In vitro and in vivo activity of clofazimine against Mycobacterium tuberculosis persisters

Int J Tuberc Lung Dis. 2012 Aug;16(8):1119-25. doi: 10.5588/ijtld.11.0752. Epub 2012 Jun 12.

Abstract

Objective: To assess the activity of clofazimine (CFZ) against Mycobacterium tuberculosis persisters using an oxygen depletion model and a low-dose aerosol mouse model of chronic tuberculosis (TB).

Design: In in vitro experiments, CFZ showed much better activity than isoniazid under anaerobic conditions. In a low-dose aerosol mouse model of TB, we evaluated the efficacy of CFZ and moxifloxacin at different doses following treatment durations of 30, 60 and 90 days.

Results: CFZ showed significant bactericidal activity in the mouse model over the wide dose range of 2-200 mg/kg. CFZ activity was dose-dependent. The bacilli were eradicated in the CFZ 200 mg/kg group after treatment for 60 days, and in the CFZ 20 mg/kg group after 90 days of treatment.

Conclusion: CFZ exhibits dose-dependent, sustained bactericidal activity against M. tuberculosis persisters, and thus warrants further study to demonstrate its potential to contribute significantly in a novel treatment-shortening regimen.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / blood
  • Antitubercular Agents / pharmacology*
  • Aza Compounds / pharmacology
  • Chronic Disease
  • Clofazimine / blood
  • Clofazimine / pharmacology*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Resistance, Bacterial
  • Fluoroquinolones
  • Isoniazid / pharmacology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Microbial Sensitivity Tests
  • Moxifloxacin
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / genetics
  • Mycobacterium tuberculosis / growth & development
  • Mycobacterium tuberculosis / isolation & purification
  • Quinolines / pharmacology
  • Rifampin / pharmacology
  • Time Factors
  • Tuberculosis, Pulmonary / diagnosis
  • Tuberculosis, Pulmonary / drug therapy*
  • Tuberculosis, Pulmonary / microbiology

Substances

  • Antitubercular Agents
  • Aza Compounds
  • Fluoroquinolones
  • Quinolines
  • Clofazimine
  • Moxifloxacin
  • Isoniazid
  • Rifampin