Drug intelligence / Profile preview

ceftaroline fosamil + avibactam

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Ceftaroline fosamil + avibactam is a fixed-dose combination of two antibacterial agents. Ceftaroline fosamil is a prodrug that, once converted to its active form (ceftaroline), acts as a broad-spectrum fifth-generation cephalosporin antibiotic with potent activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and some Gram-negative organisms. Its mechanism involves binding to penicillin-binding proteins (PBPs), notably PBP2a and others, thereby inhibiting bacterial cell wall synthesis and leading to cell death[1][5]. Avibactam is a non-beta-lactam beta-lactamase inhibitor that protects ceftaroline from degradation by certain beta-lactamases produced by resistant bacteria. Avibactam inhibits Ambler class A (including ESBLs and KPC), class C (AmpC), and some class D (OXA-like) enzymes through reversible covalent inhibition[1][6]. The combination significantly expands the spectrum of activity of ceftaroline against resistant Gram-negative pathogens. This drug has been developed for serious bacterial infections, particularly those caused by multidrug-resistant organisms[2].

Other names
ceftaroline fosamil/NXL 104
02

Targets

PBP2a (Penicillin-binding protein 2a (Streptococcus pneumoniae))Class A BL (Class A beta-lactamase)PBP1A (Penicillin-binding protein 1A)PBP2B (Penicillin-binding protein 2B)AmpC (AmpC beta-lactamase)PBP2/3 (Penicillin-binding proteins 2 and 3)

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