In a concentration-dependent manner, bromfenac (0-80 μg/mL; 24 h) inhibits the epithelial-to-mesenchymal transition of HLEC-B3 induced by transforming growth factor-β2 [2]. In the human anterior capsule, the transforming growth factor-β2-induced epithelial-to-mesenchymal transition is inhibited by bromfenac (80 μg/mL; 48 h) [2].

Rats treated with a solution of bromfenac (0.0032-3.16%; 100 or 200 μL; rubbed on the back) showed notable antimicrobial activity at concentrations as low as 0.1% (4 hours before treatment) or 0.32% (18 hours before treatment). inflammation [3]. When applied topically to the paws of rats, bromfenac (0.032-3.16%; 100 μL) exhibits dose-dependent anti-inflammatory effects [3]. Applying bromfenac (0.032-1.0%; 50 μL) directly to guinea pigs' UV-exposed skin areas inhibited erythema 26 times more effectively than indomethacin [3]. Both the dose and the duration of the application of bromfenac (0.0032-0.1%; 50 μL) to the uninjected paw of rats results in a dose- and time-dependent reduction in the volume of the hindlimbs [3]. When administered topically to the abdomen of mice challenged with acetylcholine, bromfenac (0.32%; 50 μL) significantly inhibits abdominal contractions [3]. During the 4-week period, bromfenac (eye drops; 1 μL (0.09%) per eye; twice daily) slows down and partially reduces corneal staining [4].

Cell Viability Assay[2]
Cell Types: Human anterior capsule treated with transforming growth factor-β2
Tested Concentrations: 80 μg/mL
Incubation Duration: 48 hrs (hours)
Experimental Results: Inhibition of transforming growth factor-β2-induced epithelial- mesenchymal transition (LEC).

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Cell migration assay[2]
Cell Types: HLEC-B3 Cell
Tested Concentrations: 0, 20, 40, 60 and 80 μg/mL
Incubation Duration: 24 hrs (hours)
Experimental Results: Inhibition of transforming growth factor-β2-induced cell migration in HLEC-B3 cells, and demonstrated inhibition of overexpression of epithelial-mesenchymal transition markers.

Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (150-250 g) injected with carrageenan [3]
Doses: 0.0032, 0.01, 0.032, 0.1, 0.32, 1.0, 3.16% (100 or 200 μL)
Route of Administration: 1 Carrageenan injected on back - 72 hrs (hrs (hours)) before injection
Experimental Results: Significant anti-inflammatory activity was produced when applied at 0.32% 1, 2 and 4 hrs (hrs (hours)) before carrageenan challenge. Carrageenan is effective when applied 1 or 4 hrs (hrs (hours)) before challenge, but not 0.2% when applied 24 hrs (hrs (hours)) (or more) before challenge.

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Animal/Disease Models: Male injected with Salin or BTX-B[4]
Doses: 1 μL (0.09%) per eye
Route of Administration: eye drops; 1 μL (0.09%) per eye; twice a day; 4-week
Experimental Results: Corneal fluorescein staining scores improved 4 weeks after treatment.

Absorption, Distribution and Excretion
The plasma concentration of bromfenac following ocular administration in humans is unknown.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Milk levels of bromfenac are likely to be low with the usual oral dosage, but milk levels have not been measured after higher injectable dosages. Use caution when using bromfenac in nursing mothers, especially with the injectable drug.
Maternal use of bromfenac eye drops would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[1]. Tetsuo Kida, et al. Pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs in retinochoroidal tissues in rabbits. PLoS One. 2014 May 5;9(5):e96481.
[2]. Xiaobo Zhang, et al. Drug-eluting intraocular lens with sustained bromfenac release for conquering posterior capsular opacification. Bioact Mater. 2021 Jul 23;9:343-357.
[3]. Nolan JC, et, al. The topical anti-inflammatory and analgesic properties of bromfenac in rodents. Agents Actions. 1988 Aug; 25(1-2): 77-85.
[4]. Kaevalin Lekhanont, et al. Effects of topical anti-inflammatory agents in a botulinum toxin B-induced mouse model of keratoconjunctivitis sicca. J Ocul Pharmacol Ther. 2007 Feb;23(1):27-34.

Bromfenac is 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. It has a role as a non-steroidal anti-inflammatory drug and a non-narcotic analgesic. It is a member of benzophenones, a substituted aniline, an aromatic amino acid and an organobromine compound. It is functionally related to an amfenac. It is a conjugate acid of a bromfenac(1-).
Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) for ophthalmic use. Ophthalmic NSAIDs are becoming a cornerstone for the management of ocular pain and inflammation. Their well-characterized anti-inflammatory activity, analgesic property, and established safety record have also made NSAIDs an important tool for optimizing surgical outcomes. Non-ophthalmic formulations of bromfenac were withdrawn in the US in 1998 due to cases of severe liver toxicity.
Bromfenac is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of bromfenac is as a Cyclooxygenase Inhibitor.
Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory activities. Upon ophthalmic administration, bromfenac binds to and inhibits the activity of cyclooxygenase II (COX II), an enzyme which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins (PG). By inhibiting PG formation, bromfenac is able to inhibit PG-induced inflammation, thereby preventing vasodilation, leukocytosis, disruption of the blood-aqueous humor barrier, an increase in vascular permeability and an increase in intraocular pressure (IOP).
See also: Bromfenac Sodium (has salt form); Bromfenac; prednisolone acetate (component of) ... View More ...

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Drug Indication
For the treatment of postoperative inflammation in patients who have undergone cataract extraction.
FDA Label
Treatment of postoperative ocular inflammation following cataract extraction in adults.

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Mechanism of Action
The mechanism of its action is thought to be due to its ability to block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2. Prostaglandins have been shown in many animal models to be mediators of certain kinds of intraocular inflammation. In studies performed in animal eyes, prostaglandins have been shown to produce disruption of the blood-aqueous humor barrier, vasodilation, increased vascular permeability, leukocytosis, and increased intraocular pressure.

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Pharmacodynamics
Bromfenac ophthalmic solution is a sterile, topical, nonsteroidal anti-inflammatory drug (NSAID) for ophthalmic use.

C15H12NO3BR

334.16468

333

91714-94-2

Bromfenac sodium;91714-93-1;Bromfenac sodium hydrate;120638-55-3

60726

Typically exists as solid at room temperature

1.6±0.1 g/cm3

562.2±50.0 °C at 760 mmHg

-129ºC

293.8±30.1 °C

0.0±1.6 mmHg at 25°C

1.663

2.72

2

4

4

20

366

0

O=C(CC1C(N)=C(C(C2C=CC(Br)=CC=2)=O)C=CC=1)O

ZBPLOVFIXSTCRZ-UHFFFAOYSA-N

InChI=1S/C15H12BrNO3/c16-11-6-4-9(5-7-11)15(20)12-3-1-2-10(14(12)17)8-13(18)19/h1-7H,8,17H2,(H,18,19)

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

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)