Y-39983(Y-39983) - 药物靶点：ROCK1_在研适应症：青光眼_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

ROCK1

作用机制

ROCK1抑制剂(Rho相关蛋白激酶-1抑制剂)

治疗领域

眼部疾病

在研适应症

青光眼

非在研适应症

开角型青光眼

原研机构

Mitsubishi Tanabe Pharma Corp.

在研机构

Mitsubishi Tanabe Pharma Corp.

非在研机构

Novartis Pharma AGSenju Pharmaceutical Co., Ltd.

Novartis Pharmaceuticals Corp.

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C16H17ClN4O

InChIKeyIILQESWQPZIAGP-HNCPQSOCSA-N

CAS号471843-75-1

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关联

4

项与 Y-39983 相关的临床试验

JPRN-UMIN000018866 / Completed

Phase IIb study of SNJ-1656; A dose-response study in patients with primary open angle glaucoma or ocular hypertension - A dose-response study of SNJ-1656 in patients with primary open angle glaucoma or ocular hypertension

开始日期2009-07-01

申办/合作机构

Senju Pharmaceutical Co., Ltd.

NCT00846989 / Completed临床1/2期

A 4-week Multi-center, Single-masked, Randomized, Latanoprost-controlled, Parallel Group Study to Assess the Efficacy, Tolerability and Safety of RKI983 (0.05% and 0.10%) Ophthalmic Solution Given Twice a Day Versus Once Daily Latanoprost 0.005%, in Patients With Primary Open Angle Glaucoma or Ocular Hypertension.

This purpose of this study is to access the efficacy, tolerability and safety of RKI983 (0.05% and 0.10%) ophthalmic solution bid versus once daily latanoprost 0.005%, in patients with POAG or ocular hypertension.

开始日期2009-01-01

申办/合作机构

Novartis Pharmaceuticals Corp.

JPRN-UMIN000009648 / Completed

Phase IIa study of SNJ-1656; An exploration study in patients with primary open angle glaucoma or ocular hypertension - An exploration study of SNJ-1656 in patients with primary open angle glaucoma or ocular hypertension

开始日期2008-05-08

申办/合作机构

Senju Pharmaceutical Co., Ltd.

100 项与 Y-39983 相关的临床结果

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100 项与 Y-39983 相关的转化医学

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100 项与 Y-39983 相关的专利（医药）

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23

项与 Y-39983 相关的文献（医药）

2024-03-01·Regenerative Therapy

Mass production of iPSC-derived platelets toward the clinical application

Review

作者: Eto, Koji ; Kayama, Akihiro

The ex vivo production of platelets from induced pluripotent cells (iPSCs) may offer a safer and sustainable alternative for transfusions and drug delivery systems (DDS). However, the mass production of the clinically required number of iPSC-derived platelets (iPSC-PLTs) is challenging. Here, we introduce recent technologies for mass production and the first-in-human clinical trial using ex vivo iPSC-PLTs. To this end, we established immortalized megakaryocyte progenitor cell lines (imMKCLs) as an expandable master cell bank (MCB) through the overexpression of c-MYC, BMI1 and BCL-XL, which modulated megakaryopoiesis and thrombopoiesis. We also optimized a culture cocktail for maturation of the imMKCLs by mixing an aryl hydrocarbon receptor (AhR) antagonist, SR1/GNF-316; a Rho-associated protein kinase (ROCK) inhibitor, Y-27632/Y-39983; and a small-molecule compound replacing recombinant thrombopoietin (TPO), TA-316. Finally, we discovered the importance of turbulence on the manufacturing of intact iPSC-PLTs, allowing us to develop a turbulence-based bioreactor, VerMES. Combination of the MCB and VerMES enabled us to produce more than 100 billion iPSC-PLTs, leading to the first-in-human clinical trial. Despite these advancements, many challenges remain before expanding the clinical implementation of this strategy.

2023-11-01·Journal of Ocular Pharmacology and Therapeutics

ROCK Inhibitors as an Alternative Therapy for Corneal Grafting: A Systematic Review

Review

作者: Das, Parikshit ; Kumar, Mohit ; Niri, Pakter ; Saha, Achintya ; Kamboj, Dev Vrat ; Polopalli, Subramanyam ; Chattopadhyay, Pronobesh

Currently, corneal blindness is affecting >10 million individuals worldwide, and there is a significant unmet medical need because only 1.5% of transplantation needs are met globally due to a lack of high-quality grafts. In light of this global health disaster, researchers are developing corneal substitutes that can resemble the human cornea in vivo and replace human donor tissue. Thus, this review examines ROCK (Rho-associated coiled-coil containing protein kinases) inhibitors as a potential corneal wound-healing (CWH) therapy by reviewing the existing clinical and nonclinical findings. The systematic review was done from PubMed, Scopus, Web of Science, and Google Scholar for CWH, corneal injury, corneal endothelial wound healing, ROCK inhibitors, Fasudil, Netarsudil, Ripasudil, Y-27632, clinical trial, clinical study, case series, case reports, preclinical study, in vivo, and in vitro studies. After removing duplicates, all downloaded articles were examined. The literature search included the data till January 2023. This review summarized the results of ROCK inhibitors in clinical and preclinical trials. In a clinical trial, various ROCK inhibitors improved CWH in individuals with open-angle glaucoma, cataract, iris cyst, ocular hypertension, and other ocular diseases. ROCK inhibitors also improved ocular wound healing by increasing cell adhesion, migration, and proliferation in vitro and in vivo. ROCK inhibitors have antifibrotic, antiangiogenic, anti-inflammatory, and antiapoptotic characteristics in CWH, according to the existing research. ROCK inhibitors were effective topical treatments for corneal infections. Ripasudil, Y-27632, H-1152, Y-39983, and AMA0526 are a few new ROCK inhibitors that may help CWH and replace human donor tissue.

2023-07-01·Experimental Eye Research

Identifying new drugs and targets to treat rapidly elevated intraocular pressure for angle closure and secondary glaucomas to curb visual impairment and prevent blindness

Review

作者: Sharif, Najam A

A multitude of pharmacological compounds have been shown to lower and control intraocular pressure (IOP) in numerous species of animals and human subjects after topical ocular dosing or via other routes of administration. Most researchers have been interested in finding drug candidates that exhibit a relatively long duration of action from a chronic therapeutic use perspective, for example to treat ocular hypertension (OHT), primary open-angle glaucoma and even normotensive glaucoma. However, it is equally important to seek and characterize treatment modalities which offer a rapid onset of action to help provide fast relief from quickly rising IOP that occurs in certain eye diseases. These include acute angle-closure glaucoma, primary angle-closure glaucoma, uveitic and inflammatory glaucoma, medication-induced OHT, and other secondary glaucomas induced by eye injury or infection which can cause partial or complete loss of eyesight. Such fast-acting agents can delay or prevent the need for ocular surgery which is often used to lower the dangerously raised IOP. This research survey was therefore directed at identifying agents from the literature that demonstrated ocular hypotensive activity, normalizing and unifying the data, determining their onset of action and rank ordering them on the basis of rapidity of action starting within 30-60 min and lasting up to at least 3-4 h post topical ocular dosing in different animal species. This research revealed a few health authority-approved drugs and some investigational compounds that appear to meet the necessary criteria of fast onset of action coupled with significant efficacy to reduce elevated IOP (by ≥ 20%, preferably by >30%). However, translation of the novel animal-based findings to the human conditions remains to be demonstrated but represent viable targets, especially EP₂-receptor agonists (e.g. omidenepag isopropyl; AL-6598; butaprost), mixed activity serotonin/dopamine receptor agonists (e.g. cabergoline), rho kinase inhibitors (e.g. AMA0076, Y39983), CACNA2D1-gene product inhibitors (e.g. pregabalin), melatonin receptor agonists, and certain K⁺-channel openers (e.g. nicorandil, pinacidil). Other drug candidates and targets were also identified and will be discussed.

100 项与 Y-39983 相关的药物交易

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研发状态

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
青光眼	临床2期	-	Mitsubishi Tanabe Pharma Corp.	-
开角型青光眼	药物发现	美国	Novartis Pharmaceuticals Corp.	2009-01-01

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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


ARVO2013	N/A	-	5	AMA0076	(鬱積餘窪鑰鏇蓋醖憲膚) = Hyperemia was observed with all concentrations of Y-39983 whereas only mild hyperemia was induced after administration of AMA0076 0.4% (highest concentration used) 膚艱築獵艱醖壓網範積 (衊鹹襯網製網製獵構衊 )	-	2013-06-01
				Y-39983