Ofloxacin

Summary

Ofloxacin (CHEMBL4) is an approved small molecule (ATC J01MA01) targeting TAS2R9; indicated across 18 conditions including bacterial infectious disease and eye infectious disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: J01MA01 (+2 more)
• Targets: 1 (TAS2R9)
• Indications: 18 conditions
• Clinical trials: 221
• Chemistry: 361.4 Da · C18H20FN3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4
Name	Ofloxacin
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	4583
ChEBI	CHEBI:194135
ATC	J01MA01, S02AA16, S01AE01
Molecular formula	C18H20FN3O4
Molecular weight	361.4
InChIKey	GSDSWSVVBLHKDQ-UHFFFAOYSA-N

SMILES: CC1COC2=C3N1C=C(C(=O)C3=CC(=C2N4CCN(CC4)C)F)C(=O)O

IUPAC name: 7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid

ChEBI definition: An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.

Also known as: DL-8280, Exocin, Floxin, Floxin otic, HOE 280, HOE-280, J01MA01, NSC-727071, NSC-758178, Ocuflox, Ofloxacin, Ofloxacine

Parent form; salt/anhydrous children: CHEMBL556371

Patent coverage: 14,898 distinct patent families (47,798 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 47,043 (98%) 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	DNA gyrase subunit A		5.46
TAS2R9	TAS2R9	Agonist	3.7	0%	Q9NYW1

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Lysine-specific demethylase 4E, Streptokinase A, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], CAAX prenyl protease 1, GABA-A receptor; anion channel, DNA gyrase, Trypsin, Histamine H3 receptor, Albumin.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 20 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P0AES4	5.82	IC50	1500	nM	CHEMBL_ACT_3570429
P47154	5.71	AC50	1950	nM	CHEMBL_ACT_5983277
KDM4E	5.5	Potency	3162	nM	CHEMBL_ACT_3719533
HPGD	5.5	Potency	3162	nM	CHEMBL_ACT_4755669
P10520	5.43	EC50	3694	nM	CHEMBL_ACT_4945574
P00761	5.03	AC50	9264	nM	CHEMBL_ACT_5562895
HSD17B10	5	Potency	10000	nM	CHEMBL_ACT_3685152

Target pathways

Aggregated over 1 target gene(s): TAS2R9.

Top Reactome pathways

6 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	TAS2R9
Signaling by GPCR	1	TAS2R9
GPCR downstream signalling	1	TAS2R9
G alpha (i) signalling events	1	TAS2R9
Class C/3 (Metabotropic glutamate/pheromone receptors)	1	TAS2R9
GPCR ligand binding	1	TAS2R9

Dominant GO biological processes

GO term	Targets
detection of chemical stimulus involved in sensory perception of bitter taste	1
signal transduction	1
G protein-coupled receptor signaling pathway	1
sensory perception of taste	1

Indications & clinical

Indications

18 indications (7 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
eye infectious disorder	4	MONDO:0043885	EFO:1001888
acne	4	MONDO:0011438	EFO:0003894
chronic bronchitis	4	MONDO:0005607	EFO:0006505
keratitis	4	MONDO:0003085	EFO:0009449
otitis externa	4	MONDO:0004795	EFO:0009560
otitis media	3	MONDO:0005441	EFO:0004992
urinary tract infection	3	MONDO:0100338	EFO:0003103
bacterial conjunctivitis	3	MONDO:0006668	EFO:1000829
pelvic inflammatory disease	3	MONDO:0000922	EFO:1001388
open-angle glaucoma	3	MONDO:0005338	EFO:0004190
ocular hypertension	3	MONDO:0006875	EFO:1001069
glaucoma	3	MONDO:0005041	MONDO:0005041
hearing loss disorder	1	MONDO:0005365	EFO:0004238
osteomyelitis	0	MONDO:0005246	EFO:0003102

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

Clinical trials

Total trials: 221.

Phase distribution

Phase	Trials
PHASE3	69
PHASE4	67
Not specified	36
PHASE2	21
PHASE2/PHASE3	11
PHASE1	10
PHASE1/PHASE2	6
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05061732	PHASE4	RECRUITING	Helicobacter Pylori Eradication and Follow-up
NCT05398679	PHASE4	RECRUITING	Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis
NCT06172010	PHASE4	RECRUITING	Rifampicin Combination Therapy Versus Monotherapy for Staphylococcal Prosthetic Joint Infection
NCT06200779	PHASE4	NOT_YET_RECRUITING	Tailored Vs. Empirical Helicobacter Pylori Infection Treatment
NCT06494072	PHASE4	RECRUITING	Short Versus Standard of Care Antibiotic Duration for Children Hospitalized for CAP
NCT06741917	PHASE4	ENROLLING_BY_INVITATION	Retrograde Intrarenal Surgery Low Risk Trial
NCT07021729	PHASE4	NOT_YET_RECRUITING	Comparison of Two Treatment Regimens of Helicobacter Pylori Infection
NCT07040839	PHASE4	NOT_YET_RECRUITING	Comparison of Omeprazole vs Vonoprazon in Treatment of H Pylori Infection
NCT07320534	PHASE4	NOT_YET_RECRUITING	Levofloxacin Prophylaxis to Prevent First Febrile Neutropenia in Pediatric ALL During Induction Phase
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
NCT00239161	PHASE4	TERMINATED	Safety and Efficacy Study of the Treatment of Kidney Infections With Short Course Levofloxacin
NCT00245791	PHASE4	TERMINATED	Urinary Tract Infection Study With the Antibiotic Levofloxacin Given at a Higher Dose Over a Shorter Period of Time
NCT00392275	PHASE4	COMPLETED	Penetrance of Third Generation Fluoroquinolones in Eyes With Functioning Filtering Blebs
NCT00429975	PHASE4	TERMINATED	Ceftriaxone Vs Levofloxacin on Cytokine Expression in Pneumococcal Pneumonia
NCT00480376	PHASE4	UNKNOWN	Ofloxacin vs. Gentamicin as Prophylaxis Prior Transrectal Biopsy of Prostate
NCT00495339	PHASE4	COMPLETED	MDR TB, Levofloxacin, Multi-Drug-Resistant Pulmonary Tuberculosis
NCT00645073	PHASE4	COMPLETED	Study of the Safety and Efficacy of Cefdinir and Levofloxacin for the Treatment of Subjects With Acute Bacterial Sinusitis
NCT00665327	PHASE4	COMPLETED	Avelox for Treatment of Elderly Patients With Community Acquired Pneumonia
NCT00752947	PHASE4	UNKNOWN	Efficacy and Safety Trial to Assess Moxifloxacin in Treating Community-Acquired Pneumonia (CAP) With Aspiration Factors
NCT00840580	PHASE4	COMPLETED	Effect on Wound Healing of Vigamox Versus Cravit
NCT01034176	PHASE4	COMPLETED	BK Treatment Study
NCT01353339	PHASE4	COMPLETED	Quinolone Prophylaxis for the Prevention of BK Virus Infection in Kidney Transplantation: A Pilot Study
NCT01467297	PHASE4	COMPLETED	Ceftidoren Versus Levofloxacin in the Treatment of Patients With Acute Exacerbations of Chronic Bronchitis (AECB)
NCT01524302	PHASE4	COMPLETED	Pharmacodynamic of Ceftaroline and Levofloxacin Against Pathogens Associated With Community Acquired Bacterial Pneumonia
NCT01742429	PHASE4	COMPLETED	Levofloxacin and Bismuth-containing Therapy Versus Quadruple Therapy as Second-line Treatment of Resistant Helicobacter Pylori Infection
NCT01799356	PHASE4	COMPLETED	Moxifloxacin Versus Ofloxacin Plus Metronidazole in Uncomplicated Pelvic Inflammatory Disease: Multicenter Randomized Controlled Trials
NCT02018081	PHASE4	COMPLETED	Pharmacokinetics of Levofloxacin in Intensive Care Unit
NCT02028754	PHASE4	COMPLETED	A Study of Sodium Carboxymethylcellulose for Post Cataract Surgery Dry Eye Symptoms
NCT02094703	PHASE4	UNKNOWN	The Efficacy of Solifenacin Succinate as Adjuvant Therapy for Urinary Tract Infection in Females
NCT02373137	PHASE4	UNKNOWN	Descemet Endothelial Thickness Comparison Trial
NCT02466919	PHASE4	COMPLETED	Study of Levofloxacin-based Concomitant Therapy for H. Pylori Eradication in Diabetic Patients
NCT02600806	PHASE4	UNKNOWN	Clinical Pathway Based on Procalcitonin Levels for the Management of Community-acquired Pneumonia in Outpatients
NCT02618057	PHASE4	UNKNOWN	Effects of Oral Steroid in Mycoplasma Pneumoniae Pneumonia
NCT02693574	PHASE4	UNKNOWN	Comparison Efficacy of 14-day Triple Therapy: Clarithromycin vs. Levofloxacin on Eradication of H. Pylori
NCT02757365	PHASE4	UNKNOWN	Efficiency Study of Aspirin to Prevent the Occurrence of Prostate Cancer
NCT02901288	PHASE4	UNKNOWN	Shortened Regimens for Drug-susceptible Pulmonary Tuberculosis
NCT02935010	PHASE4	COMPLETED	Tailored Versus Empiric Therapy for Helicobacter Pylori Treatment
NCT02988089	PHASE4	UNKNOWN	Antimicrobial Susceptibility Testing Guided Antibiotic Selection Strategies in Salvage Helicobacter Pylori Treatment
NCT03087656	PHASE4	UNKNOWN	Antibiotics to Decrease Post ERCP Cholangitis
NCT03139253	PHASE4	UNKNOWN	Antimicrobial Susceptibility Testing Guided Triple Therapy in Salvage Helicobacter Pylori Treatment

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for aminosalicylic acid, chloramphenicol,	CPIC	G6PD

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

1 molecules share ≥1 primary target. Top 1 by shared-target count:

Molecule	Source	Status	Shared targets
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	TAS2R9