Ceftaroline

Summary

Ceftaroline (CHEMBL4594371) is an approved small-molecule antibacterial drug; indicated across 6 conditions including bacterial infectious disease and pneumonia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 21
• Chemistry: 604.7 Da · C22H20N8O5S4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4594371
Name	Ceftaroline
Type	Small molecule
Max phase	3
FDA approved	yes
PubChem CID	9938701
ChEBI	CHEBI:70729
Molecular formula	C22H20N8O5S4
Molecular weight	604.7
InChIKey	RGFBRLNVZCCMSV-BIRGHMBHSA-N

SMILES: CCO/N=C(/C1=NSC(=N1)N)\C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)SC4=NC(=CS4)C5=CC=[N+](C=C5)C)C(=O)[O-]

IUPAC name: (6R,7R)-7-[[(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-ethoxyiminoacetyl]amino]-3-[[4-(1-methylpyridin-1-ium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

ChEBI definition: A cephalosporin that is the active metabolite of the prodrug ceftaroline fosamil. Used for the treatment of adults with acute bacterial skin and skin structure infections.

Pharmacological roles (ChEBI): antibacterial drug, antimicrobial agent.

Other ChEBI roles (chemical / environmental): drug metabolite.

Also known as: Ceftaroline, T 91825, T-91825, CEFTAROLINE, ceftaroline

Patent coverage: 718 distinct patent families (1,532 SureChEMBL compound mentions), from 1 matched compound structure(s). 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

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

Indications & clinical

Indications

6 indications (0 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	3	MONDO:0005113	EFO:0000771
pneumonia	3	MONDO:0005249	EFO:0003106
influenza	3	MONDO:0005812	EFO:0007328
bacterial pneumonia	3	MONDO:0004652	EFO:1001272
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096

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

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE4	10
PHASE1	6
PHASE3	4
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01524302	PHASE4	COMPLETED	Pharmacodynamic of Ceftaroline and Levofloxacin Against Pathogens Associated With Community Acquired Bacterial Pneumonia
NCT01734694	PHASE4	TERMINATED	Safety and Efficacy of Strategy to Prevent Drug-Induced Nephrotoxicity in High-Risk Patients
NCT02005068	PHASE4	WITHDRAWN	Ceftaroline in the Treatment of Bone and Joint Infections
NCT02307006	PHASE4	UNKNOWN	The Use of Ceftaroline as Surgical Prophylaxis in Surgery With Risk of MRSA Infection
NCT02582203	PHASE4	COMPLETED	Clinical and Economic Outcomes of Ceftaroline Fosamil for ABSSSI Documented or at Risk of MRSA
NCT02660346	PHASE4	COMPLETED	IL-10 Stratifying Tool for Towards Antibiotic Selection for MRSaB
NCT02937181	PHASE4	UNKNOWN	Antibiotic Prophylaxis in Open Fractures
NCT03771313	PHASE4	COMPLETED	Pharmacokinetic and Pharmacodynamic Analysis of Ceftaroline in Children and Adolescents With Cystic Fibrosis
NCT05156437	PHASE4	TERMINATED	Postoperative Antibiotic Management Duration Following Surgery for Intravenous Drug Abuse (IVDA) Endocarditis (OPTIMAL)
NCT05977868	PHASE4	TERMINATED	Comparing Oral Versus Parenteral Antimicrobial Therapy
NCT02735707	PHASE3	RECRUITING	Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia
NCT00423657	PHASE3	COMPLETED	Comparative Study of Ceftaroline vs. Vancomycin Plus Aztreonam in Adult Subjects With Complicated Skin Infections
NCT00424190	PHASE3	COMPLETED	Comparative Study of Ceftaroline vs. Vancomycin Plus Aztreonam in Adult Subjects With Complicated Skin Infections
NCT01371838	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of Intravenous Ceftaroline Versus Intravenous Ceftriaxone in the Treatment of Adult Hospitalised Patients With Community-Acquired Bacterial Pneumonia in Asia
NCT00633152	PHASE2	COMPLETED	Efficacy and Safety of Ceftaroline Versus Linezolid in Subjects With Complicated Skin and Skin Structure Infections
NCT00633126	PHASE1	COMPLETED	Pharmacokinetics of Ceftaroline in Subjects 12 to 17 Years of Age
NCT01290900	PHASE1	COMPLETED	A Single-centre, Randomised, Double-blind, Placebo-controlled, Four Way Crossover Phase I Study to Investigate the Effect on QT/QTc Interval of Ceftazidime NXL104 or Ceftaroline Fosamil NXL104, Compared With Placebo, Using Moxifloxacin (Avelox®) as a Positive Control, in Healthy Male Volunteers
NCT01458743	PHASE1	COMPLETED	Ceftaroline China Pharmacokinetics Study
NCT01648127	PHASE1	COMPLETED	Pharmacokinetics of Ceftaroline in Normal and Obese Subjects
NCT02600793	PHASE1	UNKNOWN	Ceftaroline Diffusion Into Cerebrospinal Fluid of Children
NCT03025841	PHASE1	COMPLETED	Population Pharmacokinetic (PK) Study of Zinforo (Ceftaroline) in Critical Care Patients With Early-onset Pneumonia and Normal or Augmented Renal Clearance

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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