In Vitro and In Vivo Activities of Contezolid (MRX-I) against Mycobacterium tuberculosis

Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00493-18. doi: 10.1128/AAC.00493-18. Print 2018 Aug.

Abstract

The in vitro activity of contezolid (MRX-I) against clinical isolates of Mycobacterium tuberculosis was evaluated using a microtiter broth dilution assay. MRX-I was as effective as linezolid (LZD) in vitro MRX-I and LZD were subsequently studied in BALB/c mice infected intranasally with M. tuberculosis Erdman. MRX-I and LZD at 100 mg/kg significantly reduced the bacterial load in lungs compared to the untreated early and late controls.

Keywords: Mycobacterium tuberculosis; in vitro; mouse model; oxazolidinones.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / pharmacology*
  • Bacterial Load / drug effects
  • Disease Models, Animal
  • Drug Administration Schedule
  • Female
  • Humans
  • Isoniazid / pharmacology
  • Linezolid / pharmacology
  • Lung / drug effects
  • Lung / microbiology
  • Mice
  • Mice, Inbred BALB C
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / growth & development
  • Mycobacterium tuberculosis / isolation & purification
  • Oxazolidinones / pharmacology*
  • Pyridones / pharmacology*
  • Tetrazoles / pharmacology
  • Tuberculosis, Multidrug-Resistant / drug therapy*
  • Tuberculosis, Multidrug-Resistant / microbiology

Substances

  • Antitubercular Agents
  • Oxazolidinones
  • PNU-100480
  • Pyridones
  • Tetrazoles
  • tedizolid
  • contezolid
  • Linezolid
  • Isoniazid