Ceftaroline

Ceftaroline (T-91825) is a cephalosporin compound and the active form of Ceftaroline fosamil (HY-14737). Ceftaroline exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and some anaerobic bacteria. Ceftaroline binds to penicillin-binding proteins 2 and 2A, thereby inhibiting the synthesis of bacterial peptidoglycan and cell wall, and acts as a bactericide, synergist, and resistance inhibitor. Ceftaroline can be used in research related to complicated skin and soft tissue infections, community-acquired pneumonia, Enterococcus faecalis infective endocarditis, and bacterial infections^[1][2][3][4]. In Vitro:Ceftaroline (T-91825) in combination with Daptomycin (HY-B0108) exhibits synergistic in vitro activity against all tested endocarditis-associated HLAR and non-HLAR Enterococcus faecalis isolates at standard initial inoculum, prevents daptomycin resistance development, and shows bactericidal activity against two HLAR strains^[2].
Ceftaroline (1/4-4 MIC; 6-24 h) exhibits rapid, potent bactericidal activity against MRSA strains OFU4 and TY6242 at concentrations of 2 MIC and higher, reducing viable cell counts significantly over 24 h^[4]. In Vivo:Ceftaroline (T-91825), delivered via its prodrug TAK-599 (Ceftaroline fosamil) (HY-14737) (1.08-4.81 mg/kg; s.c.; single dose; 1 hour post bacterial challenge), exhibits comparable or superior in vivo efficacy against systemic MRSA infection in mice, with ED₅₀ values ranging from 1.08 mg/kg to 4.81 mg/kg^[4].
Ceftaroline, delivered via its prodrug TAK-599 (20 mg/kg; s.c.; three times daily; starting 2 hours post infection or day 1 and day 2 post infection), significantly reduces MRSA bacterial counts in the lungs of neutropenic mice, even when treatment is initiated at a late stage of infection^[4].
Ceftaroline, delivered via its prodrug TAK-599 (20 mg/kg; s.c.; three doses; at 2, 20, and 26 hours post infection), reduces MRSA bacterial counts in mouse thigh muscle to 0.1% or less of control levels^[4].