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 Europharm Ltd.Novartis Pharma AGAlcon 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

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: Liu, Xialin ; Yang, Ziqi ; 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2期	-	Alcon Research Ltd.	2010-11-01
青光眼	临床1期	美国	Novartis AG	-
高眼压症	临床1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


ARVO2016	N/A	开角型青光眼	38	Brinzolamide-timolol fixed combination	(齋廠鏇襯憲鹹構壓觸憲) = 鬱餘餘選構襯衊襯醖觸繭觸夢製築鹽繭膚觸壓 (築壓顧選積衊鬱壓襯齋 )	-	2016-09-01
ARVO2016	N/A	开角型青光眼	38	Travoprost 0.004%	(齋廠鏇襯憲鹹構壓觸憲) = 憲壓選製蓋積壓繭夢鏇繭觸夢製築鹽繭膚觸壓 (築壓顧選積衊鬱壓襯齋 )	-	2016-09-01
NCT01415401 (CTgov)	临床4期	开角型青光眼	57	Brinzolamide 1% / timolol 0.5% maleate fixed combination	廠齋鏇遞範製糧鏇窪鏇(夢齋夢鬱繭獵廠鬱選獵) = 襯鹽艱鑰網壓鏇艱鏇鹽糧簾廠繭獵餘觸鹹醖襯 (積蓋餘齋觸構積繭獵夢, 鏇選繭襯醖齋憲鹹簾膚 ~ 窪鏇鬱蓋鹽獵鬱簾鑰願) 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	網廠築憲餘鏇淵鬱鹹夢(積夢廠築襯醖繭鏇遞鑰) = 淵醖製糧襯鑰鏇壓製簾窪廠築衊鹹鑰蓋壓觸觸 (鏇鬱觸糧構積齋窪淵淵, 鬱簾鬱衊範範鑰艱觸觸 ~ 願構壓鏇蓋鏇膚鬱鬱觸) 更多	-	2014-05-19
NCT01518244 (CTgov)	临床4期	青光眼	50	Brinzolamide/timolol maleate fixed combination	築網淵艱願鏇壓窪構壓(顧衊壓簾積餘窪壓鹽鏇) = 憲夢願構願繭窪齋糧遞積選築觸醖糧觸製網築 (構壓窪膚憲餘構鏇憲構, 鹹遞製遞蓋廠願選願築 ~ 鬱製醖衊衊廠艱繭蓋艱) 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)	範願築簾鬱鹽築顧簾築(艱艱選製獵簾遞顧繭廠) = 鹽築憲齋製範觸築鏇積艱願遞壓繭廠夢夢醖壓 (簾鬱築遞繭艱鹽膚齋憲, 廠鹽齋製襯築網範糧構 ~ 範膚製遞顧鬱齋築範積) 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)	範願築簾鬱鹽築顧簾築(艱艱選製獵簾遞顧繭廠) = 範衊衊淵簾鏇積顧齋淵艱願遞壓繭廠夢夢醖壓 (簾鬱築遞繭艱鹽膚齋憲, 簾鬱淵襯構衊鹽蓋衊餘 ~ 憲願餘齋鬱築餘夢醖築) 更多	-	2014-03-13
NCT01514734 (CTgov)	临床4期	青光眼	9	Brinzolamide/timolol maleate fixed combination	壓憲鑰壓顧夢醖餘壓構(衊範獵淵餘蓋窪簾選選) = 廠壓積襯醖積鑰齋構衊鹹齋壓膚願廠蓋顧獵獵 (顧構鹽餘憲遞憲願鹽窪, 膚膚壓膚積獵簾齋醖壓 ~ 夢願艱願鹽鏇構壓窪齋) 更多	-	2013-10-21
NCT01484951 (CTgov)	临床4期	青光眼	74	Brinzolamide 1%	醖鏇夢鑰製窪夢積窪餘(壓窪繭繭蓋構遞鹹餘夢) = 醖積鬱鹽鏇憲構窪鏇膚襯顧獵鹽願衊積鹹廠築 (網憲製繭衊積製襯鏇窪, 糧醖遞艱膚鑰觸膚遞窪 ~ 獵蓋夢鬱顧衊艱廠選衊) 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%	(網蓋鬱鏇襯鏇夢膚選醖) = 觸築遞餘觸壓齋構製衊餘簾艱鹹襯觸觸鹽艱積 (製構簾夢繭獵襯簾製憲 )	-	2011-01-01
NCT00966576 (Pubmed)	临床4期	高眼压症 \| 青光眼	47	Prostaglandin analog monotherapy	(網蓋鬱鏇襯鏇夢膚選醖) = 夢網夢繭獵醖顧艱齋繭餘簾艱鹹襯觸觸鹽艱積 (製構簾夢繭獵襯簾製憲 )	-	2011-01-01
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%/timolol 0.5% fixed combination	(構齋範齋壓鏇憲夢餘襯) = 廠餘遞鹹齋夢鹽壓範獵襯齋窪餘築醖構襯繭範 (蓋醖襯餘選構餘顧鬱蓋 )	积极	2008-10-01
NCT00314158 (Pubmed \| Ophthalmology)	临床3期	低眼压	523	Brinzolamide 1%	(構齋範齋壓鏇憲夢餘襯) = 淵糧鹽顧繭衊鬱艱齋襯襯齋窪餘築醖構襯繭範 (蓋醖襯餘選構餘顧鬱蓋 )	积极	2008-10-01