The primary target of Bromfenac Sodium Sesquihydrate is cyclooxygenase (COX), particularly COX-2. By inhibiting COX, the compound reduces the synthesis of prostaglandins, which are key mediators of inflammation, pain, and fever. The selective inhibition of COX-2 over COX-1 may reduce the risk of gastrointestinal side effects compared to non-selective NSAIDs.

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 vitro, bromfenac has been shown to be a potent inhibitor of COX-1 and COX-2 enzymes. It reduces the production of prostaglandins in various cell types, including ocular tissues. The compound's anti-inflammatory activity has been confirmed in various in vitro models of inflammation.

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].
In vivo, bromfenac sodium sesquihydrate is used as an ophthalmic solution for the treatment of postoperative inflammation and pain following cataract surgery. It reduces ocular inflammation, pain, and the risk of macular edema. The compound is administered topically to the eye and is generally well-tolerated.

In vitro enzyme or receptor binding (non-cell) assays for bromfenac involve measuring its inhibition of COX-1 and COX-2 enzymatic activity. The assay uses a purified COX enzyme and a substrate, such as arachidonic acid. The production of prostaglandins is measured using a colorimetric or fluorometric method. The compound is incubated with the enzyme and substrate at varying concentrations, and the IC50 is determined.

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.
In vitro cell-based assays for bromfenac are performed using ocular cell lines or other cell types. Cells are treated with the compound, and the production of prostaglandins is measured by ELISA. The compound's effects on cell viability, proliferation, and inflammatory responses are also assessed.

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.
In vivo animal experiments for bromfenac are conducted using animal models of ocular inflammation, such as the rabbit model of uveitis or the mouse model of laser-induced choroidal neovascularization. The compound is administered topically to the eye, and inflammation and pain are assessed. These studies confirm the compound's efficacy as an anti-inflammatory agent in the eye.

Absorption, Distribution and Excretion
The plasma concentration of bromfenac after ocular administration in humans is still unknown.
Pharmacokinetic (PK) properties of bromfenac sodium sesquihydrate indicate that it is rapidly absorbed after topical ocular administration. The compound has a molecular weight of 383.14 and a molecular formula of C15H11BrNNaO3·1.5H2O. It is a solid at room temperature. The compound reaches therapeutic concentrations in the aqueous humor and vitreous humor. It is metabolized in the liver and excreted renally.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
The concentration of bromfenac sodium in breast milk may be low after oral administration, but concentrations after injection of higher doses have not been measured. Caution should be exercised when using bromfenac sodium during lactation, especially the injectable form.
No adverse effects are expected on breastfed infants from maternal use of bromfenac sodium eye drops. To significantly reduce the amount of medication entering breast milk after eye drops, press your finger against the tear duct near the corner of your eye for at least 1 minute, then wipe away any excess medication with absorbent tissue.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.
Toxicology (toxicology) data for bromfenac indicate that it is generally well-tolerated when used as an ophthalmic solution. Common side effects include eye irritation, blurred vision, and conjunctival hyperemia. Systemic side effects are rare due to minimal systemic absorption. The compound should be used with caution in patients with a history of asthma or other allergic reactions to NSAIDs.

[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 a derivative of anfenac, in which the hydrogen at the 4-position of the benzoyl group is replaced by bromine. It was used to treat eye pain and inflammation in patients after cataract extraction. Due to concerns about off-label abuse and liver failure, bromfenac was withdrawn from the US market in 1998. It is a nonsteroidal anti-inflammatory drug (NSAID) and a non-narcotic analgesic. It belongs to the benzophenone class of compounds and is a substituted aniline, aromatic amino acid, and organic bromine compound. It is functionally related to anfenac. It is the conjugate acid of bromfenac (1-). Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) used in ophthalmology. Ophthalmic NSAIDs are gradually becoming the cornerstone of the treatment of eye pain and inflammation. NSAIDs have well-defined anti-inflammatory activity, analgesic properties, and good safety profiles, making them an important tool for optimizing surgical outcomes. Due to serious cases of hepatotoxicity, non-ophthalmic formulations of bromfenac were withdrawn from the US market in 1998. Bromfenac is a nonsteroidal anti-inflammatory drug. Its mechanism of action is as a cyclooxygenase inhibitor. Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory effects. After ocular application, bromfenac binds to and inhibits the activity of cyclooxygenase II (COX II). COX II is an enzyme that converts arachidonic acid into cyclic intraperoxides (precursors to prostaglandins (PGs)). By inhibiting the production of prostaglandins (PGs), bromfenac can suppress PG-induced inflammation, thereby preventing vasodilation, leukocytosis, blood-aqueous barrier disruption, increased vascular permeability, and elevated intraocular pressure (IOP). See also: Bromfenac sodium (salt form); Bromfenac; Prednisolone acetate (ingredient)... See more...

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Drug Indications
For the treatment of inflammation in patients after cataract extraction.
FDA Label
For the treatment of ocular inflammation in adults after cataract extraction.

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Mechanism of Action
Its mechanism of action is believed to be through the inhibition of cyclooxygenases 1 and 2, thereby blocking prostaglandin synthesis. Numerous animal models have confirmed that prostaglandins are mediators of certain types of intraocular inflammation. In animal ocular studies, prostaglandins have been shown to cause disruption of the blood-aqueous barrier, vasodilation, increased vascular permeability, leukocytosis, and elevated intraocular pressure.

Other information: Bromfenac Sodium Sesquihydrate is an NSAID used as an ophthalmic solution for postoperative inflammation and pain following cataract surgery. It is also known as Bromfenac sodium. The compound is available as an ophthalmic solution. Its CAS number is 120638-55-3.

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.)