Ceftriaxone

Summary

Ceftriaxone (CHEMBL161) is an approved small-molecule antibacterial drug (ATC J01DD04); indicated across 27 conditions including bacterial infectious disease and gonorrhea.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01DD04 (+1 more)
• Indications: 27 conditions
• Clinical trials: 115
• Chemistry: 554.6 Da · C18H18N8O7S3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL161
Name	Ceftriaxone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5479530
ChEBI	CHEBI:29007
ATC	J01DD04, J01DD54
Molecular formula	C18H18N8O7S3
Molecular weight	554.6
InChIKey	VAAUVRVFOQPIGI-SPQHTLEESA-N

SMILES: CN1C(=NC(=O)C(=O)N1)SCC2=C(N3[C@@H]([C@@H](C3=O)NC(=O)/C(=N\OC)/C4=CSC(=N4)N)SC2)C(=O)O

IUPAC name: (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(2-methyl-5,6-dioxo-1H-1,2,4-triazin-3-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

ChEBI definition: A third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.

Pharmacological roles (ChEBI): antibacterial drug, EC 3.5.2.6 (β-lactamase) inhibitor, drug allergen.

Also known as: Ceftriaxon, Ceftriaxona, Ceftriaxone, ceftriaxone, ceftrioxone, CEFTRIAXONE

Parent form; salt/anhydrous children: CHEMBL4101392, CHEMBL6067656

Patent coverage: 20,032 distinct patent families (71,135 SureChEMBL compound mentions), from 3 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: 9 (assay-derived). Sample: Solute carrier family 22 member 6, Organic anion transporter 3, Solute carrier family 22 member 11, Progesterone receptor, Peroxisome proliferator-activated receptor gamma, Nuclear receptor subfamily 1 group I member 2, Cytochrome P450 2J2, D-amino-acid oxidase, Alpha-synuclein.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC22A6	6.64	Ki	230	nM	CHEMBL_ACT_11002270
SNCA	6.28	Kd	530	nM	CHEMBL_ACT_22754689
NR1I2	6.21	AC50	620	nM	CHEMBL_ACT_25188351
PPARG	5.85	AC50	1400	nM	CHEMBL_ACT_25113995
NR1I2	5.8	AC50	1600	nM	CHEMBL_ACT_25223901
SLC22A11	5.62	Ki	2380	nM	CHEMBL_ACT_11002750
SLC22A8	5.36	Ki	4390	nM	CHEMBL_ACT_11003107
DAO	5	IC50	10000	nM	CHEMBL_ACT_15703079

Target pathways

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

Indications & clinical

Indications

27 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
gonorrhea	3	MONDO:0004277	DOID:7551
urinary tract infection	3	MONDO:0100338	EFO:0003103
pneumonia	3	MONDO:0005249	EFO:0003106
bacterial pneumonia	3	MONDO:0004652	EFO:1001272
Lyme disease	3	MONDO:0019632	EFO:0008510
infectious peritonitis	3	MONDO:0004522	EFO:0008588
influenza	3	MONDO:0005812	EFO:0007328
amyotrophic lateral sclerosis	3	MONDO:0004976	MONDO:0004976
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
endometritis	2	MONDO:0000918	EFO:1001312
pelvic inflammatory disease	2	MONDO:0000922	EFO:1001388
cholangitis	2	MONDO:0004789	HP:0030151
ulcerative colitis	2	MONDO:0005101	EFO:0000729
shigellosis	2	MONDO:0019345	EFO:0005585
appendicitis	2	MONDO:0005649	EFO:0007149
Parkinson disease	2	MONDO:0005180	MONDO:0005180
bipolar disorder	2	MONDO:0004985	MONDO:0004985
endocarditis	2	MONDO:0005025	EFO:0000465
Borrelia infectious disease	2	MONDO:0006681	EFO:1000842
schizoaffective disorder	1	MONDO:0005487	EFO:0005411
psychotic disorder	1	MONDO:0005485	EFO:0005407
osteomyelitis	0	MONDO:0005246	EFO:0003102

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

Clinical trials

Total trials: 115.

Phase distribution

Phase	Trials
PHASE4	37
PHASE3	26
PHASE2	21
Not specified	18
PHASE2/PHASE3	4
PHASE1	4
PHASE1/PHASE2	3
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06349122	PHASE4	NOT_YET_RECRUITING	Screen-and-treat Strategy for Vaginal Flora Abnormalities in Pregnant Women at High Risk of Preterm Birth
NCT06396078	PHASE4	RECRUITING	Improvement of PPROM Management With Prophylactic Antimicrobial Therapy (iPROMPT)
NCT06494072	PHASE4	RECRUITING	Short Versus Standard of Care Antibiotic Duration for Children Hospitalized for CAP
NCT07537413	PHASE4	NOT_YET_RECRUITING	Ceftriaxone Dosage for Non-Critical Community-Acquired Pneumonia
NCT00035347	PHASE4	COMPLETED	Intravenous Azithromycin Plus Intravenous Ceftriaxone Followed by Oral Azithromycin With Intravenous Levofloxacin Followed by Oral Levofloxacin for the Treatment of Moderate to Severely Ill Hospitalized Patients With Community Acquired Pneumonia
NCT00195351	PHASE4	COMPLETED	Study Comparing Tigecycline Versus Ceftriaxone Sodium Plus Metronidazole in Complicated Intra-abdominal Infection
NCT00358202	PHASE4	COMPLETED	Cefepime vs. Ceftriaxone to Treat Nursing Home-Acquired Pneumonia
NCT00374959	PHASE4	COMPLETED	Prevention of Pneumonia Comparing Ceftriaxone With Subglottic Aspiration
NCT00429975	PHASE4	TERMINATED	Ceftriaxone Vs Levofloxacin on Cytokine Expression in Pneumococcal Pneumonia
NCT00449800	PHASE4	UNKNOWN	Pharmacokinetic of Ceftriaxone in Septic ICU Patients
NCT00838864	PHASE4	COMPLETED	Comparison of 3 Days and 7 Days Intravenous Ceftriaxone Prophylaxis for Variceal Bleeding
NCT00895089	PHASE4	COMPLETED	Moxifloxacin Versus Ceftriaxone in the Treatment of Primary Pyogenic Liver Abscess
NCT01166932	PHASE4	COMPLETED	Comparison Between Amoxycillin/Clavulanic Acid and Oxacillin/Ceftriaxone for Community Acquired-pneumonia
NCT01265173	PHASE4	COMPLETED	Comparison of Efficacy of Cefotaxime, Ceftriaxone, and Ciprofloxacin for the Treatment of SBP in Patients With LC
NCT01278017	PHASE4	UNKNOWN	The Role of Short-course Ceftriaxone Therapy in the Treatment of Severe Nontyphoidal Salmonella Enterocolitis
NCT01390623	PHASE4	COMPLETED	Efficacy and Safety Study of Short-term Antibiotic for Pyelonephritis in Women
NCT01421693	PHASE4	COMPLETED	Gatifloxacin Versus Ceftriaxone in the Treatment of Enteric Fever
NCT01559753	PHASE4	COMPLETED	Early-onset Ventilator-associated Pneumonia in Adults: Comparison of 8 Versus 15 Days of Antibiotic Treatment
NCT01635530	PHASE4	COMPLETED	Study of Lyme Neuroborreliosis
NCT01659866	PHASE4	COMPLETED	Antibiotic Prophylaxis for Transrectal Prostate Biopsy
NCT01723150	PHASE4	COMPLETED	Antibiotics for Klebsiella Liver Abscess Study
NCT01745679	PHASE4	COMPLETED	Pharmacological Study of High Doses of Ceftriaxone in Meningitidis
NCT02224040	PHASE4	UNKNOWN	Typhoid Fever: Combined vs. Single Antibiotic Therapy
NCT02384200	PHASE4	COMPLETED	A Randomized Trial of Preoperative Prophylactic Antibiotics Prior to Kidney Stone Surgery (Percutaneous Nephrolithotomy [PCNL])
NCT03012360	PHASE4	TERMINATED	Antimicrobial Treatment in Patients With Ventilator-associated Tracheobronchitis
NCT03087656	PHASE4	UNKNOWN	Antibiotics to Decrease Post ERCP Cholangitis
NCT03179384	PHASE4	COMPLETED	Impact on the Intestinal Microbiota of Treatment With Ceftriaxone in Women’s Acute Community Pyelonephritis
NCT03560232	PHASE4	TERMINATED	Noninferiority Comparison of Prophylactic Open Fracture Antimicrobial Regimens
NCT03922919	PHASE4	UNKNOWN	Effect of Administration of 3rd Generation Cephalosporin on the Digestive Carrying of 3rd Generation Cephalosporin-resistant Enterobacteriaceae (CEF-IMPACT)
NCT04066621	PHASE4	COMPLETED	PHase IV Clinical Trial of Ceftriaxone Sodium and Sulbactam Sodium for Injection (CRO-SBT)
NCT04141787	PHASE4	UNKNOWN	Ceftriaxone as Home IV for Staph Infections
NCT04202068	PHASE4	COMPLETED	A Study Evaluating Efficacy and Safety of CRO-SBT in the Treatment of Gonorrhea
NCT04218695	PHASE4	COMPLETED	Prophylactic Antibiotics in Admitted Cirrhotics
NCT05079620	PHASE4	TERMINATED	Early Antibiotics After Aspiration in ICU Patients
NCT05156437	PHASE4	TERMINATED	Postoperative Antibiotic Management Duration Following Surgery for Intravenous Drug Abuse (IVDA) Endocarditis (OPTIMAL)
NCT05980871	PHASE4	TERMINATED	Treatment Responses of Early Syphilis to Ceftriaxone Plus Doxycycline
NCT06090565	PHASE4	COMPLETED	Cefixime Plus Doxycycline Compared to Ceftriaxone Plus Azithromycin for Treatment of Gonorrhoea
NCT02735707	PHASE3	RECRUITING	Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia
NCT06527989	PHASE2/PHASE3	NOT_YET_RECRUITING	Prophylactic Antibiotic in Subtalar Fusion Surgery
NCT06819592	PHASE3	RECRUITING	PRophylaxis Against Early VENTilator-associated Infections in Acute Brain Injury

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 9 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

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