Delving into the Latest Updates on Dorzolamide Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(4S,trans)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide, 4S,6S-dorzolamide, Dorzolamide hydrochloride (JP17/USP)

+ [5]

Target

CAs

Mechanism

CAs inhibitors(Carbonic anhydrases inhibitors)

Therapeutic Areas

Eye Diseases

Active Indication

GlaucomaOcular Hypertension

Inactive Indication

Glaucoma, Open-Angle

Originator Organization

Merck & Co., Inc.

Active Organization

Santen Pharmaceutical Co., Ltd.

Inactive Organization

Merck Sharp & Dohme Corp.

Drug Highest PhaseApproved

First Approval Date

US (09 Dec 1994),

Glaucoma, Open-AngleOcular Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC10H16N2O4S3

InChIKeyIAVUPMFITXYVAF-XPUUQOCRSA-N

CAS Registry120279-96-1

View All Structures (2)

This study is a double-blind randomized clinical trial in Diabetic patients (type 2) over 18 years of age who have diabetic macular edema with involvement of the central 1 millimeter (central macular thickness is more than 300 μm) and BCVA 20/30 or less who visit the retina clinic of Labbafinejad Hospital Are studied. (In patients with bilateral macular edema, only one eye is included in the study.) Complete ocular examinations (including best corrected visual acuity - anterior segment - intraocular pressure - dilated pupil funduscopy with severity of diabetic retinopathy), optical coherence tomography (OCT), EDI-OCT( Enhanced Depth Imaging Optical Coherence Tomography ) - as well as Optical coherence tomography angiography (OCTA ) are performed for all patients at baseline. Blood tests are also taken from patients for fasting blood sugar and HbA1C. Patients are then randomly divided into two groups. The first group is treated with injections of 1.25 mg of intravitreal bevacizumab monthly for 3 months (months 0, 1 and 2) with topical drops of Timolol twice a day and Dorzolamide twice a day. For the second group (control group), 3 injections of 1.25 mg of intravitreal bevacizumab monthly with artificial tears (twice a day as a placebo) are prescribed. Patients in both groups are visited 1 month after the third basic intravitreal bevacizumab (IVB) injection and complete ophthalmology examinations are performed and central thickness of macula is recorded based on the patient's OCT as well as the need for IVB re-injection. EDI (Enhanced Depth Imaging)-OCT and OCTA are performed again for all patients.

Start Date06 Oct 2021

Sponsor / Collaborator

Shahid Beheshti University of Medical Sciences

IRCT20210519051344N1

/ CompletedPhase 2IIT

Studying the effect of combination topical therapy using three medications (Dorzolamide drops, Ketorolac drops, Prednisolone drops) in treatment of Ivrin Gass syndrome (CME) post cataract surgery

Start Date22 Jun 2021

Sponsor / Collaborator

Tabriz University of Medical Sciences

100 Clinical Results associated with Dorzolamide Hydrochloride

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100 Translational Medicine associated with Dorzolamide Hydrochloride

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100 Patents (Medical) associated with Dorzolamide Hydrochloride

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1,179

Literatures (Medical) associated with Dorzolamide Hydrochloride

14 Jan 2025·Journal of Chromatographic Science

A Simple Validated LC-UV Method for the Simultaneous Determination of Brimonidine and Brinzolamide in the Presence of Brinzolamide’s Degradation Product (Major Metabolite) in Rabbit Aqueous Humor

Article

Author: Wahab Mubarak, Marwa A ; Mohammad, M Abdul-Azim ; El-Bagary, Ramzia I ; Elkady, Ehab ; Abo-Talib, Nisreen F

AbstractA sensitive, specific, reliable and low-cost LC-UV method has been developed and validated for simultaneous quantification of brimonidine tartrate (BM) and brinzolamide (BZ) in rabbit aqueous humor (AH) in the presence of N-desethyl-brinzolamide (NDBZ); BZ is a major degradation product, and it is also considered to be its major metabolite. Dorzolamide hydrochloride (DZ) was used as an internal standard (IS). The analytes were extracted from rabbit AH samples by a simple pre-treatment utilizing ZnSO4.7H2O as a deproteinizing agent. The analytes were separated on a cyanopropyl Waters column (4.6 × 200 mm, 5 μm) with an isocratic mobile phase consisting of 25 mM ammonium acetate pH 4.5 (adjusted with 85% phosphoric acid):methanol:acetonitrile (94:4.5:1.5, v/v) at a flow rate of 1.0 mL min−1. The detection was done at 254 nm. The lower limit of quantification in rabbit AH was 100.0 ng mL−1. The method was validated according to EMA guidelines. The method was confirmed to be accurate, precise and linear over a range of 100.0–1000.0 ng mL−1 for BM and BZ. The method developed herein is simple, safe, eco-friendly, rapid and accurately applied for the quantification of BM and BZ, along with the successful separation of NDBZ, which is considered as a potential irritant degradation product of BZ.

01 Jan 2025·American Journal of Physiology-Lung Cellular and Molecular Physiology

Effects of patient pleural effusion fluids on the BBSome components expression of human benign mesothelial cells

Article

Author: Marnas, Periklis ; Rouka, Erasmia ; Kotsiou, Ourania S. ; Gourgoulianis, Konstantinos I. ; Malami, Zoi ; Sinis, Sotiris I. ; Giannou, Anastasios D. ; Sarrigeorgiou, Ioannis ; Lymberi, Peggy ; Zarogiannis, Sotirios G. ; Pitaraki, Eleanna ; Hatzoglou, Chrissi ; Jagirdar, Rajesh M. ; Papazoglou, Eleftherios D.

Studying mesothelial PC in pleural physiology and pathophysiology is at an early stage. Previously, we have highlighted the role of the PC in mesothelial cell phenotypes as well as the role of BBSome components in the context of benign and malignant mesothelial cell physiology. Here we extended our contributions by providing evidence on the BBSome changes induced in benign mesothelial cells by their exposure to different etiology PFs.

01 Jan 2025·European Journal of Pharmacology

Dorzolamide intermediates with potential anti-inflammatory activity

Article

Author: Varma, Vivek P ; Majmudar, Chinmay Y ; Hassan, Md Imtaiyaz ; White, Fletcher A ; Siddiqi, Faaiza ; Mohammad, Taj ; Faisal, Syed M ; Nair, Krishnaprasad ; Sharma, Rahul ; Atre, Rajat ; Baig, Mirza S ; Obukhov, Alexander G ; Darwhekar, Gajanan N

Dorzolamide (DZD), a Carbonic anhydrase (CA) inhibitor clinically used to lower intraocular pressure, exhibits anti-inflammatory effects owing to the drug's ability to inhibit the TIR domain-containing adaptor protein (TIRAP)-mediated signalling in macrophages. Here, we investigated whether DZD intermediates also demonstrate any anti-inflammatory property like DZD but with a reduced inhibition of CA. We found that several intermediates of DZD show increased binding to TIRAP at the common interface of kinases, such as Protein kinase C-delta (PKCδ) and Bruton's tyrosine kinase (BTK). Such binding results in a decreased activity of TIRAP, p38 Mitogen-activating protein kinases (MAPK), and p65, which are essential for major inflammatory signaling pathways. Remarkably, the DZD intermediates were more effective than DZD in decreasing the mRNA expression levels of pro-inflammatory cytokines in Lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. The DZD intermediates also exhibit a reduced binding energy to CA II and CA IV, highlighting their improved specificity as anti-inflammatory compounds with decreased unwanted biological effects. Furthermore, we validated the anti-inflammatory effect of the most efficient DZD intermediate, DRZ V, in a model of mouse sepsis. DRZ V-treated septic mice exhibited improved survival compared to DZD-treated septic mice. Our data indicate that the tested DZD intermediates are more effectual in dampening TIRAP-mediated inflammatory signaling as compared to DZD. Thus, DZD intermediates may be a promising option for developing novel anti-inflammatory therapeutics.

100 Deals associated with Dorzolamide Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D00653	Dorzolamide Hydrochloride	S01EC03	DB00869

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	JP	Santen Pharmaceutical Co., Ltd.	12 Mar 1999
Ocular Hypertension	JP	Santen Pharmaceutical Co., Ltd.	12 Mar 1999

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


DMAC (EURETINA2024) Manual	Not Applicable	Dystrophy, Macular	32	Dorzolamidezolamide 2%	yhiucbadea(eqbhxseqsk) = llaertegyj awziiyltnb (esozewtcxh )	Negative	19 Sep 2024
				Saline	yhiucbadea(eqbhxseqsk) = iyypluaqlj awziiyltnb (esozewtcxh )
NCT00716586 (CTgov)	Phase 4	Macular Edema	44	2% dorzolamide	fbsxkuikbk(houcmidhpk) = hndczjcavj djnougbsfz (qmsydgyjah, vmruycdyvw - nzwhgzwsja) View more	-	15 Oct 2021
ARVO2021	Not Applicable	Retinitis Pigmentosa	40	Topical 1.0% Dorzolamide	(yhheikkhot) = exibwgcqdv yrbulfyiht (dwkjdhsmqz )	-	01 Jun 2021
2018 ARVO Annual Meeting (ARVO2018)	Not Applicable	Bloodshot eye	30	Dorzolamide 2%	(qbpqsflynq) = zbnbpwcvlm qktmmlkbzp (svlmyovnwi )	-	01 Jul 2018
				Placebo	(qbpqsflynq) = rkmsomrcpu qktmmlkbzp (svlmyovnwi )
ARVO2014	Not Applicable	Scleral Diseases	-	dorzolamide (Rabbit Sclera)	rirkhtyxxx(onvrjmeupn) = segxmrzuou gjlntbmjxi (lrjmeoiuzf ) View more	-	01 Apr 2014
ARVO2012	Not Applicable	Ocular Hypotension	-	Agomelatine	(gdqqkmqowp) = fudybgpcwz crklunpyqa (czbmyrulcv, ±1.4)	Positive	01 Mar 2012
				Control (saline + 1% DMSO)	(gdqqkmqowp) = lrglhnmdqu crklunpyqa (czbmyrulcv )
ARVO2010	Not Applicable	-	-	Latanoprost monotherapy	(qfksjiszgn) = idlstptiin ptdbehsudc (alnawjowcc ) View more	Positive	01 Apr 2010
				Latanoprost + Dorzolamide	(qfksjiszgn) = fnsxsaxafn ptdbehsudc (alnawjowcc ) View more
ARVO2010	Not Applicable	Macular Edema	20	Topical 2% Dorzolamide	(koigshjakq) = nbltbekxbg mgbuzseoir (wdnfyrsfco )	-	01 Apr 2010
				Topical Dorzolamide (Control Group)	(koigshjakq) = becrmusswg mgbuzseoir (wdnfyrsfco )
PO086 (AAO2007)	Not Applicable	Lipid Metabolism Disorders	120	Brimonidine Purite	(wclwgmvzjx) = cydydoxwle bxxbayweck (cldmrdtabd, 21) View more	Positive	11 Nov 2007
				Dorzolamide	(wclwgmvzjx) = kxvlbsburd bxxbayweck (cldmrdtabd, 16) View more