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

In rats, bromfenac (0.0032-3.16%; 100 or 200 μL; applied to the back) demonstrated notable antibacterial action at doses as low as 0.1% (4 hours prior to treatment) or 0.32% (18 hours prior to treatment). an increase in inflammation [3]. In rats, the application of 100 μL of bromfenac (0.032-3.16%) results in dose-dependent anti-inflammatory effects [3]. When administered directly to guinea pigs' UV-exposed skin regions, bromfenac (0.032-1.0%; 50 μL) was 26 times more effective than indomethacin at preventing erythema [3]. Rats' paw volume of both hindlimbs decreases in a dose- and time-dependent manner when bromfenac (0.0032-0.1%; 50 μL) is administered to the uninjected paw four hours a day, five days a week [3]. When administered topically to the abdomen, bromfenac (0.32%; 50 μL) dramatically prevents belly contractions in mice given acetylcholine [3]. When applied twice daily for four weeks, 1 μL (0.09%) of bromfenac eye drops per eye partially lowers corneal staining, which slows down after four weeks [4].

Cell viability assay[2]
Cell Types: Transforming growth factor-β2-treated human anterior capsule
Tested Concentrations: 80 μg/mL
Incubation Duration: 48 hrs (hours)
Experimental Results: Transforming growth factor-β2-induced epithelial-mesenchymal transition was inhibited in primary LECs .

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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]. Pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs in retinochoroidal tissues in rabbits. PLoS One. 2014 May 5;9(5):e96481.

[2]. Drug-eluting intraocular lens with sustained bromfenac release for conquering posterior capsular opacification. Bioact Mater. 2021 Jul 23;9:343-357.

[3]. The topical anti-inflammatory and analgesic properties of bromfenac in rodents. Agents Actions. 1988 Aug; 25(1-2): 77-85.

[4]. 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.

C30H28BR2N2NA2O9

766.35

333

120638-55-3

Bromfenac sodium;91714-93-1;Bromfenac;91714-94-2

60726

Light yellow to yellow solid powder

1.6±0.1 g/cm3

562.2±50.0 °C at 760 mmHg

293.8±30.1 °C

0.0±1.6 mmHg at 25°C

1.663

2.72

2

4

4

20

366

0

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

AHR10282B; AHR 10282B

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

DMSO : ≥ 100 mg/mL (~260.98 mM)
H2O : ≥ 100 mg/mL (~260.98 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: 33.33 mg/mL (86.98 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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