokinetic-pharmacodynamic targetAntimicrob. Agents Chemother.50(4)1376-1383(2006) 3.Iizawa, Y., Nagai, J., Ishikawa, T., et al.In vitro antimicrobial activity of T-91825, a novel anti-MRSA cephalosporin, and in vivo anti-MRSA activity of its prodrug, TAK-599J. Infect. Chemother.10(3)146-156(2004)