In Vitro Evolution of Cefiderocol Resistance in an NDM-Producing Klebsiella pneumoniae Due to Functional Loss of CirA

Microbiol Spectr. 2021 Dec 22;9(3):e0177921. doi: 10.1128/Spectrum.01779-21. Epub 2021 Nov 10.

Abstract

By serially exposing an NDM-producing Klebsiella pneumoniae clinical strain to cefiderocol, we obtained a mutant with cefiderocol MIC of >128 μg/ml. The mutant contained an early stop codon in the iron transporter gene cirA, and its complementation fully restored susceptibility. The cirA-deficient mutant was competed out by the parental strain in vitro, suggesting reduced fitness. IMPORTANCE Cefiderocol, a newly approved cephalosporin agent with an extensive spectrum of activity against Gram-negative bacteria, is a siderophore cephalosporin that utilizes iron transporters to access the bacterial periplasm. Loss of functional CirA, an iron transporter, has been associated with cefiderocol resistance. Here, we show that such genetic change can be selected under selective pressure and cause high-level cefiderocol resistance, but with a high fitness cost. Whether these resistant mutants can survive beyond selective pressure will inform stewardship of this agent in the clinic.

Keywords: cefiderocol; iron transporter; siderophore.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence / genetics
  • Amino Acid Substitution / genetics
  • Anti-Bacterial Agents / pharmacology
  • Cation Transport Proteins / genetics*
  • Cefiderocol
  • Cephalosporins / pharmacology*
  • Codon, Nonsense / genetics
  • Drug Resistance, Multiple, Bacterial / genetics*
  • Frameshift Mutation / genetics
  • High-Throughput Nucleotide Sequencing
  • Klebsiella Infections / drug therapy
  • Klebsiella pneumoniae / drug effects
  • Klebsiella pneumoniae / genetics*
  • Klebsiella pneumoniae / metabolism
  • Microbial Sensitivity Tests
  • Siderophores / pharmacology
  • beta-Lactamases / genetics*

Substances

  • Anti-Bacterial Agents
  • Cation Transport Proteins
  • Cephalosporins
  • Codon, Nonsense
  • Siderophores
  • beta-Lactamases
  • beta-lactamase NDM-1