bromfenac Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| anti-inflammatory agents, ibufenac derivatives | 401 | 91714-94-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID). The mechanism of its action is thought to be due to its ability to block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2, prostaglandins are mediators of certain kinds of intraocular inflammation.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.28 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 67 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.11 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 24, 2005 | FDA | BAUSCH AND LOMB INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | S01BC11 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIINFLAMMATORY AGENTS Antiinflammatory agents, non-steroids |
| FDA MoA | N0000000160 | Cyclooxygenase Inhibitors |
| FDA Chemical/Ingredient | N0000175721 | Nonsteroidal Anti-inflammatory Compounds |
| FDA EPC | N0000175722 | Nonsteroidal Anti-inflammatory Drug |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35475 | non-steroidal anti-inflammatory drug |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| MeSH PA | D000893 | Anti-Inflammatory Agents |
| MeSH PA | D000894 | Anti-Inflammatory Agents, Non-Steroidal |
| MeSH PA | D018501 | Antirheumatic Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018689 | Sensory System Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pain | indication | 22253000 | |
| Postoperative Ocular Pain | indication | ||
| Post-Op Ocular Inflammation | indication | ||
| Rheumatoid arthritis | contraindication | 69896004 | DOID:7148 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Red eye | contraindication | 75705005 | |
| Epithelial Keratopathy | contraindication |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.32 | acidic |
| pKa2 | 3.17 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 0.07% ACID | PROLENSA | BAUSCH AND LOMB | N203168 | April 5, 2013 | RX | SOLUTION/DROPS | OPHTHALMIC | 8927606 | Jan. 16, 2024 | METHOD OF TREATING OCULAR INFLAMMATION |
| EQ 0.07% ACID | PROLENSA | BAUSCH AND LOMB | N203168 | April 5, 2013 | RX | SOLUTION/DROPS | OPHTHALMIC | 8927606 | Jan. 16, 2024 | METHOD OF TREATMENT TO ALLEVIATE INFLAMMATION OF THE EYE |
| EQ 0.07% ACID | PROLENSA | BAUSCH AND LOMB | N203168 | April 5, 2013 | RX | SOLUTION/DROPS | OPHTHALMIC | 9561277 | Jan. 16, 2024 | TREATMENT OF POSTOPERATIVE INFLAMMATION AND REDUCTION OF OCULAR PAIN IN PATIENTS WHO HAVE UNDERGONE CATARACT SURGERY |
| EQ 0.075% ACID | BROMSITE | SUN PHARMA GLOBAL | N206911 | April 8, 2016 | RX | SOLUTION/DROPS | OPHTHALMIC | 8778999 | Aug. 7, 2029 | TREATMENT OF POSTOPERATIVE INFLAMMATION AND PREVENTION OF OCULAR PAIN IN PATIENTS UNDERGOING CATARACT SURGERY |
| EQ 0.07% ACID | PROLENSA | BAUSCH AND LOMB | N203168 | April 5, 2013 | RX | SOLUTION/DROPS | OPHTHALMIC | 9517220 | Nov. 11, 2033 | TREATMENT OF POSTOPERATIVE INFLAMMATION AND REDUCTION OF OCULAR PAIN IN PATIENTS WHO HAVE UNDERGONE CATARACT SURGERY |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Prostaglandin G/H synthase 2 | Enzyme | INHIBITOR | IC50 | 8.40 | WOMBAT-PK | CHEMBL | |||
| Prostaglandin G/H synthase 1 | Enzyme | INHIBITOR | IC50 | 8.29 | WOMBAT-PK | CHEMBL | |||
| Cyclooxygenase | Enzyme | IC50 | 7.10 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| C3556169 | UMLSCUI |
| D07541 | KEGG_DRUG |
| 417155005 | SNOMEDCT_US |
| 4024075 | VANDF |
| 181436 | MMSL |
| d04150 | MMSL |
| 4299 | MMSL |
| 19737 | RXNORM |
| 108520008 | SNOMEDCT_US |
| 006757 | NDDF |
| 864P0921DW | UNII |
| 5892 | INN_ID |
| 120638-55-3 | SECONDARY_CAS_RN |
| CHEMBL751 | ChEMBL_ID |
| CHEMBL1077 | ChEMBL_ID |
| DB00963 | DRUGBANK_ID |
| 27R | PDB_CHEM_ID |
| CHEBI:240107 | CHEBI |
| 7131 | IUPHAR_LIGAND_ID |
| 60726 | PUBCHEM_CID |
| C053083 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Prolensa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-602 | SOLUTION/ DROPS | 0.70 mg | OPHTHALMIC | NDA | 15 sections |
| BromSite | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49708-754 | SOLUTION/ DROPS | 0.76 mg | OPHTHALMIC | NDA | 15 sections |
| bromfenac | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50383-249 | SOLUTION/ DROPS | 1.04 mg | OPHTHALMIC | ANDA | 14 sections |
| Bromday | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50436-6301 | SOLUTION/ DROPS | 0.90 mg | OPHTHALMIC | NDA | 14 sections |
| Bromday | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6301 | SOLUTION/ DROPS | 0.90 mg | OPHTHALMIC | NDA | 14 sections |
| Bromfenac | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6343 | SOLUTION/ DROPS | 1.04 mg | OPHTHALMIC | ANDA | 12 sections |
| Bromfenac Ophthalmic Solution 0.09% | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62332-508 | SOLUTION/ DROPS | 1.04 mg | OPHTHALMIC | ANDA | 14 sections |
| BROMFENAC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68083-313 | SOLUTION/ DROPS | 0.90 mg | OPHTHALMIC | ANDA | 14 sections |
| Pred-Gati-Brom | HUMAN PRESCRIPTION DRUG LABEL | 2 | 70261-504 | SUSPENSION/ DROPS | 0.75 mg | OPHTHALMIC | unapproved drug other | 1 sections |
| Pred-Brom | HUMAN PRESCRIPTION DRUG LABEL | 2 | 70261-505 | SUSPENSION/ DROPS | 0.75 mg | OPHTHALMIC | unapproved drug other | 1 sections |
| Pred-Brom | HUMAN PRESCRIPTION DRUG LABEL | 2 | 71384-505 | SUSPENSION/ DROPS | 0.75 mg | OPHTHALMIC | unapproved drug other | 2 sections |
| Pred Phos - Brom | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71384-552 | SOLUTION/ DROPS | 0.75 mg | OPHTHALMIC | unapproved drug other | 1 sections |