Activity of β-lactam plus β-lactam-enhancer combination cefepime/zidebactam against Klebsiella pneumoniae harbouring defective OmpK35/36 porins and carbapenemases

Diagn Microbiol Infect Dis. 2021 Oct;101(2):115481. doi: 10.1016/j.diagmicrobio.2021.115481. Epub 2021 Jul 9.

Abstract

Cefepime/zidebactam is a β-lactam/β-lactam-enhancer based novel antibiotic which is in clinical development for treating infections caused by multidrug-resistant Gram-negative bacteria. Here, in vitro activity of cefepime/zidebactam was determined against multicentre Klebsiella pneumoniae clinical isolates co-expressing serine and/or metallo-carbapenemases and defective OmpK35 and OmpK36 porins. The MICs were determined using the reference broth microdilution method. Outer membrane protein expression was assessed using SDS-PAGE and mutations in the genes encoding OmpK35 and OmpK36 were identified by DNA sequencing. Among 34 isolates studied, carbapenemase genes, blaKPC and blaOXA-48-like, were present in 18 and 11 isolates, respectively; 5 isolates harboured both blaOXA-48-like and blaNDM. Point mutations, insertions, and duplications in OmpK35 and OmpK36, which are known to impact the activity of carbapenems, were detected. Against these isolates, cefepime/zidebactam (1:1) showed a consistent activity (MICs ≤4 mg/L). In conclusion, cefepime/zidebactam overcomes enzymatic, and non-enzymatic carbapenem-impacting resistance mechanisms concurrently expressed in K. pneumoniae.

Keywords: Carbapenemases; Klebsiella pneumoniae; Outer membrane porins; Zidebactam; β-lactam enhancer.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Azabicyclo Compounds / pharmacology
  • Bacterial Proteins / antagonists & inhibitors*
  • Bacterial Proteins / genetics*
  • Bacterial Proteins / metabolism
  • Carbapenems / pharmacology
  • Cephalosporins / pharmacology
  • Cyclooctanes / pharmacology
  • Drug Resistance, Multiple, Bacterial
  • Humans
  • Klebsiella Infections / drug therapy*
  • Klebsiella Infections / microbiology
  • Klebsiella pneumoniae / drug effects
  • Klebsiella pneumoniae / enzymology*
  • Klebsiella pneumoniae / genetics
  • Microbial Sensitivity Tests
  • Mutation
  • Porins / genetics*
  • Porins / metabolism
  • beta-Lactamases / genetics
  • beta-Lactamases / metabolism
  • beta-Lactams / pharmacology

Substances

  • Anti-Bacterial Agents
  • Azabicyclo Compounds
  • Bacterial Proteins
  • Carbapenems
  • Cephalosporins
  • Cyclooctanes
  • OmpK35 porin, Klebsiella pneumoniae
  • OmpK36 protein, Klebsiella pneumoniae
  • Porins
  • WCK 5222
  • beta-Lactams
  • beta-Lactamases
  • carbapenemase