Cross-resistance between clofazimine and bedaquiline through upregulation of MmpL5 in Mycobacterium tuberculosis

Antimicrob Agents Chemother. 2014 May;58(5):2979-81. doi: 10.1128/AAC.00037-14. Epub 2014 Mar 3.

Abstract

The antileprosy drug clofazimine is also of interest for the treatment of multidrug-resistant tuberculosis. To understand possible resistance mechanisms, clofazimine-resistant Mycobacterium tuberculosis mutants were isolated in vitro, and, unexpectedly, found to be cross-resistant to bedaquiline. Mutations in the transcriptional regulator Rv0678, with concomitant upregulation of the multisubstrate efflux pump, MmpL5, accounted for this cross-resistance. Mutation in Rv0678 should therefore be considered a confounding factor for the treatment of tuberculosis with clofazimine or bedaquiline.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / pharmacology*
  • Clofazimine / pharmacology*
  • Diarylquinolines / pharmacology*
  • Drug Resistance, Multiple, Bacterial
  • Mycobacterium tuberculosis / drug effects*

Substances

  • Antitubercular Agents
  • Diarylquinolines
  • bedaquiline
  • Clofazimine