布林佐胺噻吗洛尔(Brinzolamide/Timolol Maleate) - 药物靶点：CA2 x β-adrenoceptors_在研适应症：青光眼，开角型青光眼，高眼压症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Azarga、Brinzolamide and Timolol Maleate、Brinzolamide/timolol

+ [5]

靶点

CA2 x β-adrenoceptors

作用机制

CA2抑制剂(碳酸酐酶II抑制剂)、β-adrenoceptors拮抗剂(β-肾上腺素能受体家族拮抗剂)

治疗领域

眼部疾病

在研适应症

青光眼开角型青光眼高眼压症

非在研适应症-

原研机构

Alcon AG

在研机构

Novartis Pharma AGNovartis Europharm Ltd.Alcon Laboratories UK Ltd.

非在研机构

Novartis AGAlcon Research Ltd.

最高研发阶段批准上市

首次获批日期

欧盟 (2008-11-25),

开角型青光眼高眼压症

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C25H45N7O8S4

InChIKeyYPIMJBXEIGRISS-LARVRRBISA-N

CAS号1110563-69-3

关联

23

项与布林佐胺噻吗洛尔相关的临床试验

NCT02325518 / Completed临床4期

The Efficacy and Safety of Brinzolamide 1%/Timolol 0.5% Fixed Combination Versus Dorzolamide 1%/Timolol 0.5% in Patients With Open-Angle Glaucoma and Ocular Hypertension

The purpose of this study is to evaluate AZORGA® Ophthalmic Suspension compared to COSOPT® Ophthalmic Solution for IOP-lowering efficacy in subjects with open-angle glaucoma or ocular hypertension.

开始日期2014-12-01

申办/合作机构

Alcon AG

NCT03966560 / Completed临床4期IIT

Choroidal Thickness and Its Correlations With Ocular Parameters in Cases With Primary Open-angle Glaucoma

Glaucoma is one of the leading causes of blindness worldwide that is a chronic public health problem. Unfortunately, glaucoma can be diagnosed when the disease reaches a certain level in today's conditions. The aim of this study was to investigate the diagnostic methods that can diagnose glaucoma before it reaches the advanced level and to identify pathophysiological processes. In this study, choroidal thickness was investigated in primary open-angle glaucoma cases and its correlations with OCT and multifocal ERG parameters were evaluated.

开始日期2014-01-01

申办/合作机构

Afyon Kocatepe University

NCT01514734 / Terminated临床4期

Assessing the Efficacy and Tolerability of AZARGA® (Brinzolamide 1%/Timolol 0.5% Fixed Combination) as Replacement Therapy in Patients on Brimonidine 0.2%/Timolol 0.5% Fixed Combination Therapy (COMBIGAN®) in Brazil

The purpose of this study was to assess the efficacy and tolerability of changing to AZARGA® from prior COMBIGAN® pharmacotherapy in patients with open-angle glaucoma or ocular hypertension.

开始日期2012-03-01

申办/合作机构

Alcon Research Ltd.

100 项与布林佐胺噻吗洛尔相关的临床结果

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100 项与布林佐胺噻吗洛尔相关的转化医学

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100 项与布林佐胺噻吗洛尔相关的专利（医药）

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10

项与布林佐胺噻吗洛尔相关的文献（医药）

2023-12-01·American Journal of Ophthalmology Case Reports

PreserFlo Microshunt for the management of intraocular pressure elevation in iridocorneal endothelial syndrome

作者: Ruparelia, Sunil ; Eadie, Brennan D ; Darwich, Rami

PurposeTo report on a case of angle-closure glaucoma secondary to iridocorneal endothelial (ICE) syndrome effectively managed with the PreserFlo Microshunt.ObservationsWe report successful implantation of a PreserFlo Microshunt in a 57-year-old patient with secondary angle-closure glaucoma in the context of ICE syndrome. Following failure of medical therapy to adequately control intraocular pressure (IOP), the patient was consented for surgical intervention and underwent combined cataract surgery and PreserFlo Microshunt implantation. IOP at the last post-operative follow-up (5 months) was 12 mmHg with the patient on brinzolamide/timolol maleate (Azarga®). We report no complications in the post-operative period.Conclusions and importanceThe PreserFlo Microshunt may be a promising option for patients with ICE syndrome who fail medical therapy. Implantation of this device was well tolerated in the presented case.

2023-10-17·Biomolecules

HIF-1α Reduction by Lowering Intraocular Pressure Alleviated Retinal Neovascularization.

Article

作者: Yang, Ziqi ; Liu, Xialin ; Ni, Biyan ; Zhou, Tian ; Huang, Zijing ; He, Chang ; Zhou, Hong ; Zhou, Yang ; Lin, Shiya

Hypoxia-induced retinal neovascularization is a leading cause of blindness worldwide. Oxygen-induced retinopathy (OIR) mouse, a well-established angiogenesis model, has been extensively used to evaluate the effect of anti-angiogenic agents through intravitreal injection. Here, we serendipitously found that the needles used for intravitreal injection caused an unexpected "anti-angiogenic" effect in the OIR mice. To evaluate the effects of various intravitreal puncture sizes on retinal neovascularization and explore the potential underlying mechanism, intravitreal punctures using 0.5 mm (25 G), 0.3 mm (30 G), or 0.21 mm (33 G) needles were performed in OIR mice. Compared with 0.3 mm and 0.21 mm puncture, the 0.5 mm puncture remarkably suppressed the formation of pathological angiogenesis, inhibited vascular leakage, and remodeled the retinal vasculature. Mechanistically, the 0.5 mm puncture induced a substantial reduction in intraocular pressure (IOP), leading to an improvement in oxygen partial pressure (pO₂) and significant reduction in Hif1a expression, resulting in resolution of angiogenic and inflammatory responses. Furthermore, IOP-lowering drugs, Travatan or Azarga, also promoted the alleviation of hypoxia and exhibited a potent anti-angiogenesis efficacy. Our study revealed an acute and significant reduction in IOP caused by a large puncture, which could remarkably suppress HIF-1α-mediated retinal neovascularization, indicating that lowering IOP may be a promising therapeutic avenue for treating retinal neovascular diseases.

2022-01-01·Vestnik oftal'mologii

Efficacy and safety of a fixed combination drug Brinzolol Duo in the treatment of patients with primary open-angle glaucoma

Article

作者: Loskutov, I A ; Poromov, A A ; Bleskina, M Yu ; Lisitsyn, A B ; Kolotilina, N E

PURPOSETo evaluate the efficacy and safety of a new fixed combination of brinzolamide and timolol in patients with stages I and II of primary open-angle glaucoma (POAG).MATERIAL AND METHODSStudy patients were divided into 2 groups. The patients of the first group were prescribed Brinzolol Duo, the second group received an original drug Azarga. Regimen for both drugs was 1 drop 2 times per day for 84 days. The study included 7 monitoring visits: visit 0 (screening - 124 patients), visit 1 (randomization and treatment initiation - 120 patients), visits 2-4 (therapy), visit 5 (end of therapy - 117 patients), visit 6 (follow-up, study completion).RESULTSOut of 120 patients included in the study, 117 subjects had completed all study procedures. It was shown that both compared drugs significantly reduce intraocular pressure (IOP). After 3 months, 46.5% of patients in the Brinzolol Duo group and 46.9% of patients in the Azarga group had IOP lowered by more than 30% compared to baseline, with IOP amounting to ≤18 mm Hg in 36.6% and 30.2% of patients, respectively. Hypotensive efficacy and safety of the drugs were comparable between the groups (p>0.05). The drugs were well tolerated, all adverse events (AEs) were mild or moderate in severity.CONCLUSIONThe new drug Brinzolol Duo (brinzolamide + timolol) significantly reduces IOP in POAG patients with efficacy comparable to Azarga.

100 项与布林佐胺噻吗洛尔相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	S01ED51	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
青光眼	日本	Novartis Pharma AG	2013-09-20
开角型青光眼	欧盟	Novartis Europharm Ltd.	2008-11-25
开角型青光眼	挪威	Novartis Europharm Ltd.	2008-11-25
开角型青光眼	冰岛	Novartis Europharm Ltd.	2008-11-25
开角型青光眼	列支敦士登	Novartis Europharm Ltd.	2008-11-25
高眼压症	冰岛	Novartis Europharm Ltd.	2008-11-25
高眼压症	挪威	Novartis Europharm Ltd.	2008-11-25
高眼压症	欧盟	Novartis Europharm Ltd.	2008-11-25
高眼压症	列支敦士登	Novartis Europharm Ltd.	2008-11-25

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
开角型青光眼	临床3期	-	Alcon Research Ltd.	2010-11-01
青光眼	临床3期	美国	Novartis AG	-
高眼压症	临床3期	美国	Novartis AG	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01514734 (CTgov)	临床4期	青光眼	9	Brinzolamide/timolol maleate fixed combination	(構構築膚齋夢餘淵繭糧) = 衊鏇製構廠鏇繭積衊廠選獵衊獵鹹艱願網獵願 (繭構餘遞築蓋窪齋醖願, 壓艱餘獵簾廠淵醖構窪 ~ 醖積襯構網簾積繭鏇觸) 更多	-	2013-10-21
NCT01263444 (CTgov)	临床4期	青光眼	47	Habitual prostaglandin monotherapy+Brinzolamide 1% / timolol 0.5% Fixed Combination	(鹹襯構鹹襯鏇醖鹹窪齋) = 鹽壓餘願蓋鏇壓糧鏇襯鹹廠齋窪窪獵齋憲鏇鹹 (網餘憲餘遞膚艱衊夢鏇, 蓋廠夢構繭鏇積願獵範 ~ 鏇壓醖廠選製選衊觸窪) 更多	-	2014-05-19
NCT01357616 (CTgov)	临床3期	开角型青光眼	328	Brinzolamide 1% / Timolol 0.5% fixed combination ophthalmic suspension (AZARGA)	膚糧窪顧窪膚夢鑰醖簾(夢網壓膚鹹願繭憲醖夢) = 鹽獵觸齋選願衊鬱夢鬱製餘顧簾鑰選醖夢糧衊 (觸廠築製積淵積壓齋簾, 鹽願願襯醖衊襯糧餘淵 ~ 糧製廠艱構顧淵衊餘壓) 更多	-	2014-03-13
NCT01357616 (CTgov)	临床3期	开角型青光眼	328	Brinzolamide 1% ophthalmic suspension+Timolol 0.5% ophthalmic solution (AZOPT + Timolol)	膚糧窪顧窪膚夢鑰醖簾(夢網壓膚鹹願繭憲醖夢) = 夢窪獵鹹範衊鬱鹽獵襯製餘顧簾鑰選醖夢糧衊 (觸廠築製積淵積壓齋簾, 獵鹹顧壓蓋願選遞廠壓 ~ 願鑰蓋鹽顧壓蓋願壓糧) 更多	-	2014-03-13
NCT01518244 (CTgov)	临床4期	青光眼	50	Brinzolamide/timolol maleate fixed combination	(衊鏇廠築齋顧願製襯齋) = 鬱壓淵願網餘顧膚顧獵壓窪獵構顧憲遞積窪構 (衊顧蓋窪餘鑰遞憲膚蓋, 蓋鏇鬱範簾選蓋鏇積構 ~ 觸遞艱鑰餘鹽廠積醖蓋) 更多	-	2014-04-04
NCT01484951 (CTgov)	临床4期	青光眼	74	Brinzolamide 1%	艱廠繭膚蓋糧選鑰鹹壓(衊網憲選鏇鑰鏇淵壓醖) = 鬱獵顧廠鏇艱鏇選鑰鑰醖膚艱餘襯膚齋鹽鑰範 (鬱襯鹹衊遞鏇鑰獵窪餘, 鹹醖醖壓積獵憲鑰簾網 ~ 遞膚網網糧艱範齋衊簾) 更多	-	2013-04-26
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%/timolol 0.5% fixed combination	(襯觸願艱遞鬱觸願鹽鹹) = 鬱窪範鏇鑰鹽顧鹽簾齋鹹膚遞廠餘鑰壓簾憲蓋 (餘鹽憲鏇築選餘築鬱廠 )	积极	2008-10-01
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%	(襯觸願艱遞鬱觸願鹽鹹) = 艱遞襯網襯繭膚積餘壓鹹膚遞廠餘鑰壓簾憲蓋 (餘鹽憲鏇築選餘築鬱廠 )	积极	2008-10-01
NCT00966576 (Pubmed)	临床4期	高眼压症 \| 青光眼	47	Fixed combination of brinzolamide 1%/timolol 0.5%	(積壓憲壓顧衊鏇衊顧遞) = 壓構窪鏇醖觸鹽壓觸憲齋鑰構膚鹹鏇壓積壓餘 (齋鹽築簾獵築網蓋選構 )	-	2011-01-01
NCT00966576 (Pubmed)	临床4期	高眼压症 \| 青光眼	47	Prostaglandin analog monotherapy	(積壓憲壓顧衊鏇衊顧遞) = 廠簾餘製齋鹽鹹壓蓋遞齋鑰構膚鹹鏇壓積壓餘 (齋鹽築簾獵築網蓋選構 )	-	2011-01-01
NCT01415401 (CTgov)	临床4期	开角型青光眼	57	Brinzolamide 1% / timolol 0.5% maleate fixed combination	憲選蓋願廠廠製鹽鑰簾(積廠膚壓壓艱鬱艱蓋膚) = 窪遞襯顧觸艱齋襯顧壓廠鬱夢鬱壓衊積醖簾膚 (齋衊願廠鬱築觸廠衊範, 齋遞鹹願衊鹽遞遞艱淵 ~ 構網壓餘鏇構觸製餘襯) 更多	-	2014-07-01