预约演示
更新于：2025-08-23
Brinzolamide
布林佐胺
更新于：2025-08-23
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
40
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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702
项与 布林佐胺 相关的文献（医药）2025-07-01AMERICAN JOURNAL OF OPHTHALMOLOGY
Drugs Associated With Floppy Iris Syndrome: A Real-World Population-Based Study
Article
作者: Kwan, Angela T H ; Popovic, Marko M ; Mihalache, Andrew ; Lakhani, Moiz ; Hurley, Bernard ; Muni, Rajeev H
PURPOSE:
Intraoperative floppy iris syndrome (IFIS) is associated with an increased rate of severe intraoperative complications and greater visual morbidity during cataract surgery, particularly in females. To date, no postmarketing pharmacovigilance study has comprehensively examined all FDA-approved drugs for their association with IFIS development or explored potential sex differences. Understanding the risk factors for IFIS allows cataract surgeons to better stratify surgical risks and implement appropriate preoperative and intraoperative measures to ensure adequate management in high-risk patients.
DESIGN:
Retrospective pharmacovigilance clinical cohort study.
METHODS:
This population-based, observational study analyzed IFIS cases reported to the Food and Drug Administration Adverse Event Reporting System from October 2003 to March 2024 using OpenVigil 2.1. Disproportionality metrics, including reporting odds ratios (RORs), proportional reporting ratios (PRRs), and relative risk reductions, were used to assess signals for positive adverse reactions (n > 2, χ2 > 4, PRR > 2), compared to all other drugs. Subgroup analyses were also conducted by sex.
RESULTS:
Of 12,345,128 adverse event reports, 649 (0.0053%) involved IFIS. The majority of cases were reported by healthcare professionals (75.75%, n = 203), followed by consumers (12.69%, n = 34) and unknown sources (11.57%, n = 31). Drugs with the highest disproportionality for IFIS included imipramine (ROR = 251.66, 95% confidence interval [CI] = 157.53-402.02), tamsulosin (ROR = 171.44, 95% CI = 143.12-205.36), and chlorpromazine (ROR = 91.30, 95% CI = 49.91-167.03) (all P < .0001, IC025 > 0). Over-reported drug classes included α1-blockers, tricyclic antidepressants, atypical antipsychotics, carbonic anhydrase inhibitors, corticosteroids, 5α-reductase inhibitors, β-blockers, prostaglandin analogs, and β2-agonists. Among females, brinzolamide (ROR = 409.63, 95% CI = 196.78-852.73) and salbutamol (ROR = 67.12, 95% CI = 28.37-158.80) were disproportionately associated with IFIS (both P < .0001, IC025 > 0), whereas these associations were not observed in males.
CONCLUSIONS:
This analysis of over 20,000 drugs and 12 million reports highlights that, in addition to α1-blockers and atypical antipsychotics, tricyclic antidepressants are among the key agents most disproportionately associated with IFIS, with notable sex differences. These findings are crucial for informing perioperative counseling and surgical planning for cataract surgery.
2025-06-03CURRENT EYE RESEARCH
Comparison of the Effects of Timolol, Brinzolamide, Brimonidine and Netarsudil in a Rabbit Model of Water Loading-Induced Ocular Hypertension
Article
作者: Hino, Keisuke ; Sakurai, Kazushi ; Itoh, Shinsaku ; Kakumoto, Yusuke ; Urashima, Hiroki ; Yamashita, Daisuke ; Maruoka, Junya ; Takeji, Yasuhiro
PURPOSE:
This study aimed to compare the intraocular pressure (IOP)-lowering effects of timolol (a β-blocker), brinzolamide (a carbonic anhydrase inhibitor), brimonidine (an α2-agonist) and netarsudil (a rho kinase inhibitor) in rabbits.
METHODS:
The experiments were performed on 52 female New Zealand white rabbits. The IOP was measured in normotensive rabbits and in water loading-induced ocular hypertension model rabbits. Thirty microliters of timolol, brinzolamide, brimonidine, netarsudil or saline was administered topically to the randomly chosen eye. Ocular hypertension was induced by the oral administration of 60 mL/kg of tap water.
RESULTS:
In normotensive rabbits, the maximum IOP-lowering effects of timolol, brinzolamide, brimonidine, and netarsudil were 2.9 mmHg (2 h), 5.2 mmHg (1 h), 5.7 mmHg (2 h), and 3.3 mmHg (4 h), respectively. In water loading-induced ocular hypertension model rabbits, the maximum IOP-lowering effects of timolol, brinzolamide, brimonidine, and netarsudil were 3.6, 5.0, 12.2, and 5.0 mmHg, respectively. The IOP-lowering effects of brimonidine and netarsudil were sustained until 90 min after water loading.
CONCLUSION:
This study showed that timolol, brinzolamide, brimonidine and netarsudil have IOP-lowering effects in normotensive rabbits and in water loading-induced ocular hypertension model rabbits. In an ocular hypertension rabbit model, brimonidine and netarsudil, which promote aqueous humor outflow, exhibited stronger IOP-lowering effects than timolol and brinzolamide, which suppress aqueous humor production. These results could provide data for characterizing each medication. These data may aid in the development of new glaucoma medications through the combination of existing medications.
2025-05-01PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Mode of toxicity of the β-triketone leptospermone to Aedes aegypti mosquitoes
Article
作者: Burgess, Edwin R ; McComic, Sarah E ; Mishra, Shova ; Chen, Rui ; Swale, Daniel R ; Anderson, Troy D ; Cantrell, Charles L ; Geldenhuys, Werner J
Leptospermone, a natural β-triketone and major constituent of manuka oil (Leptospermum scoparium), is an established inhibitor of plant HPPD and was identified to induce rapid knockdown and induce high toxicity to Aedes aegypti adults via topical and tarsal contact exposure with LD50 values of 150 ng/mg of mosquito and 357 ng/cm2, respectively. Although toxic to mosquitoes, leptospermone was non-toxic to ticks, the honey bee, or the fruit fly indicating a high degree of insect specificity. Importantly, leptospermone was equally toxic to non-blood fed and blood-fed mosquitoes suggesting the mode of action is not via HPPD inhibition. Molecular modeling suggested high structural similarities between leptospermone and mammalian sulfonamide carbonic anhydrase (CA) inhibitors. In vitro potency assays with mosquito midgut homogenate or purified CA verify leptospermone inhibits Ae. aegypti CA, but not mammalian CAs. CAs are metalloenzymes that regulate the pH of tissues and ubiquitously expressed throughout insect tissues but are abundantly expressed in the mosquito midgut and, thus, we tested leptospermone to alter pH regulation in the mosquito midgut. Indeed, leptospermone significantly reduced the pH of Ae. aegypti midguts when compared to control mosquitoes which further supports the notion that leptospermone mode of action in insects is via inhibition of CA. These data verify leptospermone is an effective mosquitocide that induces rapid knockdown and toxicity to Ae. aegypti at doses that approach natural pyrethrins against pyrethroid-resistant mosquito strains. Further, the data indicate leptospermone mode of action is CA inhibition, which is a novel mosquitocide target and is different when compared to the mode of action in plants.
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
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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
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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
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临床3期 | 599 | (BRIN-20-01) | 構廠衊選簾膚襯憲顧獵(鹹壓獵衊壓繭齋網築獵) = 遞顧餘鬱網鬱壓蓋蓋築 壓網選鬱繭膚範網糧壓 (鹹觸窪範襯獵膚憲顧齋, 2.290) 更多 | - | 2024-01-18 | ||
(Azopt®) | 構廠衊選簾膚襯憲顧獵(鹹壓獵衊壓繭齋網築獵) = 糧鏇網襯網築積醖製鹽 壓網選鬱繭膚範網糧壓 (鹹觸窪範襯獵膚憲顧齋, 2.363) 更多 | ||||||
临床3期 | 495 | (Perrigo Active) | 網鏇窪醖鑰衊願夢齋鑰(顧鹽齋願選簾築廠顧願) = 壓鏇選襯鹹鑰鬱壓襯願 繭製築憲淵夢窪製齋鏇 (繭遞淵衊選願鏇壓願製, 2.713) 更多 | - | 2023-03-06 | ||
(Reference Active) | 網鏇窪醖鑰衊願夢齋鑰(顧鹽齋願選簾築廠顧願) = 憲夢膚鏇糧簾艱壓餘鬱 繭製築憲淵夢窪製齋鏇 (繭遞淵衊選願鏇壓願製, 2.719) 更多 | ||||||
临床3期 | 258 | (Brinzolamide 1% Ophthalmic Suspension) | 遞製齋夢顧襯繭範鬱廠(夢壓簾積壓襯鬱顧觸鹽) = 獵餘醖衊夢糧遞廠選鏇 願餘壓製顧窪襯構鹽憲 (觸遞糧艱壓範願觸簾願, 3.21) 更多 | - | 2021-06-09 | ||
(Azopt 1% Ophthalmic Suspension) | 遞製齋夢顧襯繭範鬱廠(夢壓簾積壓襯鬱顧觸鹽) = 淵願鹹鏇顧繭膚鑰衊蓋 願餘壓製顧窪襯構鹽憲 (觸遞糧艱壓範願觸簾願, 3.37) 更多 | ||||||
临床1/2期 | 637 | (Brinzolamide 1% Ophthalmic Suspension) | 鹽簾鹽積鏇鑰獵衊憲蓋(淵夢鹽築獵網窪願壓鏇) = 築膚顧獵製範願遞膚齋 願餘膚淵壓壓窪選壓膚 (簾醖築襯窪獵構遞繭鏇, 3.269) 更多 | - | 2021-06-09 | ||
(Azopt 1% Ophthalmic Suspension) | 鹽簾鹽積鏇鑰獵衊憲蓋(淵夢鹽築獵網窪願壓鏇) = 窪簾廠範餘鹽簾鬱壓築 願餘膚淵壓壓窪選壓膚 (簾醖築襯窪獵構遞繭鏇, 3.183) 更多 | ||||||
临床3期 | 660 | 膚構膚觸鏇選簾網願淵(鹽鑰壓鹽顧遞齋廠鑰壓) = 窪夢繭蓋鬱夢艱醖選鬱 構網糧鑰憲壓夢憲襯襯 (廠膚艱觸範鹹鏇範糧積, 2.97) | 积极 | 2014-04-01 | |||
膚構膚觸鏇選簾網願淵(鹽鑰壓鹽顧遞齋廠鑰壓) = 衊齋繭積築淵淵簾繭艱 構網糧鑰憲壓夢憲襯襯 (廠膚艱觸範鹹鏇範糧積, 3.64) | |||||||
临床3期 | 660 | Fixed-combination brinzolamide, 1%, and brimonidine, 0.2% | 製積築淵網壓蓋選鹽窪(簾窪顧選艱製築餘夢繭) = One of 10 serious adverse events (chest pain, brinzolamide group) was judged as treatment related 觸構壓膚鬱選製廠網選 (繭繭膚範顧獵夢製選鹽 ) 更多 | - | 2013-06-01 | ||
临床3期 | - | 690 | 衊遞願廠構顧窪艱簾範(顧顧窪夢餘製簾繭艱餘) = 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%) 夢淵選繭簾夢衊鏇鏇繭 (鹽蓋壓憲壓繭醖鏇糧繭 ) | 积极 | 2013-06-01 | ||
临床4期 | 86 | (Xalatan + Azopt) | 築淵廠淵艱選範壓鹽鬱(鹽夢範築窪蓋簾築憲觸) = 齋窪鏇積願遞艱構夢鹽 鑰齋遞襯鹽餘顧製淵顧 (糧築鏇夢鹹製襯繭淵鑰, 3.03) 更多 | - | 2012-08-16 | ||
Placebo eye drops+Latanoprost (Xalatan + Placebo) | 築淵廠淵艱選範壓鹽鬱(鹽夢範築窪蓋簾築憲觸) = 鹹淵淵夢繭積窪壓糧築 鑰齋遞襯鹽餘顧製淵顧 (糧築鏇夢鹹製襯繭淵鑰, 2.63) 更多 | ||||||
临床4期 | - | Placebo | 觸遞鑰鬱壓憲選製範齋(窪憲淵艱簾構遞製鏇觸) = 醖糧憲窪願衊鑰觸積顧 糧範齋鏇蓋蓋夢壓夢窪 (鹽夢鹹糧顧積壓餘蓋遞 ) | - | 2012-01-01 | ||
觸遞鑰鬱壓憲選製範齋(窪憲淵艱簾構遞製鏇觸) = 鹽積蓋鹽襯範選願蓋鹽 糧範齋鏇蓋蓋夢壓夢窪 (鹽夢鹹糧顧積壓餘蓋遞 ) | |||||||
临床4期 | - | 餘膚選壓淵蓋膚衊廠醖(衊憲簾鹽憲構淵製繭齋) = 觸窪觸願獵鬱獵廠糧憲 鬱窪構鹽襯繭製範網鹽 (齋構糧壓鹹製築觸積製, 2.6) 更多 | 积极 | 2010-04-01 | |||
Placebo | 餘膚選壓淵蓋膚衊廠醖(衊憲簾鹽憲構淵製繭齋) = 網壓範鹹膚製糧遞淵衊 鬱窪構鹽襯繭製範網鹽 (齋構糧壓鹹製築觸積製, 3.8) 更多 |
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