Overview
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase II (CA-II) inhibitor indicated to reduce ocular pressure in patients with ocular hypertension or open-angle glaucoma. Although the exact pathophysiology of glaucoma is still unknown, one of the main hallmarks of this disease is vascular dysregulation and abnormalities. The resulting vascular resistance increases intraocular pressure, thus impairing ocular perfusion. Although systemic anti-carbonic anhydrase (CA) therapy has been used for almost 50 years with varying degrees of success, systemic administration results in an increase in incidences of adverse effects. Brinzolamide was developed as a topical solution to the systemic side effects and dorzolamide, the first-ever approved topical CA inhibitor with contrasting results and evidence. Unlike dorzolamide, brinzolamide has a higher lipophilicity to facilitate diffusion across the blood-retinal barrier. Brinzolamide was approved by the FDA in 1998 as a standalone product and in 2013 as a combination product with brimonidine tartrate. In Europe, it was also approved as a combination product with timolol in 2008.
Background
Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase II (CA-II) inhibitor indicated to reduce ocular pressure in patients with ocular hypertension or open-angle glaucoma. Although the exact pathophysiology of glaucoma is still unknown, one of the main hallmarks of this disease is vascular dysregulation and abnormalities. The resulting vascular resistance increases intraocular pressure, thus impairing ocular perfusion. Although systemic anti-carbonic anhydrase (CA) therapy has been used for almost 50 years with varying degrees of success, systemic administration results in an increase in incidences of adverse effects. Brinzolamide was developed as a topical solution to the systemic side effects and dorzolamide, the first-ever approved topical CA inhibitor with contrasting results and evidence. Unlike dorzolamide, brinzolamide has a higher lipophilicity to facilitate diffusion across the blood-retinal barrier. Brinzolamide was approved by the FDA in 1998 as a standalone product and in 2013 as a combination product with brimonidine tartrate. In Europe, it was also approved as a combination product with timolol in 2008.
Indication
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.
Associated Conditions
- Increased Intra Ocular Pressure (IOP)
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2021/08/26 | Phase 3 | Completed | |||
2019/07/18 | Phase 3 | Completed | |||
2019/04/01 | Phase 1 | Completed | |||
2018/05/31 | Phase 2 | UNKNOWN | |||
2017/05/12 | Phase 4 | Completed | |||
2016/05/12 | Phase 4 | Completed | |||
2016/04/07 | Phase 4 | Terminated | |||
2015/04/17 | Phase 4 | Completed | |||
2015/03/17 | Phase 3 | Completed | |||
2015/01/15 | Phase 3 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Alcon Laboratories, Inc. | 0065-4147 | OPHTHALMIC | 10 mg in 1 mL | 5/16/2023 | |
Bausch & Lomb Incorporated | 24208-464 | OPHTHALMIC | 10 mg in 1 mL | 7/7/2023 | |
Novartis Pharmaceuticals Corporation | 0078-0722 | OPHTHALMIC | 10 mg in 1 mL | 8/2/2021 | |
Oceanside Pharmaceuticals. | 68682-464 | OPHTHALMIC | 10 mg in 1 mL | 7/1/2021 | |
Bryant Ranch Prepack | 72162-2201 | OPHTHALMIC | 10 mg in 1 mL | 12/19/2023 | |
Sandoz Inc | 0781-6014 | OPHTHALMIC | 10 mg in 1 mL | 11/4/2015 | |
Actavis Pharma, Inc. | 0591-2127 | OPHTHALMIC | 10 mg in 1 mL | 7/21/2023 | |
Padagis US LLC | 0574-4012 | OPHTHALMIC | 10 mg in 1 mL | 7/28/2023 | |
Bryant Ranch Prepack | 63629-8793 | OPHTHALMIC | 10 mg in 1 mL | 9/10/2021 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 11/25/2008 | ||
Authorised | 7/18/2014 | ||
Authorised | 3/9/2000 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
SIMBRINZA EYE DROPS, SUSPENSION 10 MG/ML + 2 MG/ML | SIN15085P | SUSPENSION, STERILE | 10 mg/mL | 9/6/2016 | |
AZOPT OPHTHALMIC SUSPENSION 1% | SIN11029P | SOLUTION | 10 mg/ml | 7/19/1999 | |
Azarga 10mg/mL + 5mg/mL eye drops, suspension | SIN13802P | SUSPENSION, STERILE | 10mg/mL | 5/19/2010 | |
BRITIL EYE DROPS, SUSPENSION 1% w/v | SIN17215P | SUSPENSION, STERILE | 10.00mg/mL | 4/8/2025 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
Brinzolamide Eye Drops | 国药准字HJ20140976 | 化学药品 | 滴眼剂 | 1/31/2024 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
No PPB approvals found for this drug. |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
BRINZOQUIN 1.0% brinzolamide 10mg/mL eye drops | 99179 | Medicine | A | 5/20/2004 | |
AZOPT 1.0% brinzolamide 10mg/mL eye drops bottle | 72750 | Medicine | A | 11/6/2000 | |
SIMBRINZA 1%/0.2% brinzolamide 1% and brimonidine tartrate 0.2% eye drops suspension bottle | 219839 | Medicine | A | 11/20/2014 | |
AZARGA brinzolamide 1% and timolol 0.5% eye drops. | 156500 | Medicine | A | 2/5/2010 |