Delving into the Latest Updates on Brinzolamide/Timolol Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Azarga, Brinzolamide and Timolol Maleate, Brinzolamide/timolol

+ [5]

Target

CA2 x β-adrenoceptors

Mechanism

CA2 inhibitors(Carbonic anhydrase II inhibitors), β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas

Eye Diseases

Active Indication

GlaucomaGlaucoma, Open-AngleOcular Hypertension

Inactive Indication-

Originator Organization

Alcon AG

Active Organization

Novartis Pharma AGNovartis Europharm Ltd.Alcon Laboratories UK Ltd.

Inactive Organization

Alcon Research Ltd.

Drug Highest PhaseApproved

First Approval Date

EU (25 Nov 2008),

Glaucoma, Open-AngleOcular Hypertension

Regulation-

Login to view timeline

Structure

Molecular FormulaC25H45N7O8S4

InChIKeyYPIMJBXEIGRISS-LARVRRBISA-N

CAS Registry1110563-69-3

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.

Start Date01 Jan 2014

Sponsor / Collaborator

Afyon Kocatepe University

NCT01514734 / TerminatedPhase 4

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.

Start Date01 Mar 2012

Sponsor / Collaborator

Alcon Research Ltd.

100 Clinical Results associated with Brinzolamide/Timolol Maleate

Login to view more data

100 Translational Medicine associated with Brinzolamide/Timolol Maleate

Login to view more data

100 Patents (Medical) associated with Brinzolamide/Timolol Maleate

Login to view more data

10

Literatures (Medical) associated with Brinzolamide/Timolol Maleate

01 Dec 2023·American Journal of Ophthalmology Case Reports

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

Author: 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.

17 Oct 2023·Biomolecules

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

Article

Author: 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.

01 Jan 2022·Vestnik oftal'mologii

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

Article

Author: 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 Deals associated with Brinzolamide/Timolol Maleate

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	S01ED51	-

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Glaucoma	JP	Novartis Pharma AG	20 Sep 2013
Glaucoma, Open-Angle	LI	Novartis Europharm Ltd.	25 Nov 2008
Glaucoma, Open-Angle	IS	Novartis Europharm Ltd.	25 Nov 2008
Glaucoma, Open-Angle	EU	Novartis Europharm Ltd.	25 Nov 2008
Glaucoma, Open-Angle	NO	Novartis Europharm Ltd.	25 Nov 2008
Ocular Hypertension	NO	Novartis Europharm Ltd.	25 Nov 2008
Ocular Hypertension	IS	Novartis Europharm Ltd.	25 Nov 2008
Ocular Hypertension	EU	Novartis Europharm Ltd.	25 Nov 2008
Ocular Hypertension	LI	Novartis Europharm Ltd.	25 Nov 2008

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Glaucoma, Open-Angle	Phase 3	-	Alcon Research Ltd.	01 Nov 2010

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2016	Not Applicable	Glaucoma, Open-Angle	38	Brinzolamide-timolol fixed combination	(fvxrrvotya) = bzpjzptqtd kymvewatig (gcdqawxzbu )	-	01 Sep 2016
ARVO2016	Not Applicable	Glaucoma, Open-Angle	38	Travoprost 0.004%	(fvxrrvotya) = vlastpeaec kymvewatig (gcdqawxzbu )	-	01 Sep 2016
NCT01415401 (CTgov)	Phase 4	Glaucoma, Open-Angle	57	Brinzolamide 1% / timolol 0.5% maleate fixed combination	esilljbzxg(zmqwnzbmrs) = wbwhwszyfz snhhescnim (lricslbjya, cobpithnos - lhytqubeqp) View more	-	01 Jul 2014
NCT01263444 (CTgov)	Phase 4	Glaucoma	47	Habitual prostaglandin monotherapy+Brinzolamide 1% / timolol 0.5% Fixed Combination	quscpxcxxy(rbnsowjjwx) = shdxwkoecj bxoknznxrs (nwllcapvlb, galthbkgnz - ryvlqlexjf) View more	-	19 May 2014
NCT01518244 (CTgov)	Phase 4	Glaucoma	50	Brinzolamide/timolol maleate fixed combination	ddyhqmffnf(dcjmsyrezi) = vclkitqfxj oekuraazua (wjaquwqrop, axrsutedia - tnnzknlyyo) View more	-	04 Apr 2014
NCT01357616 (CTgov)	Phase 3	Glaucoma, Open-Angle	328	Brinzolamide 1% / Timolol 0.5% fixed combination ophthalmic suspension (AZARGA)	oxvgezdfbk(lhhoaeusmp) = jnloshgyhf eoaysapqli (tnrlalsoks, lxewjkbtoq - axzsyfzupw) View more	-	13 Mar 2014
NCT01357616 (CTgov)	Phase 3	Glaucoma, Open-Angle	328	Brinzolamide 1% ophthalmic suspension+Timolol 0.5% ophthalmic solution (AZOPT + Timolol)	oxvgezdfbk(lhhoaeusmp) = etqowkaeuf eoaysapqli (tnrlalsoks, hikbnlhybm - jsbxytdahs) View more	-	13 Mar 2014
NCT01514734 (CTgov)	Phase 4	Glaucoma	9	Brinzolamide/timolol maleate fixed combination	rbltcmcuph(jvdvkyonlo) = dsrkxsnbcl tohqyragwa (lxsgtugyff, rnoedmulex - iuikweuhsq) View more	-	21 Oct 2013
NCT01484951 (CTgov)	Phase 4	Glaucoma	74	Brinzolamide 1%	qyakqapswy(bbbwhernvb) = khrijtwkwr zplgeyzwlz (gwjzncnsot, ognlsrhbng - lrfusvogow) View more	-	26 Apr 2013
NCT00966576 (Pubmed)	Phase 4	Ocular Hypertension \| Glaucoma	47	Fixed combination of brinzolamide 1%/timolol 0.5%	(goczfpwbny) = mvclqflnip ktpdpyojsd (mzdiehmicv )	-	01 Jan 2011
NCT00966576 (Pubmed)	Phase 4	Ocular Hypertension \| Glaucoma	47	Prostaglandin analog monotherapy	(goczfpwbny) = sbutudtdug ktpdpyojsd (mzdiehmicv )	-	01 Jan 2011
NCT00314158 (Pubmed \| Ophthalmology)	Phase 3	Ocular Hypotension	523	Brinzolamide 1%/timolol 0.5% fixed combination	(jtzwtluigf) = vcntgdxgav meejypwsve (ysfaxnkldh )	Positive	01 Oct 2008
NCT00314158 (Pubmed \| Ophthalmology)	Phase 3	Ocular Hypotension	523	Brinzolamide 1%	(jtzwtluigf) = ywfqjgdapr meejypwsve (ysfaxnkldh )	Positive	01 Oct 2008