Drug intelligence / Profile preview

linezolid + ceftazidime

Development stage
Preclinical
Lead developer
Pfizer
Modality
Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Linezolid + ceftazidime is a combination of two antibiotics used for their complementary antibacterial spectra. Linezolid is a synthetic oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S ribosomal subunit, thereby preventing formation of the functional 70S initiation complex essential for bacterial reproduction. It is primarily effective against Gram-positive bacteria, including resistant strains such as MRSA and VRE[2][6][8]. Ceftazidime is a third-generation cephalosporin beta-lactam antibiotic that exerts its bactericidal effect by inhibiting penicillin-binding proteins (PBPs), disrupting cell wall synthesis in susceptible bacteria, with strong activity against Gram-negative organisms[3]. The combination may be considered in clinical scenarios where both Gram-positive and Gram-negative coverage are required; however, studies indicate no significant synergistic or antagonistic interaction between these agents when used together[1][4]. This combination has been explored in fixed-dose formulations for broad-spectrum antibacterial therapy[4].

02

Targets

PBP2 (Penicillin-binding protein 2)PBP1A (Penicillin-binding protein 1A)23S rRNA (23S ribosomal RNA)PBP1b (Penicillin-binding protein 1B)

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