Linezolid is an oxazolidinone antibiotic used to treat infections by susceptible strains of aerobic Gram-positive bacteria. Its effects are bacteriostatic against both enterococci and staphylococci and bactericidal against most isolates of streptococci.
- Mechanism
- Curator reviewed · 3 references
Linezolid exerts its antibacterial effects by interfering with bacterial protein translation. It binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is essential for bacterial reproduction, thereby preventing bacteria from dividing.
Point mutations in the bacterial 23S rRNA can lead to linezolid resistance, and the development of linezolid-resistant Enterococcus faecium and Staphylococcus aureus have been documented during its clinical use. As antimicrobial susceptibility patterns are geographically distinct, local antibiograms should be consulted to ensure adequate coverage of relevant pathogens prior to use.
- Primary indication
- Linezolid is indicated in adults and children for the treatment of infections caused by susceptible Gram-positive bacteria, including nosocomial pneumonia, community-acquired pneumonia, skin and skin structure infections, and vancomycin-resistant Enterococcus faecium infections.Curator reviewed · 11 structured indications
- Formula / weight
- C16H20FN3O4 · 337.3461 g/mol (avg)
- First approval
- Canada, 2003 · United States, 2000
- Code names
- INF 0026 · PNU 100766 · U 100 · U-100,766 · U 766
- Brand names
Resolves to
TYZROVQLWOKYKF-ZDUSSCGKSA-NSMILESCC(=O)NC[C@H]1CN(C(=O)O1)C1=CC(F)=C(C=C1)N1CCOCC1What you can answer from here — as of September 23, 2026
Which other approved drugs treat the same conditions as Linezolid, and which companies have late-stage candidates in those indications?
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