Tedizolid (TR-701): a new oxazolidinone with enhanced potency

Expert Opin Investig Drugs. 2012 Apr;21(4):515-22. doi: 10.1517/13543784.2012.660250. Epub 2012 Feb 13.

Abstract

Introduction: Tedizolid phosphate (TR-701) is a new oxazolidinone prodrug that is transformed in the serum into the active drug tedizolid (TR-700). Tedizolid acts by inhibiting protein synthesis and has broad activity against Gram-positive pathogens, including strains that are resistant to linezolid.

Areas covered: This review summarizes the currently available data on this new antimicrobial agent. In vitro activity, pharmacokinetics/pharmacodynamics, clinical efficacy and safety are all addressed.

Expert opinion: Tedizolid will provide a useful addition to the antimicrobial armamentarium, particularly in complicated skin and skin structure infections, due to its high oral bioavailability and once-daily dosing. The results of future studies will serve to better position tedizolid among the newly approved agents for infections caused by Gram-positive organisms.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use*
  • Clinical Trials as Topic
  • Gram-Positive Bacteria / drug effects
  • Humans
  • Oxazolidinones / pharmacokinetics
  • Oxazolidinones / pharmacology*
  • Oxazolidinones / therapeutic use*
  • Protein Synthesis Inhibitors / pharmacokinetics
  • Protein Synthesis Inhibitors / pharmacology
  • Protein Synthesis Inhibitors / therapeutic use
  • Randomized Controlled Trials as Topic
  • Tetrazoles / pharmacokinetics
  • Tetrazoles / pharmacology*
  • Tetrazoles / therapeutic use*

Substances

  • Anti-Bacterial Agents
  • Oxazolidinones
  • Protein Synthesis Inhibitors
  • Tetrazoles