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Brinzolamide

Generic Name
Brinzolamide
Brand Names
Azarga, Azopt, Simbrinza
Drug Type
Small Molecule
Chemical Formula
C12H21N3O5S3
CAS Number
138890-62-7
Unique Ingredient Identifier
9451Z89515

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

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.
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