Ceftaroline hydrochloride is a cephalosporin compound and the active form of Ceftaroline fosamil. Ceftaroline hydrochloride exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and some anaerobic bacteria. Ceftaroline hydrochloride 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 hydrochloride 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 Vivo, Ceftaroline hydrochloride (T-91825 hydrochloride), delivered via its prodrug TAK-599 (Ceftaroline fosamil) (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 hydrochloride, 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 hydrochloride, 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].
In Vitro, Ceftaroline hydrochloride (T-91825 hydrochloride) in combination with Daptomycin 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 (6-24 h) hydrochloride 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].
References:
[1]. Matzneller P, et al. Single- and Repeated-Dose Pharmacokinetics of Ceftaroline in Plasma and Soft Tissues of Healthy Volunteers for Two Different Dosing Regimens of Ceftaroline Fosamil. Antimicrobial agents and chemotherapy. 2016 Jun;60(6):3617-25.
[2]. Cañas MA, et al. In vitro and in vivo activity of daptomycin plus ceftaroline for the treatment of experimental endocarditis due to Enterococcus faecalis with and without high-level aminoglycoside resistance. The Journal of antimicrobial chemotherapy. 2026 Apr 03;81(5):dkag136.
[3]. Sader HS, et al. Antimicrobial activity and spectrum of PPI-0903M (T-91825), a novel cephalosporin, tested against a worldwide collection of clinical strains. Antimicrobial agents and chemotherapy. 2005 Aug;49(8):3501-12.
[4]. Iizawa Y, et al. In vitro antimicrobial activity of T-91825, a novel anti-MRSA cephalosporin, and in vivo anti-MRSA activity of its prodrug, TAK-599. Journal of infection and chemotherapy: official journal of the Japan Society of Chemotherapy. 2004 Jun;10(3):146-56.
In Vivo, Ceftaroline hydrochloride (T-91825 hydrochloride), delivered via its prodrug TAK-599 (Ceftaroline fosamil) (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 hydrochloride, 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 hydrochloride, 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].
In Vitro, Ceftaroline hydrochloride (T-91825 hydrochloride) in combination with Daptomycin 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 (6-24 h) hydrochloride 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].
References:
[1]. Matzneller P, et al. Single- and Repeated-Dose Pharmacokinetics of Ceftaroline in Plasma and Soft Tissues of Healthy Volunteers for Two Different Dosing Regimens of Ceftaroline Fosamil. Antimicrobial agents and chemotherapy. 2016 Jun;60(6):3617-25.
[2]. Cañas MA, et al. In vitro and in vivo activity of daptomycin plus ceftaroline for the treatment of experimental endocarditis due to Enterococcus faecalis with and without high-level aminoglycoside resistance. The Journal of antimicrobial chemotherapy. 2026 Apr 03;81(5):dkag136.
[3]. Sader HS, et al. Antimicrobial activity and spectrum of PPI-0903M (T-91825), a novel cephalosporin, tested against a worldwide collection of clinical strains. Antimicrobial agents and chemotherapy. 2005 Aug;49(8):3501-12.
[4]. Iizawa Y, et al. In vitro antimicrobial activity of T-91825, a novel anti-MRSA cephalosporin, and in vivo anti-MRSA activity of its prodrug, TAK-599. Journal of infection and chemotherapy: official journal of the Japan Society of Chemotherapy. 2004 Jun;10(3):146-56.