Side-by-Side Profiling of Oxazolidinones to Estimate the Therapeutic Window against Mycobacterial Infections

Antimicrob Agents Chemother. 2023 Apr 18;67(4):e0165522. doi: 10.1128/aac.01655-22. Epub 2023 Mar 15.

Abstract

New oxazolidinones are in clinical development for the treatment of tuberculosis and nontuberculous mycobacterial (NTM) infections, as a replacement for linezolid and tedizolid, which cause mitochondrial toxicity after prolonged treatment. Here, we carried out side-by-side measurements of mitochondrial protein synthesis inhibition and activity against clinically relevant mycobacterial pathogens of approved and novel oxazolidinones. We found a large range of selectivity indices suggesting TBI-223 and sutezolid as promising candidates against tuberculosis and NTM lung disease caused by Mycobacterium kansasii.

Keywords: mitochondrial toxicity; nontuberculous mycobacteria; oxazolidinone; tuberculosis.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use
  • Humans
  • Linezolid / pharmacology
  • Linezolid / therapeutic use
  • Mycobacterium Infections, Nontuberculous* / drug therapy
  • Mycobacterium Infections, Nontuberculous* / microbiology
  • Nontuberculous Mycobacteria
  • Oxazolidinones* / pharmacology
  • Oxazolidinones* / therapeutic use
  • Tuberculosis* / drug therapy

Substances

  • Anti-Bacterial Agents
  • Oxazolidinones
  • Linezolid