Cefiderocol: a novel siderophore cephalosporin

doi:10.12092/j.issn.1009-2501.2026.01.015

Abstract

Abstract:

Cefiderocol is the first-in-class siderophore cephalosporin. With its unique mechanism of action and high stability independent of β-lactamase inhibitor, Cefiderocol exhibits potent activity against multidrug-resistant gram-negative bacilli or carbapenem-resistant gram-negative bacilli, making it an important choice for the treatment of such pathogens in current clinical practice. This article provides a review of its mechanism of action, antibacterial activity, pharmacokinetics/pharmacodynamics, clinical research, safety, and resistance mechanisms, in order to provide reference for clinical anti drug-resistance gram-negative bacilli infections.

Key words: cefiderocol, siderophore, β-lactams, multidrug-resistant gram-negative bacilli, carbapenem-resistant gram-negative bacilli

CLC Number:

R969

Shifeng ZHAO, Hengbin CAO, Ronghua WANG, Yumei YUAN. Cefiderocol: a novel siderophore cephalosporin[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2026, 31(1): 133-144.

Figures/Tables 6

References 57

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Organisms	MIC breakpoint (μg/mL)
	CLSI			FDA			EUCAST
	S	I	R	S	I	R	S	R
Enterobacterales*	≤4	8	≥16	≤4	8	≥16	≤2	>2
Pseudomonas aeruginosa	≤4	8	≥16	≤1	2	≥4	≤2	>2
Acinetobacter baumannii	≤4	8	≥16	≤1	2	≥4	IE	IE
Stenotrophomonas maltophilia	≤1	-	-	-	-	-	IE	IE

Organisms	MIC breakpoint (μg/mL)
	CLSI			FDA			EUCAST
	S	I	R	S	I	R	S	R
Enterobacterales*	≤4	8	≥16	≤4	8	≥16	≤2	>2
Pseudomonas aeruginosa	≤4	8	≥16	≤1	2	≥4	≤2	>2
Acinetobacter baumannii	≤4	8	≥16	≤1	2	≥4	IE	IE
Stenotrophomonas maltophilia	≤1	-	-	-	-	-	IE	IE

Organism (no. of isolates)	Antimicrobial agents	MIC (μg/mL)			CLSI MIC interpretation*
Organism (no. of isolates)	Antimicrobial agents	MIC₅₀	MIC₉₀	Range	% S	% I	% R
Enterobacterales (31896)	Cefiderocol	0.12	1	≤0.002 to >256	99.8	0.2	0.1
	Cefepime	≤0.12	16	≤0.06 to >64	85.9	3.0	11.2
	Ceftazidime-avibactam	0.12	0.5	≤0.03 to >64	99.2	NA	0.8
	Ceftolozane-tazobactam	0.25	2	≤0.06 to >64	91.7	1.8	6.6
	Ciprofloxacin	≤0.12	>8	≤0.06 to >8	74.5	3.2	22.3
	Meropenem	≤0.06	0.12	≤0.06 to >64	96.8	0.4	2.9
P. aeruginosa (7700)	Cefiderocol	0.12	0.5	≤0.002 to 8	99.9	0.1	0
	Cefepime	4	16	≤0.06 to >64	82.9	9.1	8.0
	Ceftazidime-avibactam	2	8	≤0.03 to >64	93.8	NA	6.2
	Ceftolozane-tazobactam	0.5	2	≤0.06 to >64	94.0	1.0	5.0
	Ciprofloxacin	0.25	>8	≤0.06 to >8	70.8	6.5	22.7
	Meropenem	0.5	16	≤0.06 to >64	77.2	5.8	17.0
A. baumannii complex (5225)	Cefiderocol	0.12	1	≤0.002 to >256	96.0	1.3	2.7
	Cefepime	8	>64	≤0.06 to >64	52.0	9.5	38.5
	Ceftazidime-avibactam	16	>64	≤0.06 to >64	NA	NA	NA
	Ceftolozane-tazobactam	8	>64	≤0.06 to >64	NA	NA	NA
	Ciprofloxacin	>8	>8	≤0.12 to >8	40.0	0.7	59.3
	Meropenem	16	>64	≤0.06 to >64	46.2	1.3	52.5

Organism (no. of isolates)	Antimicrobial agents	MIC (μg/mL)			CLSI MIC interpretation*
Organism (no. of isolates)	Antimicrobial agents	MIC₅₀	MIC₉₀	Range	% S	% I	% R
Enterobacterales (31896)	Cefiderocol	0.12	1	≤0.002 to >256	99.8	0.2	0.1
	Cefepime	≤0.12	16	≤0.06 to >64	85.9	3.0	11.2
	Ceftazidime-avibactam	0.12	0.5	≤0.03 to >64	99.2	NA	0.8
	Ceftolozane-tazobactam	0.25	2	≤0.06 to >64	91.7	1.8	6.6
	Ciprofloxacin	≤0.12	>8	≤0.06 to >8	74.5	3.2	22.3
	Meropenem	≤0.06	0.12	≤0.06 to >64	96.8	0.4	2.9
P. aeruginosa (7700)	Cefiderocol	0.12	0.5	≤0.002 to 8	99.9	0.1	0
	Cefepime	4	16	≤0.06 to >64	82.9	9.1	8.0
	Ceftazidime-avibactam	2	8	≤0.03 to >64	93.8	NA	6.2
	Ceftolozane-tazobactam	0.5	2	≤0.06 to >64	94.0	1.0	5.0
	Ciprofloxacin	0.25	>8	≤0.06 to >8	70.8	6.5	22.7
	Meropenem	0.5	16	≤0.06 to >64	77.2	5.8	17.0
A. baumannii complex (5225)	Cefiderocol	0.12	1	≤0.002 to >256	96.0	1.3	2.7
	Cefepime	8	>64	≤0.06 to >64	52.0	9.5	38.5
	Ceftazidime-avibactam	16	>64	≤0.06 to >64	NA	NA	NA
	Ceftolozane-tazobactam	8	>64	≤0.06 to >64	NA	NA	NA
	Ciprofloxacin	>8	>8	≤0.12 to >8	40.0	0.7	59.3
	Meropenem	16	>64	≤0.06 to >64	46.2	1.3	52.5

Organism	Genotype (no. of isolates)	MIC (μg/mL)			CLSI MIC interpretation
Organism	Genotype (no. of isolates)	MIC₅₀	MIC₉₀	Range	% S	% I	% R
Enterobacterales	MBL (211)^a	2	4	0.06 to 128	91.5	5.7	2.8
	VIM (113)^a	1	4	0.12 to 16	96.5	1.8	1.8
	NDM (96)^a	2	8	0.12 to 128	85.4	10.4	4.2
	KPC (382)^b	1	4	0.015 to 8	98.4	1.6	0
	OXA-48 group (256)^c	0.5	4	0.015 to 16	97.3	2.3	0.4
	Carbapenemase negative (154)^d	0.5	2	0.008 to 8	98.7	1.3	0
P. aeruginosa	MBL (227)^a	0.25	2	0.008 to 4	100	0	0
	VIM (200)^a	0.25	1	0.008 to 4	100	0	0
	IMP (25)^a	2	4	0.12 to 4	100	0	0
	GES (carbapenemase) (34)^e	0.25	1	0.06 to 1	100	0	0
	Carbapenemase negative (1497)^d	0.25	1	≤0.002 to 8	99.8	0.2	0
A. baumannii complex	MBL (25)^a	4	8	0.12 to >64	60.0	32.0	8.0
	OXA-23 group (1783)^f	0.25	2	≤0.002 to >256	95.6	1.9	2.6
	OXA-24 group (570)^f	0.5	8	0.004 to >256	89.5	1.9	8.6
	OXA-58 group (69)^f	1	1	0.06 to 4	100	0	0
	OXA-23and24 group (19)^f	0.5	2	0.06 to 2	100	0	0
	OXA-23and58 group (34)^f	0.25	0.5	0.06 to 0.5	100	0	0
	PER/VEB (103)^g	128	>256	0.12 to >256	15.5	10.7	73.8
	Carbapenemase negative (309)^d	0.25	2	0.008 to >256	95.5	2.6	1.9