NCX-201(NCX-201) - 药物靶点：CA3_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [3]

靶点

CA3

作用机制

CA3抑制剂(碳酸酐酶III抑制剂)

治疗领域

眼部疾病

在研适应症-

非在研适应症

开角型青光眼

原研机构

Nicox SA

在研机构-

非在研机构

Pfizer Inc.

Nicox SA

最高研发阶段终止药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 NCX-201 相关的临床结果

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100 项与 NCX-201 相关的转化医学

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100 项与 NCX-201 相关的专利（医药）

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1

项与 NCX-201 相关的文献（医药）

2012-02-01·Journal of Enzyme Inhibition and Medicinal Chemistry2区 · 医学

A new approach to antiglaucoma drugs: carbonic anhydrase inhibitors with or without NO donating moieties. Mechanism of action and preliminary pharmacology

2区 · 医学

ArticleOA

作者: Somma, Teresa ; Supuran, Claudiu T. ; Galassi, Fernando ; Scozzafava, Gabriele ; Mincione, Francesco ; Masini, Emanuela ; Fabrizi, Francesca ; Impagnatiello, Francesco

The clinically used sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitor dorzolamide (DRZ), a new sulfonamide CA inhibitor also incorporating NO-donating moieties, NCX250, and isosorbide mononitrate (ISMN) (an NO-donating compound with no CA inhibitory properties) were investigated for their intraocular pressure (IOP) lowering effects in rabbits with carbomer-induced glaucoma. NCX250 was more effective than DRZ or ISMN on lowering IOP, increasing ocular hemodynamics, decreasing the inflammatory processes and ocular apoptosis in this animal model of glaucoma. NO participate to the regulation of IOP in glaucoma, having also antiapoptotic and anti-inflammatory effects. The ophthalmic artery, both systolic and diastolic velocities, were significantly reduced in NCX250-treated eyes in comparison to DRZ treated ones, suggesting thus a beneficial effect of NCX250 on the blood supply to the optic nerve. Combining CA inhibition with NO-donating moieties in the same compound offers an excellent approach for the management of glaucoma.

100 项与 NCX-201 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
开角型青光眼	药物发现	美国	Pfizer Inc.	-
开角型青光眼	药物发现	意大利	Nicox SA	-
开角型青光眼	药物发现	意大利	Nicox SA	-
开角型青光眼	药物发现	美国	Pfizer Inc.	-