Cefiderocol is a siderophore cephalosporin antibiotic with a catechol moiety on the 3-position side chain. It has in vitro activity against the non-fermenting Gram-negative bacteria causing urinary track infections. It combines a catechol-type siderophore and cephalosporin core with side chains similar to cefepime and ceftazidime.
|Mechanism of Action||Cefiderocol binds to iron enters the bacterial cell using the bacteria's own iron transport system. Cefiderocol acts by binding to and inhibiting penicillin-binding proteins (PBPs), preventing cell wall synthesis and ultimately causing death of the bacterial cell.
Cefiderocol can enter bacteria by binding to iron and using the bacteria's own iron-transport system to evade the bacterial porin channels. The concept of carrying compounds into other cells has been liked to the 'Trojan horse' and the siderophore technology is being explored in
|Spectrum||The utility of siderophore antibiotics by virtue of their activity are effective against an array of ESBLs . It can also enter cells by passive diffusion through porin channels and is stable against all known classes of β-lactamases. Cefiderocol has vitro and vivo activity against Gram-negative bacteria including MDR Gram-negative pathogens, including carbapenem-resistant strains of Enterobacteriaceae, Pseudomonas aeruginosa, Acinetobacter baumannii, and Klebsiella pneumoniae.|
|Microbiology Applications||Cefiderocol (S-649266), a novel siderophore cephalosporin conjugated with a catechol moiety, has a characteristic antibacterial spectrum with a potent activity against a broad range of aerobic Gram-negative bacterial species, including carbapenem-resistant strains of Enterobacteriaceae and nonfermenting bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii. Cefiderocol has affinity mainly for penicillin-binding protein 3 (PBP3) of Enterobacteriaceae and nonfermenting bacteria similar to that of Ceftazidime.|
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Ito A et al (2017) In vitro antibacterial properties of Cefiderocol, a novel siderophore cephalosporin, against Gram-negative bacteria. Antimicrob. Agents Chemother. 62(1). pii: e01454-17 PMID 29061741
Jean SS, Hsueh SC, Lee WS, Hsueh PR (2019) Cefiderocol: a promising antibiotic against multidrug-resistant Gram-negative bacteria. Expert Rev Anti Infect Ther.17(5):307-309. PMID: 31055983
Katsube T et al (2017) Cefiderocol, a siderophore cephalosporin for Gram-negative bacterial infections: Pharmacokinetics and safety in subjects with renal impairment. J. Clin. Pharmacol. 57(5):584-591 PMID 27874971
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