Bromfenac

Summary

Bromfenac (CHEMBL1077) is an approved small-molecule non-steroidal anti-inflammatory drug (ATC S01BC11) targeting PTGS1; indicated across 8 conditions including eye disorder and atopic conjunctivitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: S01BC11
• Targets: 1 (PTGS1)
• Indications: 8 conditions
• Clinical trials: 33
• Chemistry: 334.16 Da · C15H12BrNO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1077
Name	Bromfenac
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	60726
ChEBI	CHEBI:240107
ATC	S01BC11
Molecular formula	C15H12BrNO3
Molecular weight	334.16
InChIKey	ZBPLOVFIXSTCRZ-UHFFFAOYSA-N

SMILES: C1=CC(=C(C(=C1)C(=O)C2=CC=C(C=C2)Br)N)CC(=O)O

IUPAC name: 2-[2-amino-3-(4-bromobenzoyl)phenyl]acetic acid

ChEBI definition: Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.

Pharmacological roles (ChEBI): non-steroidal anti-inflammatory drug, non-narcotic analgesic.

Also known as: Bromfenac, Bromfenaco, ISV-303, SID26757971, bromfenac, BROMFENAC, BromfenacÊ, BromfenacÂ, Bromenfac

Parent form; salt/anhydrous children: CHEMBL3181947

Patent coverage: 3,075 distinct patent families (12,495 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

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
PTGS1	COX-1	Inhibition	8.07	0%	P23219

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Prelamin-A/C, Prostaglandin G/H synthase 1, Adenosine receptor A1, Prostaglandin G/H synthase 2, Bile salt export pump.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PTGS2	8.32	IC50	4.8	nM	CHEMBL_ACT_7602588
PTGS1	8.17	AC50	6.7	nM	CHEMBL_ACT_25205822
PTGS1	8.07	IC50	8.48	nM	CHEMBL_ACT_7602586
PTGS1	7.46	AC50	34.6	nM	CHEMBL_ACT_25206752

Target pathways

Aggregated over 1 target gene(s): PTGS1.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
COX reactions	1	PTGS1
Synthesis of Prostaglandins (PG) and Thromboxanes (TX)	1	PTGS1

Dominant GO biological processes

GO term	Targets
prostaglandin biosynthetic process	1
response to oxidative stress	1
regulation of blood pressure	1
cyclooxygenase pathway	1
regulation of cell population proliferation	1
long-chain fatty acid biosynthetic process	1
lipid metabolic process	1
fatty acid metabolic process	1
fatty acid biosynthetic process	1
prostaglandin metabolic process	1
prostanoid biosynthetic process	1
cellular oxidant detoxification	1

Indications & clinical

Indications

8 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
eye disorder	4	MONDO:0005328	EFO:0005752
atopic conjunctivitis	3	MONDO:0005642	EFO:0007141
dry eye syndrome	3	MONDO:0006733	EFO:1000906
cataract	3	MONDO:0005129	MONDO:0005129
age-related macular degeneration	2	MONDO:0005150	EFO:0001365
presbyopia	1	MONDO:0001330	MONDO:0001330

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

Clinical trials

Total trials: 33.

Phase distribution

Phase	Trials
PHASE4	17
PHASE3	8
PHASE2	3
PHASE1	2
Not specified	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00377546	PHASE4	COMPLETED	Comparison of Vitreous Levels of Acular LS 0.04%, Xibrom 0.09%, and Nevanac 0.1%
NCT00520260	PHASE4	COMPLETED	Bromfenac 0.09% vs Ketorolac 0.4% for Cyclosporine Induction Phase
NCT00595543	PHASE4	COMPLETED	Treatment of Acute Pseudophakic Cystoid Macular Edema: Bromfenac 0.09% Versus Diclofenac Sodium 0.1% Versus Ketorolac Tromethamine 0.5%
NCT00758199	PHASE4	COMPLETED	Determination of Optimum Duration of Treatment With Bromfenac (Xibrom) Eyedrops Following Cataract Surgery
NCT01001806	PHASE4	COMPLETED	A Comparison of Peak Aqueous Penetration of Acuvail (Ketorolac 0.45%), Xibrom (Bromfenac 0.09%), and Nevanac (Nepafenac 0.1%)in Patients Undergoing Phacoemulsification
NCT01021761	PHASE4	COMPLETED	A Comparison of Prostaglandin E2 (PGE2) Inhibition of Acuvail(Ketorolac 0.45%), Xibrom (Bromfenac 0.09%)and Nevanac (Nepafenac)in Patients Undergoing Phacoemulsification
NCT01023724	PHASE4	COMPLETED	A Comparison of Post Phacoemulsification Aqueous Flare in Patients Using Ketorolac 0.45% 2 Times Daily (BID) and Bromfenac 0.09% 2 Times Daily (BID)
NCT01310127	PHASE4	COMPLETED	Clinical Outcomes of Bromday (Bromfenac Ophthalmic Solution) 0.09% QD vs. Nevanac (Nepafenac Ophthalmic Suspension) 0.1%
NCT03317847	PHASE4	COMPLETED	Bromfenac Versus Dexamethasone After Cataract Surgery
NCT03578276	PHASE4	COMPLETED	Prophylactic Treatment: Lessdrops™ vs Standard Drops Regimen
NCT03751059	PHASE4	UNKNOWN	NSAID vs Steroid in Trabeculectomy Wound Management
NCT03831984	PHASE4	UNKNOWN	Topical Bromfenac for Intraoperative Miosis and Pain Reduction
NCT03886779	PHASE4	COMPLETED	Study Title: Clinical Outcomes of Prolensa (Bromfenac Ophthalmic Solution) 0.07% QD vs. Ilevro (Nepafenac Ophthalmic Suspension) 0.3% QD With Extra (Pulse) Dose on Day of Surgery for Treatment of Ocular Inflammation Associated With Cataract Surgery in a Randomized, Single Masked Clinical Trial
NCT04022811	PHASE4	COMPLETED	Effect of Bromfenac on Pain Related to Pterygium Surgery
NCT04343222	PHASE4	COMPLETED	Control of Pain in Intravitreal Injections Using Topical NSAIDs
NCT06785090	PHASE4	COMPLETED	Effects of Bromfenac on Macular Thickness After Phacoemulsification Surgery
NCT07090044	PHASE4	COMPLETED	Comparing Post-intravitreal Injection Pain Scores Using Loteprednol, Bromfenac Sodium, and Artificial Tears Over a 24-hour Period
NCT00198445	PHASE3	COMPLETED	Safety and Efficacy Study of Topical Bromfenac Versus Placebo to Treat Ocular Inflammation After Cataract Surgery
NCT00423007	PHASE3	COMPLETED	Efficacy and Safety of Topical Bromfenac Ophthalmic Solution vs. Placebo in Subjects With Allergic Conjunctivitis
NCT00704418	PHASE3	COMPLETED	Efficacy and Safety of Bromfenac Ophthalmic Solution in Cataract Surgery
NCT01576952	PHASE3	COMPLETED	Comparison Study of ISV-303 to DuraSite Vehicle in Cataract Surgery Subjects
NCT01774474	PHASE3	COMPLETED	PRevention of Macular EDema After Cataract Surgery
NCT01808547	PHASE3	COMPLETED	Comparison Study of ISV-303 to Durasite Vehicle in Cataract Surgery Subjects
NCT02361645	PHASE3	COMPLETED	NSAIDs and PGE2 Levels in Vitrectomy Patients
NCT05158699	PHASE3	TERMINATED	Effectiveness of Periocular Drug Injection in CATaract Surgery
NCT00438243	PHASE2	WITHDRAWN	Pilot Study of the Effect of Topical Bromfenac Ophthalmic Solution 0.09%in Patients With Acute Post-operative Cystoid Macular Edema.
NCT00805233	PHASE2	COMPLETED	Combination Ranibizumab and Bromfenac for Neovascular Age-related Macular Degeneration
NCT01190878	PHASE1/PHASE2	COMPLETED	Study to Compare Differing Dosing Regimens of ISV-303 (Bromfenac in DuraSite) to Xibrom and Vehicle in Post Cataract Surgery Volunteers
NCT01387464	PHASE2	COMPLETED	Aqueous Humor Concentration of InSite Vision (ISV) 303 (Bromfenac in DuraSite) to Bromday Once Daily (QD) Prior to Cataract Surgery
NCT01535443	PHASE1	COMPLETED	Safety and Tolerability of PRO-155 Ophthalmic Solution 0.09% in Healthy Volunteers.
NCT05001243	PHASE1	UNKNOWN	Comparison of a Compound With Pilocarpine and Brimonidine to Improve Near Vision in Healthy Presbyopic Patients
NCT07178639	Not specified	RECRUITING	Comparing Efficacy of Bromfenac 0.09%, Nepafenac 0.3% and Diclofenac 0.1% in Patients After Cataract Surgery
NCT01475877	Not specified	COMPLETED	Bromday Versus Nevanac Eye Drops to Control Pain Following Photorefractive Keratectomy

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

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.

275 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
2-MERCAPTOETHANESULFONIC ACID	ChEMBL	Phase 4 (approved)	PTGS1
3,3’,4’,5-TETRACHLOROSALICYLANILIDE	ChEMBL	Phase 4 (approved)	PTGS1
ACARBOSE	ChEMBL	Phase 4 (approved)	PTGS1
ACEMETACIN	ChEMBL	Phase 4 (approved)	PTGS1
ACETOHYDROXAMIC ACID	ChEMBL	Phase 4 (approved)	PTGS1
ALITRETINOIN	ChEMBL	Phase 4 (approved)	PTGS1
AMDINOCILLIN	ChEMBL	Phase 4 (approved)	PTGS1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	PTGS1
ASCORBIC ACID	ChEMBL	Phase 4 (approved)	PTGS1
ASPIRIN	ChEMBL	Phase 4 (approved)	PTGS1
AVATROMBOPAG	ChEMBL	Phase 4 (approved)	PTGS1
BELINOSTAT	ChEMBL	Phase 4 (approved)	PTGS1
BENDAMUSTINE	ChEMBL	Phase 4 (approved)	PTGS1
BENZIODARONE	ChEMBL	Phase 4 (approved)	PTGS1
BETA CAROTENE	ChEMBL	Phase 4 (approved)	PTGS1
BRIGATINIB	ChEMBL	Phase 4 (approved)	PTGS1
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	PTGS1
CAPSAICIN	ChEMBL	Phase 4 (approved)	PTGS1
CAPTOPRIL	ChEMBL	Phase 4 (approved)	PTGS1
CARBARIL	ChEMBL	Phase 4 (approved)	PTGS1
CARPROFEN	ChEMBL	Phase 4 (approved)	PTGS1
CASPOFUNGIN	ChEMBL	Phase 4 (approved)	PTGS1
CEFPODOXIME PROXETIL	ChEMBL	Phase 4 (approved)	PTGS1
CELECOXIB	ChEMBL	Phase 4 (approved)	PTGS1
CEPHALOGLYCIN	ChEMBL	Phase 4 (approved)	PTGS1
CEPHALORIDINE	ChEMBL	Phase 4 (approved)	PTGS1
CHLORPROTHIXENE	ChEMBL	Phase 4 (approved)	PTGS1
CHOLECALCIFEROL	ChEMBL	Phase 4 (approved)	PTGS1
CIANIDANOL	ChEMBL	Phase 4 (approved)	PTGS1
CLOMIPHENE	ChEMBL	Phase 4 (approved)	PTGS1
COLISTIN	ChEMBL	Phase 4 (approved)	PTGS1
CYCLOSERINE	ChEMBL	Phase 4 (approved)	PTGS1
CYSTEINE	ChEMBL	Phase 4 (approved)	PTGS1
DACTINOMYCIN	ChEMBL	Phase 4 (approved)	PTGS1
DELAMANID	ChEMBL	Phase 4 (approved)	PTGS1
DEQUALINIUM	ChEMBL	Phase 4 (approved)	PTGS1
DESLORATADINE	ChEMBL	Phase 4 (approved)	PTGS1
DESMOPRESSIN	ChEMBL	Phase 4 (approved)	PTGS1
DESOGESTREL	ChEMBL	Phase 4 (approved)	PTGS1
DEXIBUPROFEN	ChEMBL	Phase 4 (approved)	PTGS1
DEXKETOPROFEN	ChEMBL	Phase 4 (approved)	PTGS1
DEXPANTHENOL	ChEMBL	Phase 4 (approved)	PTGS1
DEXRAZOXANE	ChEMBL	Phase 4 (approved)	PTGS1
DICLOFENAC	ChEMBL	Phase 4 (approved)	PTGS1
DIETHYLSTILBESTROL	ChEMBL	Phase 4 (approved)	PTGS1
DIRITHROMYCIN	ChEMBL	Phase 4 (approved)	PTGS1
DOPAMINE	ChEMBL	Phase 4 (approved)	PTGS1
DOXORUBICIN	ChEMBL	Phase 4 (approved)	PTGS1
DROXIDOPA	ChEMBL	Phase 4 (approved)	PTGS1
EDARAVONE	ChEMBL	Phase 4 (approved)	PTGS1
ELIGLUSTAT	ChEMBL	Phase 4 (approved)	PTGS1
ENASIDENIB	ChEMBL	Phase 4 (approved)	PTGS1
EPIRUBICIN	ChEMBL	Phase 4 (approved)	PTGS1
ERGOCALCIFEROL	ChEMBL	Phase 4 (approved)	PTGS1
ERLOTINIB	ChEMBL	Phase 4 (approved)	PTGS1
ERTAPENEM	ChEMBL	Phase 4 (approved)	PTGS1
ESFLURBIPROFEN	ChEMBL	Phase 4 (approved)	PTGS1
ESTRADIOL CYPIONATE	ChEMBL	Phase 4 (approved)	PTGS1
ESTRADIOL VALERATE	ChEMBL	Phase 4 (approved)	PTGS1
ESTRIOL	ChEMBL	Phase 4 (approved)	PTGS1