Drug intelligence / Profile preview

ceftaroline + vancomycin

Development stage
Preclinical
Lead developer
Allergan
Modality
Small Molecules
Administration
Intravenous
01

Overview

Ceftaroline + vancomycin is a combination of two intravenous antibiotics used primarily as salvage therapy for persistent or complicated methicillin-resistant Staphylococcus aureus (MRSA) bacteremia and endocarditis. Ceftaroline is a fifth-generation cephalosporin with activity against MRSA, acting by binding to penicillin-binding proteins and inhibiting bacterial cell wall synthesis. Vancomycin is a glycopeptide antibiotic that inhibits cell wall biosynthesis in Gram-positive bacteria by binding to D-alanyl-D-alanine termini of cell wall precursors, preventing peptidoglycan polymerization. The combination has been explored for synergy in cases where monotherapy fails, particularly in severe or persistent MRSA infections[1][10][7]. While some studies suggest rapid clearance of bacteremia and high microbiological cure rates with this regimen, clinical outcomes such as mortality and recurrence are not consistently superior to monotherapy[1][10]. Both drugs are administered intravenously and require monitoring for adverse effects such as nephrotoxicity (vancomycin) and rash or neutropenia (ceftaroline)[10].

02

Targets

PBP3 (Peptidoglycan D,D-transpeptidase FtsI)D-Ala-D-Ala (D-Ala-D-Ala terminus)PBP2a (Penicillin-binding protein 2a (Streptococcus pneumoniae))PBP4 (Penicillin-binding protein 4)

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