Cefiderocol

Summary

Cefiderocol (CHEMBL3989974) is an approved small-molecule antibacterial drug (ATC J01DI04); indicated across 7 conditions including bacterial infectious disease and pneumonia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01DI04
• Indications: 7 conditions
• Clinical trials: 19
• Chemistry: 752.2 Da · C30H34ClN7O10S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3989974
Name	Cefiderocol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	77843966
ChEBI	CHEBI:140376
ATC	J01DI04
Molecular formula	C30H34ClN7O10S2
Molecular weight	752.2
InChIKey	DBPPRLRVDVJOCL-FQRUVTKNSA-N

SMILES: CC(C)(C(=O)O)O/N=C(/C1=CSC(=N1)N)\C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C[N+]4(CCCC4)CCNC(=O)C5=C(C(=C(C=C5)O)O)Cl)C(=O)[O-]

IUPAC name: (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(2-carboxypropan-2-yloxyimino)acetyl]amino]-3-[[1-[2-[(2-chloro-3,4-dihydroxybenzoyl)amino]ethyl]pyrrolidin-1-ium-1-yl]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

ChEBI definition: A fourth-generation siderophore cephalosporin antibiotic having {1-[2-(2-chloro-3,4-dihydroxybenzamido)ethyl]pyrrolidinium-1-yl}methyl and [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-{[(2-carboxypropan-2-yl)oxy]imino}acetyl]amino side groups located at positions 3 and 7 respectively, developed to combat a variety of bacterial pathogens, including β-lactam- and carbapenem-resistant organisms.

Pharmacological roles (ChEBI): antibacterial drug, siderophore.

Also known as: Cefiderocol, GSK-2696266, GSK2696266, RSC-649266, RSC649266, S-649266, S649266, CEFIDEROCOL

Parent form; salt/anhydrous children: CHEMBL4297211, CHEMBL5568852, CHEMBL5572971

Patent coverage: 185 distinct patent families (387 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 386 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Voltage-gated inwardly rectifying potassium channel KCNH2.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KCNH2	7.38	IC50	42	nM	CHEMBL_ACT_25984172

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

7 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
bacterial infectious disease	4	MONDO:0005113	EFO:0000771
pneumonia	3	MONDO:0005249	EFO:0003106
urinary tract infection	2	MONDO:0100338	EFO:0003103
gram-negative bacterial infections	2	MONDO:0021678	MONDO:0021678
bacterial pneumonia	1	MONDO:0004652	EFO:1001272

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 19.

Phase distribution

Phase	Trials
PHASE1	6
PHASE2	5
PHASE4	4
PHASE3	2
Not specified	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05922124	PHASE4	RECRUITING	Cefiderocol and Ampicillin-sulbactam vs. Colistin +/- Meropenem for Carbapenem Resistant A. Baumannii
NCT07004049	PHASE4	RECRUITING	Optimising TREATment for Severe Gram-Negative Bacterial Infections
NCT07465432	PHASE4	RECRUITING	Pharmacokinetic Analysis of Cefiderocol in Patients With Acute Burn Injuries
NCT05314764	PHASE4	COMPLETED	Cefiderocol Pharmacokinetics in Adult Patients With Cystic Fibrosis
NCT02714595	PHASE3	COMPLETED	Study of Cefiderocol (S-649266) or Best Available Therapy for the Treatment of Severe Infections Caused by Carbapenem-resistant Gram-negative Pathogens
NCT03032380	PHASE3	COMPLETED	Clinical Study of Cefiderocol (S-649266) for the Treatment of Nosocomial Pneumonia Caused by Gram-negative Pathogens
NCT02321800	PHASE2	COMPLETED	A Study of Efficacy and Safety of Intravenous Cefiderocol (S-649266) Versus Imipenem/Cilastatin in Complicated Urinary Tract Infections
NCT03869437	PHASE2	COMPLETED	RCT Cefiderocol vs BAT for Treatment of Gram Negative BSI
NCT04215991	PHASE2	COMPLETED	A Study to Assess the Safety, Tolerability, and Pharmacokinetics of Cefiderocol in Hospitalized Pediatric Participants
NCT04335539	PHASE2	COMPLETED	A Study to Assess the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses of Cefiderocol in Hospitalized Pediatric Participants
NCT06086626	PHASE2	COMPLETED	A Study to Assess the Safety, Tolerability, and Pharmacokinetics of Cefiderocol in Hospitalized Neonates and Infants
NCT07104162	PHASE1	RECRUITING	A Study to Investigate Safety and Pharmacokinetics of Intravenous Cefiderocol/Xeruborbactam in Participants With Renal Impairment
NCT03862040	PHASE1	TERMINATED	Cefiderocol Concentrations in the Lungs of Hospitalized Patients With Bacterial Pneumonia
NCT04995835	PHASE1	COMPLETED	Cefiderocol PK in Patients on ECMO
NCT05373615	PHASE1	COMPLETED	Cefiderocol Plasma Concentrations in Patients Receiving Renal Replacement Therapy
NCT05395104	PHASE1	COMPLETED	A Study to Assess the Effect of Cefiderocol on the Pharmacokinetics (PK) of Midazolam in Healthy Participants
NCT06547554	PHASE1	COMPLETED	A DDI Study to Investigate PK and Safety of Cefiderocol in Combination With Xeruborbactam in Healthy Adult Participants
NCT03780140	Not specified	APPROVED_FOR_MARKETING	Expanded Access to Cefiderocol for the Intravenous Treatment of Severe Gram Negative Bacterial Infections
NCT05789199	Not specified	COMPLETED	Use of Cefiderocol in the Management of Gram-Negative Infections

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).