A pairwise approach to revitalize β-lactams for the treatment of TB

Antimicrob Agents Chemother. 2024 Jun 5;68(6):e0003424. doi: 10.1128/aac.00034-24. Epub 2024 May 1.

Abstract

The dual β-lactam approach has been successfully applied to overcome target redundancy in nontuberculous mycobacteria. Surprisingly, this approach has not been leveraged for Mycobacterium tuberculosis, despite the high conservation of peptidoglycan synthesis. Through a comprehensive screen of oral β-lactam pairs, we have discovered that cefuroxime strongly potentiates the bactericidal activity of tebipenem and sulopenem-advanced clinical candidates-and amoxicillin, at concentrations achieved clinically. β-lactam pairs thus have the potential to reduce TB treatment duration.

Keywords: Mycobacterium tuberculosis; amoxicillin; cefuroxime; potentiation; sulopenem; tebipenem; β-lactam.

MeSH terms

  • Amoxicillin / pharmacology
  • Amoxicillin / therapeutic use
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use
  • Antitubercular Agents* / pharmacology
  • Antitubercular Agents* / therapeutic use
  • Carbapenems
  • Cefuroxime / therapeutic use
  • Drug Synergism
  • Humans
  • Microbial Sensitivity Tests*
  • Mycobacterium tuberculosis* / drug effects
  • Tuberculosis / drug therapy
  • beta-Lactams* / pharmacology
  • beta-Lactams* / therapeutic use

Substances

  • beta-Lactams
  • Antitubercular Agents
  • tebipenem
  • Amoxicillin
  • Cefuroxime
  • Anti-Bacterial Agents
  • Carbapenems