Delving into the Latest Updates on Ripasudil Hydrochloride Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ripasudil, Ripasudil hydrochloride hydrate (JAN), Ripasudil hydrocholoride hydrate

+ [5]

Target

ROCK

Action

inhibitors

Mechanism

ROCK inhibitors(Rho-associated kinases inhibitors)

Therapeutic Areas

Eye DiseasesCongenital DisordersOther Diseases

Active Indication

GlaucomaOcular HypertensionFuchs' Endothelial Dystrophy+ [2]

Inactive Indication-

Originator Organization

Kowa Co., Ltd.

Active Organization

Kowa Research Institute, Inc.

Kowa Pharmaceuticals America, Inc.

Kowa Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (26 Sep 2014),

GlaucomaOcular Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC15H21ClFN3O3S

InChIKeyDRZAXKMMRYEBQP-IDMXKUIJSA-N

CAS Registry887375-67-9

View All Structures (2)

The purpose of this research is to investigate the effects of ripasudil administered as an ophthalmic solution in patients with FED after femtosecond laser assisted cataract surgery. The secondary aim is to identity the characteristics of patients who will benefit the most with the use of ripasudil based on the test results obtained from this study.

Start Date01 Mar 2025

Sponsor / Collaborator

Singapore Eye Research Institute

CTRI/2024/10/075399

/ Not yet recruitingNot ApplicableIIT

Role of Ripasudil in treatment of corneal edema following cataract surgery: A double blinded randomized controlled trial - NIL

Start Date01 Nov 2024

Sponsor / Collaborator

Jawaharlal Institute of Post Graduate Medical Education & Re

CTRI/2024/06/069429

/ Not yet recruitingPhase 4IIT

A prospective comparative study to evaluate the effect of different Rho kinase inhibitors as a co adjuvant for endothelial cell survival in post Penetrating Keratoplasty patients

Start Date02 Jul 2024

Sponsor / Collaborator-

100 Clinical Results associated with Ripasudil Hydrochloride Hydrate

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100 Translational Medicine associated with Ripasudil Hydrochloride Hydrate

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100 Patents (Medical) associated with Ripasudil Hydrochloride Hydrate

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245

Literatures (Medical) associated with Ripasudil Hydrochloride Hydrate

01 Jan 2025·Journal of Ophthalmology

Effect of Ripasudil on the Change Rates of the Circumpapillary Retinal Nerve Fiber Layer Thickness in Patients With Primary Open‐Angle Glaucoma

Article

Author: Kameda, Takanori ; Sakurai, Katsumasa ; Suda, Kenji ; Hasegawa, Tomoko ; Akagi, Tadamichi ; Ikeda, Hanako Ohashi ; Tsujikawa, Akitaka ; Miyake, Masahiro

Purpose: The effect of the Rho‐kinase inhibitor ripasudil on the retinal optic nerve fiber layer (RNFL) remains unclear. We aimed to determine this effect in patients with primary open‐angle glaucoma (POAG) using optical coherence tomography (OCT) measurements and linear mixed analysis.Methods: This study prospectively included outpatients from a single center with POAG without a history of vitreoretinal or glaucoma surgery from December 2014 to June 2020, in whom the circumpapillary RNFL thickness (cpRNFLT) was measured more than three times before and after ripasudil initiation, without additional medication or surgery during the period. Measurements were performed using OCT in the follow‐up mode. The cpRNFLT change rates were compared before and after treatment using linear mixed models with adjustments for intraocular pressure (IOP) changes.Results: Thirty eyes of 20 patients (12 males and eight females) were included. Upon ripasudil prescription, the average cpRNFLT was 60.2 ± 2.1 μm. The average IOP was 15.1 ± 0.5 and 13.5 ± 0.5 mmHg, respectively, before and after treatment initiation, with a difference of −1.6 ± 0.3 mmHg. Analysis of 343 cpRNFLT measurements using linear mixed models revealed that the cpRNFLT change rate was −0.91 ± 0.15 and −0.40 ± 0.14 μm/year, respectively, before and after treatment onset, with an increase of 0.51 ± 0.21 μm/year. After adjusting for IOP changes, the improvement in cpRNFLT change rate was 0.33 ± 0.23 μm/year, albeit not statistically significant.Conclusion: The cpRNFLT change rate significantly increased after ripasudil administration, whereas the contribution of the IOP decline was not significant.

01 Dec 2024·Current Eye Research

Effects of Ripasudil Hydrochloride on Epithelial Repair in a Mouse Cornea

Article

Author: Saika, Shizuya ; Sumioka, Takayoshi ; Okada, Yuka ; Takada, Yukihisa ; Yasuda, Shingo ; Tamura, Tadahiko ; Yamanaka, Osamu

PURPOSEEffect of topical administration of a Rho kinase inhibitor, ripasudil, on epithelial wound healing in a mouse cornea was investigated. Effects of treatment of cultured human corneal epithelial cell (HCEC) line and organ-cultured corneal epithelium with ripasudil on expression of p-ERK was also examined.METHODSEpithelial defects with a diameter of 2.0 mm were prepared in the central corneas of C57BL/6 mice with or without 1-week travoprost pre-treatment, to which ripasudil or PBS as a control was instilled every 6 h immediately after preparation. The mice eyes were cultured with or without travoprost for 24-hrs. The expression levels of p-ERK in epithelium of mice eyes were compared by immunostaining after further 24-hrs culture with or without ripasudil for 24-hrs. HCEC were cultured with or without ripasudil and processed for examination for proliferation activity and protein expression of p-ERK by either immunostaining or Western blotting. The cells were also treated with or without travoprost for 24-hrs, and were further cultured with or without ripasudil. Expression levels of p-ERK were examined by Western blotting.RESULTSRipasudil treatment suppressed post-debridement epithelial healing in association with reduced proliferation activity in peripheral (limbal) epithelium in cornea with or without pre-treatment with travoprost. Ripasudil treatment accelerated p-ERK expression. Ripasudil supplementation upregulated proliferation with increased p-ERK in HCEC.CONCLUSIONRipasudil treatment promotes wound healing of the mouse corneal epithelium by enhancing cell proliferation on peripheral (limbal) epithelium.

01 Dec 2024·Canadian Journal of Ophthalmology

In vivo confocal microscopy findings after Descemet stripping only with and without topical ripasudil supplementation in Fuchs endothelial dystrophy

Article

Author: Moloney, Gregory ; Devasahayam, Raj N ; Oliver, Cameron ; Burgos-Blasco, Barbara ; Northey, Luke C ; Trinh, Tanya

OBJECTIVETo report corneal epithelial and corneal endothelial cell (CEC) changes following Descemet stripping only (DSO) with and without topical ripasudil using in vivo confocal microscopy (IVCM).METHODSProspective interventional case series of patients who underwent DSO for Fuchs endothelial dystrophy with or without postoperative topical ripasudil (4%, 6 times per day). Patients underwent IVCM (ConfoScan 3; NIDEK Technologies, Padova, Italy) at baseline, monthly until corneal clearance, and then every 6 months. En face images were obtained of the epithelium, anterior and posterior corneal stroma, and endothelium of the central and superior cornea. The epithelial and endothelial layer images were evaluated qualitatively.RESULTSIVCM imaging was obtained from 34 patients, 26 (76%) of whom were supplemented with ripasudil and 8 (24%) of whom were not. Two eyes (6%) did not clear and required a keratoplasty. IVCM confirmed epithelial and endothelial cell morphology changes and reestablishment of a CEC mosaic. Hyperreflective nuclei, pleomorphism, multinucleated cells, and pseudoguttae were identified within the descemetorhexis. In patients on ripasudil, epithelial cells demonstrated transition from stratified squamous to spindle cell shape in regions of ripasudil-induced honeycomb edema. Migrating cells adopted an amoeboid shape and cytoplasm elongation when crossing to central stroma. Transient epithelial cell morphology changes and endothelial cell amoeboid shape changes appear to be uniquely associated with ripasudil. Rarely, figures were noted in both ripasudil-treated and non-ripasudil-treated corneas that resembled mitotic bodies.CONCLUSIONSCECs display a range of adaptive mechanisms during healing to re-form the endothelial mosaic following DSO. Ripasudil administration appears to induce unique epithelial and endothelial cell changes.

100 Deals associated with Ripasudil Hydrochloride Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D10463	Ripasudil Hydrochloride Hydrate	S01EX	DB13165

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	Japan	Kowa Co., Ltd.	26 Sep 2014
Ocular Hypertension	Japan	Kowa Co., Ltd.	26 Sep 2014

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Fuchs' Endothelial Dystrophy	Phase 3	Germany	Kowa Research Institute, Inc.	30 Mar 2023
Fuchs' Endothelial Dystrophy	Phase 3	United States	Kowa Research Institute, Inc.	30 Mar 2023
Fuchs' Endothelial Dystrophy	Phase 3	Denmark	Kowa Research Institute, Inc.	30 Mar 2023
Fuchs' Endothelial Dystrophy	Phase 3	Canada	Kowa Research Institute, Inc.	30 Mar 2023
Fuchs' Endothelial Dystrophy	Phase 3	Spain	Kowa Research Institute, Inc.	30 Mar 2023
Fuchs' Endothelial Dystrophy	Phase 3	United Kingdom	Kowa Research Institute, Inc.	30 Mar 2023
Corneal Edema	Phase 3	United States	Kowa Research Institute, Inc.	04 Aug 2022
Corneal Edema	Phase 3	Puerto Rico	Kowa Research Institute, Inc.	04 Aug 2022
Ophthalmologic surgical procedures	Phase 3	United States	Kowa Research Institute, Inc.	04 Aug 2022
Ophthalmologic surgical procedures	Phase 3	Puerto Rico	Kowa Research Institute, Inc.	04 Aug 2022

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04250207 (CTgov)	Phase 2	Fuchs' Endothelial Dystrophy	65	K-321 Solution (K-321 QID)	laufjqyaxv(ztzojixcbj) = akhqpnbcsg ncdsbtkgnn (oeeqtzgjsh, vrasjgeigt - iyeykacqwn) View more	-	05 Nov 2024
				Placebo Solution+K-321 Solution (K-321 BID)	laufjqyaxv(ztzojixcbj) = xympjatjsz ncdsbtkgnn (oeeqtzgjsh, jqevpujlmc - hipbdghbsx) View more
APAO2023	Not Applicable	Corneal Edema	-	Pseudophakic Corneal Edema patients prescribed with Ripasudil	ldffxbsytl(vmzugdenid) = All cases had diffused conjunctival congestion and itching in the eyes cduuivblra (hfxsricubz ) View more	-	23 Feb 2023
				Ripasudil (Reticular Corneal Edema cases)
AAO2022	Not Applicable	Fuchs' Endothelial Dystrophy	23	Topical Ripasudil	rwmuddzdcc(bvxfkzdjoy) = nxwhxhqgmf poozsxjirw (juhkfkjwqh )	-	29 Sep 2022
ARVO2022	Not Applicable	-	-	Ripasudil ophthalmic solution	(lfsxsirnkp) = oeaiiiwwts ivcmbowjad (nzzxlxwtps )	Negative	01 May 2022
				Balanced salt solution (BSS)	(lfsxsirnkp) = yurnwlfdti ivcmbowjad (nzzxlxwtps )
AAO2021	Not Applicable	Fuchs' Endothelial Dystrophy	-	DMEK+ripasudil	fsgqlcnrin(wnlmfvotnx) = csrmyfjoiv daucziadvr (wsbcdbdooo ) View more	-	13 Nov 2021
				Ripasudil	fsgqlcnrin(wnlmfvotnx) = tamuffubpa daucziadvr (wsbcdbdooo ) View more
APAO2021	Not Applicable	-	-	Ripasudil (Ctrl group)	vlymxcpveg(cbhxxgvgrn) = khzymzubyv yusrlvuaso (jnczhihvkr )	-	05 Sep 2021
				TGF-Î² group	vlymxcpveg(cbhxxgvgrn) = nzxombzivm yusrlvuaso (jnczhihvkr )
ARVO2019	Not Applicable	-	-	Placebo	(rufixsavcy) = xzgpjoucfg puloatmgvw (lacqttszoa ) View more	-	01 Jul 2019
				Ripasudil 0.04%	(rufixsavcy) = eirwqsqhln puloatmgvw (lacqttszoa ) View more
2018 ARVO Annual Meeting (ARVO2018)	Not Applicable	-	20	Placebo instillation	hrzqgdlneg(euemwgdrpz) = connysskhz vdvidelqrd (hzzrkbjvyh ) View more	Positive	01 Jul 2018
				0.04% Ripasudil instillation	hrzqgdlneg(euemwgdrpz) = glfgfxrcau vdvidelqrd (hzzrkbjvyh ) View more
2018 ARVO Annual Meeting (ARVO2018)	Not Applicable	Ocular Hypotension	9	Ripasudil 0.4% ophthalmic solution	(ohairbnizl) = mycplodhwl xzcjywdpyq (yjjpnbknll )	Negative	01 Jul 2018
ARVO2018	Not Applicable	Hyperemia	20	Brimonidine	(xweawkygvb) = lnwtfgffsi iyphmfrwwu (redomneipj ) View more	-	01 Jul 2018
				Ripasudil	(xweawkygvb) = lvafhpglph iyphmfrwwu (redomneipj ) View more