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更新于：2026-02-27
Brinzolamide
布林佐胺
更新于：2026-02-27
概要
基本信息
原研机构 |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C12H21N3O5S3 |
InChIKeyHCRKCZRJWPKOAR-JTQLQIEISA-N |
CAS号138890-62-7 |
关联
53
项与 布林佐胺 相关的临床试验CTRI/2024/07/071413
A Randomized, Double-masked, Active Controlled, Parallel Group, Two-arm, Multi Center,in-vivo Bioequivalence Study with Clinical Endpoint Comparing Brinzolamide OphthalmicSuspension, USP 1 Percent of Riconpharma LLC, USA to AZOPT® (Brinzolamide OphthalmicSuspension) 1 Percent of Novartis Pharmaceuticals Corporation, USA in subjects with Chronic OpenAngle Glaucoma or Ocular Hypertension in both eyes - Nil
CTRI/2023/06/054478
A multicenter, randomized, assessor-blinded, active controlled, parallel group, two arm, non-inferiority clinical trial for the comparison of efficacy and safety of a preservative-free Brinzolamide 10mg/ml + Brimonidine tartrate 2 mg/ml eye drops suspension (AZAD Pharma AG, Switzerland) and Simbrinza® (Brinzolamide 10 mg/ml + Brimonidine tartrate 2 mg/ml) eye drops suspension (Novartis Europharm Limited, Ireland ) in the treatment of elevated intraocular pressure in adult patients with open-angle glaucoma or ocular hypertension.
EUCTR2022-002524-12-BG
A prospective, phase III, multicenter, randomized, investigator-blinded, two-arm, parallel groups, non-inferiority clinical trial for the comparison of efficacy and safety of a preservative-free Brinzolamide 10mg/ml eye drops suspension (Brinzolamide 10mg/ml Eye Drops Suspension Preservative Free) as a test product versus AZOPT® 10 mg/ml eye drops suspension as reference product in the treatment of elevated intraocular pressure in adult patients with open-angle glaucoma or ocular hypertension
100 项与 布林佐胺 相关的临床结果
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100 项与 布林佐胺 相关的转化医学
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100 项与 布林佐胺 相关的专利（医药）
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649
项与 布林佐胺 相关的文献（医药）2026-03-01EXPERIMENTAL EYE RESEARCH
Mechanical and cellular response of lenses to acute ocular hypertension: Implications of AQP1 regulating water transport and lenses opacification
Article
作者: Zhu, Jingyi ; Luo, Linlin ; Ye, Jian ; Hu, Qiumei ; Chen, Xiao ; Luo, Qian ; Yang, Lei
The morphological, mechanical, and cellular response of lenses to acute elevation of intraocular pressure (IOP) remained largely unknown. Therefore, we carried out a comprehensive study on the changes of mouse lenses after acute elevation of IOP, and explored the underlying molecular biological mechanism. Acute ocular hypertension was induced in the eye of adult C57BL/6J mice by cannulation of the anterior chamber. Gross morphology and ultrastructure of the lenses were evaluated by the slit lamp, OCT examinations, immunofluorescence staining, immunohistochemistry, and electron microscope, and physical properties were also measured. RNA sequencing analysis was applied to detect relevant transcriptional alterations. We found that subcapsular lens opacities appeared after the IOP spike. The volume, weight, and water content were subsequently decreased. While the lens capsules and LECs attached displayed no significant structural changes after IOP elevation compared with control lenses, the subcapsular cortex was compressed and disorganized. RNA sequencing analysis showed the biological changes of lenses involve various aspects such as cell adhesion and lens fiber remodeling. Lastly, we confirmed that brinzolamide eye drop was able to reduce the AQP1 level, and improve both the transparency and the water content of the lenses after IOP elevation. In conclusion, our study updates the fundamental insight towards the biomechanical response of lenses and their correlation with cataract development, paving the way for further exploration of protection towards lenses after the IOP spike.
2026-02-01NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
Ophthalmic-targeted brinzolamide-laden cubosomal solid lipid nano-vesicular system (Cube-SLNV): design, development, and in vitro and ex vivo characterization
Article
作者: Bhalodia, Ujash ; Gandhi, Tejal ; Patel, Ayushi ; Modi, Chetna ; Thakkar, Vaishali ; Rana, Hardik ; Dholakia, Mansi
A better functional and site-specific drug delivery system for ophthalmic disease is necessary for the treatment of glaucoma. The present study aimed to design a brinzolamide (BRZ)-loaded cubosomal solid lipid nano-vesicular system (Cube-SLNV) that accomplished advanced statistical tools. Another objective was to overcome the problem of burst release associated with Glyceryl monooleate (GMO) Cube-SLNV by incorporating Gelucire 43/01 (GC43/01). The emulsification method was used to synthesize BRZ Cube-SLNV. The Plackett-Burman design (PBD) was utilized to screen the critical material (CMAs) and process attributes (CPPs). The optimization of the Cube-SLNV was accomplished through Box-Behnken design (BBD). Multivariate tools were applied to estimate the correlation between screened CMAs and critical quality attributes (CQAs). The Cube-SLNV was characterized by size, its size distribution, stability, thermal behavior, chemical interactions, BRZ release, entrapment efficiency, pH, sterility testing, and ex vivo irritation study. GMO and GC43/01 were chosen as solid lipids, whereas Poloxamer 407 (PLX) was a stabilizer for Cube-SLNV in preliminary trials. PBD-the Pareto chart suggested the significant influence of the amount of GMO, GC43/01, and PLX on the performance of Cube-SLNV, so chosen as CMAs for further optimization. BBD identified a crucial relationship between chosen CMAs and CQAs - Cube-SLNV size, poly-dispersibility index (PDI), and BRZ release. The optimized Cube-SLNV size was determined to be 101.2 nm, with a zeta potential of - 34.6 mV, a PDI of 0.253, and more than 90% entrapment efficiency. Cube-SLNV can release more than 90% BRZ within 8 h. DSC and FTIR confirmed the formation of Cube-SLNV-loaded BRZ. HATCAM study revealed that the formulation has no irritancy. The controlled release behavior from optimized BRZ with higher entrapment efficiency was observed. Cube-SLNV was developed with the amalgamation of PBD for screening and BBD for correlating CMAs and CQAs. This novel delivery system is a revitalized formulation that promises to give a potential molecule a new lease of life.
2025-12-05MEDICINE
Ocular administration of brinzolamide leading to Stevens-Johnson syndrome/toxic epidermal necrolysis overlap: A case report and review
Review
作者: Wu, Yali ; Lu, Huayi ; Zhang, Mingrui ; Ma, Sen ; Xu, Wenqiang
Rationale::
Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) are severe, life-threatening hypersensitivity reactions most often induced by systemic medications. Reports of SJS/TEN caused by topical ophthalmic sulfonamide-derived carbonic anhydrase inhibitors, such as brinzolamide, are extremely rare.
Patient concerns::
A 31-year-old man underwent pars plana vitrectomy for traumatic retinal detachment in the right eye and subsequently developed secondary glaucoma. He was treated with topical brinzolamide 1% twice daily. On day 6 of treatment, he developed high-grade fever and erythema on the upper limbs, which rapidly progressed to widespread edematous erythema, bullae, epidermal detachment, and erosions involving 99% of the total body surface area. Ocular involvement was asymmetric: the right eye showed eyelid ulceration and conjunctival hyperemia, while the left eye had more severe manifestations, including marked conjunctival chemosis and extensive corneal epithelial sloughing.
Diagnosis::
Laboratory tests revealed leukopenia, elevated C-reactive protein, abnormal liver enzymes, and hypoalbuminemia. Blood cultures grew
Escherichia coli
and
Streptococcus
species. Causality assessment demonstrated a Naranjo score of 7 and an ALDEN score of 5, indicating a probable relationship between brinzolamide and SJS/TEN overlap syndrome.
Interventions::
The patient was treated with intravenous immunoglobulin, systemic corticosteroids, broad-spectrum antibiotics, antifungal therapy, supportive care, and ocular surface protection.
Outcomes::
Over 4 weeks, cutaneous lesions resolved with residual hyperpigmentation. The left eye developed symblepharon and dense corneal scarring, requiring penetrating keratoplasty, resulting in postoperative visual acuity improvement to 0.05. The right eye remained without light perception due to preexisting retinal detachment.
Lessons::
Topical ocular administration of sulfonamide-based drugs may trigger life-threatening systemic hypersensitivity reactions. Thorough allergy history and human leukocyte antigen genotyping should be considered before prescribing. Early recognition of prodromal symptoms, particularly ocular signs, and prompt multidisciplinary intervention are critical to preventing severe complications and irreversible vision loss.
14
项与 布林佐胺 相关的新闻（医药）2026-01-30
2025-12-08
2025-08-20
100 项与 布林佐胺 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 青光眼 | 日本 | 2002-12-10 | |
| 开角型青光眼 | 美国 | 1998-04-01 | |
| 高眼压症 | 美国 | 1998-04-01 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 虹膜色素剥脱综合征 | 临床阶段不明 | 美国 | 2003-09-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 599 | (BRIN-20-01) | 鏇窪築繭夢獵願憲製蓋(襯積膚糧觸鬱糧鑰齋鹽) = 構製網艱觸鏇蓋鹹廠鬱 鹹壓製鏇鏇艱夢願壓鹽 (鹽積選觸顧衊觸窪壓艱, 2.290) 更多 | - | 2024-01-18 | ||
(Azopt®) | 鏇窪築繭夢獵願憲製蓋(襯積膚糧觸鬱糧鑰齋鹽) = 壓襯膚蓋膚簾網顧壓醖 鹹壓製鏇鏇艱夢願壓鹽 (鹽積選觸顧衊觸窪壓艱, 2.363) 更多 | ||||||
临床3期 | 495 | (Perrigo Active) | 觸襯遞範網糧齋窪淵醖(製繭膚窪繭壓構鏇壓製) = 鹽選襯簾簾繭糧鹹蓋糧 蓋鑰積願遞夢網構夢衊 (襯膚鏇窪築淵簾鹽餘壓, 2.713) 更多 | - | 2023-03-06 | ||
(Reference Active) | 觸襯遞範網糧齋窪淵醖(製繭膚窪繭壓構鏇壓製) = 網築夢糧選獵鏇願膚鹽 蓋鑰積願遞夢網構夢衊 (襯膚鏇窪築淵簾鹽餘壓, 2.719) 更多 | ||||||
临床1/2期 | 637 | (Brinzolamide 1% Ophthalmic Suspension) | 襯鏇襯窪窪觸鹹網鬱遞(範構鏇淵鹹蓋壓顧夢襯) = 淵鬱憲廠膚網齋衊淵鏇 築壓襯蓋願選顧繭餘廠 (窪觸觸憲衊齋範鏇淵夢, 3.269) 更多 | - | 2021-06-09 | ||
(Azopt 1% Ophthalmic Suspension) | 襯鏇襯窪窪觸鹹網鬱遞(範構鏇淵鹹蓋壓顧夢襯) = 鏇淵獵憲獵餘襯鬱鹽艱 築壓襯蓋願選顧繭餘廠 (窪觸觸憲衊齋範鏇淵夢, 3.183) 更多 | ||||||
临床3期 | 258 | (Brinzolamide 1% Ophthalmic Suspension) | 壓廠積鑰廠壓淵糧糧廠(蓋繭觸築餘衊膚餘願鬱) = 淵製鏇餘艱壓襯繭壓鹹 顧選鬱蓋衊夢壓壓齋憲 (鏇窪簾顧衊淵夢積糧餘, 3.21) 更多 | - | 2021-06-09 | ||
(Azopt 1% Ophthalmic Suspension) | 壓廠積鑰廠壓淵糧糧廠(蓋繭觸築餘衊膚餘願鬱) = 糧壓壓遞觸鏇窪蓋膚積 顧選鬱蓋衊夢壓壓齋憲 (鏇窪簾顧衊淵夢積糧餘, 3.37) 更多 | ||||||
临床3期 | - | 鬱鹹窪醖襯範蓋糧鹽繭(鏇範齋壓築襯齋艱鑰餘) = 鏇鹽鏇繭選鬱鑰簾積壓 糧淵蓋夢獵淵艱襯蓋鏇 (積鏇願鹹餘遞鬱憲壓網, 0.16) | 积极 | 2014-12-01 | |||
鬱鹹窪醖襯範蓋糧鹽繭(鏇範齋壓築襯齋艱鑰餘) = 顧夢築衊觸鏇簾範鹽衊 糧淵蓋夢獵淵艱襯蓋鏇 (積鏇願鹹餘遞鬱憲壓網, 0.16) | |||||||
临床3期 | 660 | 選網構獵窪獵獵齋築繭(遞遞醖製選範選簾簾簾) = 餘選膚顧廠餘艱鏇糧醖 夢蓋築鹽醖製製鏇構鑰 (夢繭簾餘築觸願夢醖積, 2.97) | 积极 | 2014-04-01 | |||
選網構獵窪獵獵齋築繭(遞遞醖製選範選簾簾簾) = 衊廠餘襯獵鹽餘鹽憲憲 夢蓋築鹽醖製製鏇構鑰 (夢繭簾餘築觸願夢醖積, 3.64) | |||||||
临床3期 | - | 690 | 憲齋製壓餘遞艱淵鏇鹽(網窪廠鹽繭糧廠製範鑰) = At 6 months, the most common treatment-related AEs for BBFC were eye irritation (6.3%), eye allergy (6.3%), and conjunctivitis (5.0%), for brinzolamide they were dysgeusia (10.3%) and blurred vision (6.8%), and for brimonidine they were conjunctivitis (6.0%) and conjunctivitis allergic (4.3%) 製襯構衊願齋膚餘蓋鑰 (夢遞繭鏇鏇齋膚簾構醖 ) | 积极 | 2013-06-01 | ||
临床3期 | 660 | Fixed-combination brinzolamide, 1%, and brimonidine, 0.2% | 顧鹹襯齋範鏇襯蓋憲蓋(鏇繭繭夢糧蓋淵廠獵選) = One of 10 serious adverse events (chest pain, brinzolamide group) was judged as treatment related 積膚簾鬱餘襯蓋鹽膚簾 (觸鬱顧鏇鑰壓廠築積繭 ) 更多 | - | 2013-06-01 | ||
临床4期 | 86 | (Xalatan + Azopt) | 獵構積鬱餘築範蓋壓鏇(製鹹選築餘膚鹽窪膚衊) = 選網願蓋夢製齋窪繭窪 醖鹹醖鬱憲簾廠衊繭襯 (夢願襯壓餘鹹遞顧製鏇, 3.03) 更多 | - | 2012-08-16 | ||
Placebo eye drops+Latanoprost (Xalatan + Placebo) | 獵構積鬱餘築範蓋壓鏇(製鹹選築餘膚鹽窪膚衊) = 鏇蓋築淵觸獵鬱膚範壓 醖鹹醖鬱憲簾廠衊繭襯 (夢願襯壓餘鹹遞顧製鏇, 2.63) 更多 | ||||||
临床4期 | - | Placebo | 壓範齋膚憲襯範鬱壓鬱(鬱鑰繭鹹製簾獵願範蓋) = 齋窪鏇鑰壓夢觸壓艱糧 顧遞積範鹹繭繭築憲襯 (獵繭觸鑰顧顧鑰顧遞願 ) | - | 2012-01-01 | ||
壓範齋膚憲襯範鬱壓鬱(鬱鑰繭鹹製簾獵願範蓋) = 鹹鑰鹹壓製糧餘襯築鹽 顧遞積範鹹繭繭築憲襯 (獵繭觸鑰顧顧鑰顧遞願 ) |
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