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Brinzolamide | CAS No: 138890-62-7 | GMP-certified suppliers
A medication that lowers elevated intraocular pressure in ocular hypertension and open-angle glaucoma, used alone or combined with other agents for ophthalmic treatment.
Therapeutic categories
Primary indications
- Brinzolamide, either as a standalone agent or in combination with brimonidine, is approved by the FDA for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma
- Brinzolamide is also approved in Europe to be used in combination with timolol to treat the same conditions
Product Snapshot
- Brinzolamide is available primarily as ophthalmic solutions and suspensions intended for conjunctival administration
- It is used mainly for the treatment of elevated intraocular pressure associated with ocular hypertension and open-angle glaucoma
- The compound is FDA approved in the US and holds approval in the European Union, with additional market presence in Canada
Clinical Overview
Pharmacologically, brinzolamide selectively and reversibly inhibits CA-II in the ciliary body of the eye. This enzyme catalyzes the reversible hydration of carbon dioxide to bicarbonate ions, a process integral to aqueous humor production. By inhibiting CA-II, brinzolamide decreases bicarbonate formation, thereby reducing fluid transport and lowering IOP—a key modifiable risk factor in glaucoma pathogenesis. Unlike systemically administered carbonic anhydrase inhibitors, topical brinzolamide minimizes systemic exposure and related adverse effects.
Following ocular administration, brinzolamide demonstrates local activity with minimal systemic absorption. The drug’s lipophilicity facilitates ocular tissue penetration, including potential traversal of the blood-retinal barrier. Its metabolism involves multiple cytochrome P450 enzymes, including CYP2A6, CYP2B6, CYP2C8, CYP2C9, and CYP3A4 isoforms, indicating potential for drug interactions at the metabolic level. Excretion is primarily renal with unaltered and metabolized forms detectable in urine.
Safety considerations focus on ocular tolerability. The most frequently observed adverse reactions include mild, transient ocular discomfort and local irritation. Systemic adverse effects are rare due to limited systemic bioavailability. Brinzolamide exhibits a favorable safety profile without significant off-target receptor binding, contributing to its selective pharmacologic effect. Pediatric usage has been evaluated, demonstrating efficacy comparable to adults in treatment-naive patients, with safety profiles consistent with known effects.
From a chemical classification perspective, brinzolamide belongs to thienothiazines, heterocyclic compounds comprising fused thiophene and thiazine rings. Its CAS number is 138890-62-7.
Effective API sourcing for brinzolamide requires adherence to stringent purity criteria and regulatory compliance. Manufacturers must verify conformational and structural integrity, as well as residual solvent levels, using validated analytical methods. Given its therapeutic context, API batches must meet ophthalmic-grade standards to ensure safety and efficacy in final formulations. Supply chain transparency and robust quality assurance protocols are essential to maintain continuous availability for clinical and commercial use.
Identification & chemistry
| Generic name | Brinzolamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 138890-62-7 |
| UNII | 9451Z89515 |
| DrugBank ID | DB01194 |
Pharmacology
| Summary | Brinzolamide is a selective, reversible inhibitor of carbonic anhydrase isoenzyme II, primarily targeting the ciliary body in the eye to reduce bicarbonate formation and aqueous humor secretion. This mechanism decreases intraocular pressure, addressing elevated pressure associated with ocular hypertension and open-angle glaucoma. Its specificity for carbonic anhydrase contributes to a favorable safety profile with minimal off-target interactions. |
|---|---|
| Mechanism of action | Brinzolamide is a highly specific, reversible, non-competitive inhibitor of carbonic anhydrases (CA), the enzymes catalyzing the reversible reaction of water and carbon dioxide (CO2) to form bicarbonate ions. Although there are 7 isoforms of CA in human tissues, brinzolamide has the highest affinity to CA II. Brinzolamide and its active metabolites were not found to displace any known ligands in vitro from their respective receptors or enzymes commonly involved in producing side effects or ancillary pharmacology, thus explaining brinzolamide's high order of safety. |
| Pharmacodynamics | Inhibition of carbonic anhydrase II (CA-II) in the ciliary process of the eye slows the formation of bicarbonate and thus fluid flow, lowering intraocular pressure (IOP). The IOP-reducing effect of brinzolamide as adjunctive therapy to the prostaglandin analog travoprost was studied. Following a 4-week run-in with travoprost, patients with an IOP ≥19 mmHg were randomized to receive added treatment with brinzolamide or timolol. An additional decrease in mean diurnal IOP of 3.2 to 3.4 mmHg for the brinzolamide group and 3.2 to 4.2 mmHg for the timolol group were observed. There was an overall higher incidence of non-serious ocular adverse reactions, mainly related to signs of local irritation, in the brinzolamide/travoprost groups. The events were mild and did not affect the overall discontinuation rates in the studies. A clinical trial was conducted with brinzolamide in 32 pediatric patients less than 6 years of age, diagnosed with glaucoma or ocular hypertension. Some patients were naive to IOP therapy whilst others were on other IOP-lowering medicinal product(s). Those who had been on previous IOP medicinal products were not required to discontinue their IOP medicinal product(s) until the initiation of monotherapy with brinzolamide. Among patients who were naive to IOP therapy (10 patients), the efficacy of brinzolamide was similar to that seen previously in adults, with mean IOP reductions from baseline ranging up to 5 mmHg. Among patients who were on topical IOP-lowering medicinal products (22 patients), mean IOP increased slightly from baseline in the brinzolamide group. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Carbonic anhydrase 2 | Humans | inhibitor |
| Carbonic anhydrase 1 | Humans | inhibitor |
| Carbonic anhydrase 4 | Humans | inhibitor |
ADME / PK
| Absorption | Brinzolamide is absorbed through the cornea following topical ocular administration. The substance is also absorbed into the systemic circulation where it binds strongly to carbonic anhydrase in red blood cells (RBCs). Plasma concentrations are very low. |
|---|---|
| Half-life | Due to its affinity for CAII, brinzolamide distributes extensively into the red blood cells (RBCs) and exhibits a long half-life in whole blood (approximately 111 days). |
| Protein binding | Binding to plasma proteins is approximately 60%. |
| Metabolism | Brinzolamide is metabolized by hepatic cytochrome P450 isozymes, specifically CYP3A4, CYP2A6, CYP2B6, CYP2C8 and CYP2C9. The primary metabolite is N-desethylbrinzolamide followed by the N-desmethoxypropyl and O-desmethyl metabolites as well as an N-propionic acid analog formed by oxidation of the N-propyl side chain of O-desmethyl brinzolamide. Brinzolamide and N-desethylbrinzolamide do not inhibit cytochrome P450 isozymes at concentrations at least 100-fold above maximum systemic levels. Brimonidine is extensively metabolized by hepatic aldehyde oxidase with the formation of 2-oxobrimonidine, 3-oxobrimonidine, and 2,3-dioxobrimonidine being the major metabolites. Oxidative cleavage of the imidazoline ring to 5-bromo-6-guanidinoquinoxaline is also observed. |
| Route of elimination | Brinzolamide is eliminated predominantly in the urine as unchanged drug.N-Desethyl brinzolamide is also found in the urine along with lower concentrations of the N-desmethoxypropyl and O-desmethyl metabolites. |
Formulation & handling
- Brinzolamide is a small molecule primarily formulated for ophthalmic use as solutions or suspensions for topical administration.
- Due to its moderate water solubility and low lipophilicity (LogP -0.58), formulation strategies should consider solubilization and suspension stability.
- Handling considerations include protection from microbial contamination and physical stability of suspensions to maintain dosing consistency.
Regulatory status
| Lifecycle | The API is marketed in Canada, the EU, and the US, with key patent protections in the US expiring between 2010 and 2019, while the latest patent remains active until 2030. This indicates a mature market with ongoing patent protection primarily in the US. |
|---|
| Markets | Canada, EU, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Brinzolamide is characterized by a limited number of originator companies, with Alcon Laboratories serving as a key packager. Branded products such as Azarga and Azopt maintain a presence across major markets including the US, EU, and Canada. The presence of patents extending to 2030 indicates potential exclusive marketing rights, suggesting that generic competition is currently limited or forthcoming after patent expiry. |
|---|
Safety
| Toxicity | Developmental toxicity studies with brinzolamide in rabbits at oral doses of 1, 3, and 6 mg/kg/day (20, 60, and 120 times the recommended human ophthalmic dose) produced maternal toxicity at 6 mg/kg/day and a significant increase in the number of fetal variations, such as accessory skull bones, which was only slightly higher than the historical value at 1 and 6 mg/kg. In rats, statistically, decreased body weights of fetuses from dams receiving oral doses of 18 mg/kg/day (180 times the recommended human ophthalmic dose) during gestation were proportional to the reduced maternal weight gain, with no statistically significant effects on organ or tissue development. Increases in unossified sternebrae, reduced ossification of the skull, and unossified hyoid that occurred at 6 and 18 mg/kg were not statistically significant. No treatment-related malformations were seen. Following oral administration of 14C-brinzolamide 14Cbrinzolamide to pregnant rats, radioactivity was found to cross the placenta and was present in the fetal tissues and blood. Developmental toxicity studies performed in rats with oral doses of 0.66 mg brimonidine base/kg revealed no evidence of harm to the fetus. Dosing at this level resulted in a plasma drug concentration approximately 100 times higher than that seen in humans at the recommended human ophthalmic dose. In animal studies, brimonidine crossed the placenta and entered into fetal circulation to a limited extent. There are no adequate and well-controlled studies in pregnant women. Brinzolamide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Brinzolamide caused urinary bladder tumors in female mice at oral doses of 10 mg/kg/day and in male rats at oral doses of 8 mg/kg/day in 2-year studies. Brinzolamide was not carcinogenic in male mice or female rats dosed orally for up to 2 years. The carcinogenicity appears secondary to kidney and urinary bladder toxicity. These levels of exposure cannot be achieved with topical ophthalmic dosing in humans. The following tests for the mutagenic potential of brinzolamide were negative: (1) in vivo mouse micronucleus assay; (2) in vivo sister chromatid exchange assay; and (3) Ames E. coli test. The in vitro mouse lymphoma forward mutation assay was negative in the absence of activation, but positive in the presence of microsomal activation. In this assay, there was no consistent dose-response relationship to the increased mutation frequency and cytotoxicity likely contributed to the high mutation frequency. Carbonic anhydrase inhibitors, as a class, are not mutagenic and the weight of evidence supports that brinzolamide is consistent with the class. In reproduction studies of brinzolamide in rats, there were no adverse effects on the fertility or reproductive capacity of males or females at doses up to 18 mg/kg/day (180 times the recommended human ophthalmic dose). Brimonidine tartrate was not carcinogenic in either a 21-month mouse or 24-month rat study. In these studies, dietary administration of brimonidine tartrate at doses up to 2.5 mg/kg/day in mice and 1 mg/kg/day in rats resulted in plasma drug concentrations 80 and 120 times higher than the human plasma drug level at the recommended clinical dose, respectively. Brimonidine tartrate was not mutagenic or cytogenic in a series of in vitro and in vivo studies including the Ames test, chromosomal aberration assay in Chinese Hamster Ovary (CHO) cells, a host-mediated assay and cytogenic studies in mice, and a dominant lethal assay. In reproductive studies performed in rats with oral doses of 0.66 mg brimonidine base/kg (approximately 100 times the plasma drug concentration level seen in humans following multiple ophthalmic doses), fertility was not impaired. |
|---|
- Brinzolamide demonstrated developmental toxicity in rabbits at high oral doses (≥6 mg/kg/day) with maternal toxicity and increased fetal skeletal variations
- Placental transfer to fetal tissues was observed in rats
- Chronic oral administration of brinzolamide caused urinary bladder tumors in female mice and male rats at doses ≥8 mg/kg/day in carcinogenicity studies, likely secondary to renal and urinary toxicity
Brinzolamide is a type of Ocular preparations
Ocular preparations are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the formulation of medications and treatments for various eye conditions. These specialized formulations are designed to deliver therapeutic agents directly to the eye, ensuring maximum effectiveness and minimal systemic absorption.
Ocular preparations encompass a wide range of products, including eye drops, ointments, gels, and inserts. These formulations may contain API components such as antibiotics, corticosteroids, antihistamines, lubricants, or mydriatics, depending on the intended therapeutic purpose.
Eye drops are the most common form of ocular preparations, delivering medications in liquid form directly onto the eye surface. They are often used to treat conditions like dry eyes, glaucoma, allergies, and infections. Ointments and gels provide a more viscous consistency, enabling longer contact time with the eye surface and prolonged drug release. Inserts, such as punctal plugs, are used to deliver sustained-release medications.
Ocular preparations are formulated to ensure compatibility with the delicate structures of the eye and to enhance drug penetration. Factors like pH, osmolality, and viscosity are carefully controlled to optimize drug delivery and patient comfort. Additionally, preservatives are often added to prevent microbial contamination and maintain product stability.
In summary, ocular preparations are crucial in treating various eye conditions effectively. They provide targeted drug delivery and ensure optimal therapeutic outcomes with minimal side effects. Whether in the form of eye drops, ointments, gels, or inserts, these pharmaceutical APIs play a vital role in promoting eye health and improving patient well-being.
Brinzolamide (Ocular preparations), classified under Ophthalmic Agents
Ophthalmic agents belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category specifically designed for ophthalmic applications. These agents are formulated to treat various eye conditions and disorders. Ophthalmic agents encompass a wide range of medications, including eye drops, ointments, gels, and intraocular implants.
These agents are developed to address specific therapeutic needs related to the eyes, such as reducing intraocular pressure in glaucoma, treating inflammation and infection, relieving dryness and itching, and managing allergies. They may also be used to dilate the pupils during diagnostic procedures or surgeries.
Ophthalmic agents are formulated with precise concentrations of active ingredients to ensure efficacy and safety. Common classes of ophthalmic agents include beta-blockers, prostaglandin analogs, carbonic anhydrase inhibitors, corticosteroids, and antihistamines.
When administering ophthalmic agents, it is crucial to follow proper application techniques to ensure optimal drug delivery and minimize side effects. Eye drops, for example, are typically applied as a gentle instillation into the conjunctival sac, while ointments are applied along the lower eyelid.
These pharmaceutical API ophthalmic agents undergo rigorous quality control and regulatory scrutiny to meet industry standards and ensure patient safety. Manufacturers must comply with Good Manufacturing Practices (GMP) and adhere to stringent quality assurance protocols.
Overall, ophthalmic agents play a vital role in the management and treatment of various eye conditions, providing patients with targeted relief and improving ocular health. It is important to consult with a healthcare professional to determine the appropriate ophthalmic agent for individual needs and to receive proper guidance on usage and potential side effects.
Brinzolamide API manufacturers & distributors
Compare qualified Brinzolamide API suppliers worldwide. We currently have 15 companies offering Brinzolamide API, with manufacturing taking place in 7 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | European Union | CoA, EDMF/ASMF, GMP, GDP, MSDS, USDMF | 243 products |
| Bakul Pharma Private Limi... | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 52 products |
| Biocon | Producer | India | India | CoA, USDMF | 36 products |
| Duke Chem | Producer | Spain | Spain | CoA, GMP, JDMF, USDMF | 8 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| ICROM | Producer | Italy | Italy | CoA, GMP, JDMF, USDMF | 19 products |
| Indoco Remedies | Producer | India | India | CoA, GMP, USDMF, WC | 19 products |
| Industriale Chimica | Producer | Italy | Unknown | CoA, USDMF | 33 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Quimdis | Distributor | France | Unknown | CoA | 17 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, GMP, USDMF | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shandong Chenghui Shuangd... | Producer | China | China | BSE/TSE, CoA, ISO9001, MSDS | 98 products |
| Socosur | Distributor | France | Unknown | CoA | 21 products |
When sending a request, specify which Brinzolamide API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Brinzolamide API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
