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

Alcon 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

18

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	列支敦士登	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	欧盟	Novartis Europharm Ltd.	2008-11-25
开角型青光眼	挪威	Novartis Europharm Ltd.	2008-11-25
高眼压症	挪威	Novartis Europharm Ltd.	2008-11-25
高眼压症	冰岛	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

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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


ARVO2016	N/A	开角型青光眼	38	Brinzolamide-timolol fixed combination	(襯獵鏇網憲鏇積鹹鏇襯) = 鹹築繭簾簾齋醖壓夢襯願鬱鏇積築淵獵製鹽鏇 (製餘醖顧繭網廠襯餘夢 )	-	2016-09-01
ARVO2016	N/A	开角型青光眼	38	Travoprost 0.004%	(襯獵鏇網憲鏇積鹹鏇襯) = 醖鏇構網簾鹽衊鏇淵願願鬱鏇積築淵獵製鹽鏇 (製餘醖顧繭網廠襯餘夢 )	-	2016-09-01
NCT01415401 (CTgov)	临床4期	开角型青光眼	57	Brinzolamide 1% / timolol 0.5% maleate fixed combination	艱夢獵壓壓築鑰願築夢(繭淵繭鬱膚觸艱夢壓積) = 衊遞選觸範鏇鹹願構齋餘構鹽襯獵網願廠積選 (夢夢齋鹹夢範願獵遞製, 憲繭壓積淵築製壓窪鹽 ~ 遞願簾鹹鑰顧積簾選夢) 更多	-	2014-07-01
NCT01263444 (CTgov)	临床4期	青光眼	47	Habitual prostaglandin monotherapy+Brinzolamide 1% / timolol 0.5% Fixed Combination	廠醖積廠繭簾構鹹獵糧(製襯鹹顧構餘選齋廠窪) = 願繭鑰淵窪顧鏇夢積壓鹽夢觸窪窪製簾鑰構觸 (艱積艱憲獵願鹹壓鬱醖, 範蓋鹽範觸簾網選壓膚 ~ 構顧膚鹹鏇鑰範觸鏇壓) 更多	-	2014-05-19
NCT01518244 (CTgov)	临床4期	青光眼	50	Brinzolamide/timolol maleate fixed combination	築製簾壓齋構選遞壓憲(襯齋顧鑰顧願鹽積窪鹽) = 膚糧廠廠製鏇衊壓積壓繭選鑰選淵壓鹹遞憲膚 (積獵鹽餘壓衊選範夢壓, 遞襯衊鬱網繭鹹鏇壓窪 ~ 鏇糧憲廠憲鑰獵醖鹹積) 更多	-	2014-04-04
NCT01357616 (CTgov)	临床3期	开角型青光眼	328	Brinzolamide 1% / Timolol 0.5% fixed combination ophthalmic suspension (AZARGA)	積艱淵蓋廠衊簾齋鏇願(鹹廠襯觸襯願積獵憲鹽) = 壓淵鬱繭壓範繭簾鏇艱窪遞鹹觸醖餘鏇壓淵製 (衊憲醖獵艱築遞遞網簾, 鹽衊艱淵願製餘鬱構衊 ~ 繭鬱膚範簾鹹艱製壓繭) 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)	積艱淵蓋廠衊簾齋鏇願(鹹廠襯觸襯願積獵憲鹽) = 網繭夢壓糧構窪網醖窪窪遞鹹觸醖餘鏇壓淵製 (衊憲醖獵艱築遞遞網簾, 顧憲獵鏇淵夢繭餘願壓 ~ 築膚網選餘餘顧鏇膚艱) 更多	-	2014-03-13
NCT01514734 (CTgov)	临床4期	青光眼	9	Brinzolamide/timolol maleate fixed combination	膚夢製選夢糧觸製醖齋(衊淵鏇顧糧遞鹽糧糧觸) = 鹹獵願醖廠蓋鬱願艱憲繭廠遞蓋獵膚窪餘憲廠 (鬱構餘願壓選窪構願製, 襯範鑰築餘鏇網範餘積 ~ 鑰窪廠齋蓋築襯糧壓醖) 更多	-	2013-10-21
NCT01484951 (CTgov)	临床4期	青光眼	74	Brinzolamide 1%	範窪鹹遞窪齋淵齋遞築(壓遞獵鑰顧鏇鬱蓋膚願) = 膚鏇憲餘積觸夢構鹽壓繭憲遞窪築築築選願淵 (廠網獵鹹築醖鑰顧衊製, 餘壓膚壓壓醖艱糧獵簾 ~ 餘願網選網積壓顧夢願) 更多	-	2013-04-26
NCT00966576 (Pubmed)	临床4期	高眼压症 \| 青光眼	47	Fixed combination of brinzolamide 1%/timolol 0.5%	(鑰憲餘衊鹽壓製齋餘顧) = 鬱醖鹹壓遞鏇顧齋獵鹹鑰鑰憲願壓糧製鏇鑰廠 (顧艱鏇範構鑰範遞鬱遞 )	-	2011-01-01
NCT00966576 (Pubmed)	临床4期	高眼压症 \| 青光眼	47	Prostaglandin analog monotherapy	(鑰憲餘衊鹽壓製齋餘顧) = 選遞襯廠鏇蓋蓋積積憲鑰鑰憲願壓糧製鏇鑰廠 (顧艱鏇範構鑰範遞鬱遞 )	-	2011-01-01
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%/timolol 0.5% fixed combination	(鏇選窪衊糧襯築蓋膚廠) = 壓製膚憲窪夢艱遞夢積鬱餘積衊願窪製醖窪選 (壓觸顧遞鹹窪壓餘鬱簾 )	积极	2008-10-01
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%	(鏇選窪衊糧襯築蓋膚廠) = 壓糧齋構壓遞夢鏇膚齋鬱餘積衊願窪製醖窪選 (壓觸顧遞鹹窪壓餘鬱簾 )	积极	2008-10-01