更新于：2024-11-21

Icoduline Hydrochloride

艾考度林

更新于：2024-11-21

概要

概要

基本信息

药物类型

小分子化药

别名

Icoduline、Icodulinum

+ [1]

靶点

5-LOX x COX

作用机制

5-LOX抑制剂(5-脂氧合酶抑制剂)、COX抑制剂(环氧化酶抑制剂)

治疗领域

眼部疾病皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

眼部疾病皮肤疾病

原研机构

Chauvin Pharmaceuticals Ltd.

在研机构-

非在研机构

Chauvin Pharmaceuticals Ltd.Groupe Chauvin

最高研发阶段终止临床3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C10H11ClN2OS

InChIKeyOAQDENGCTUPZEL-UHFFFAOYSA-N

CAS号110952-54-0

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关联

100 项与艾考度林相关的临床结果

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100 项与艾考度林相关的转化医学

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100 项与艾考度林相关的专利（医药）

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项与艾考度林相关的文献（医药）

1995-08-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Electrochemical oxidation of CBA-113 A, a new anti-inflammatory drug: applicability to liquid chromatography-electrochemical detection

3区 · 医学

Article

作者: Pierre Leroy ; Marie-Dominique Blanchin ; Olga Baudrit ; Alain Nicolas ; Huguette Fabre

The electrochemical properties of a new non-steroidal anti-inflammatory drug (2-hydroxy-4-methylphenyl-2-aminothiazole hydrochloride; CBS-113 A) have been studied using voltammetry in direct current and cyclic modes at glassy carbon disk electrodes. The results show an oxidative process with a diffusion-controlled and a reversible mechanism; these data agree with those obtained in a reversed-phase high-performance liquid chromatography (HPLC) system coupled either with amperometric (single glassy carbon electrode) or coulometric detection (two porous graphite electrodes in series) set at potentials of +0.65 V (vs. Ag/AgCl) and +0.4 V (vs. Pd/H2), respectively. Similar electrochemical properties were found for 2-hydroxyphenyl-2-amino-5'-methylthiazole hydrochloride (RD-1546) which is a potential internal standard. An HPLC system coupled with a UV detector (lambda = 272 nm) and an amperometric detector (+0.65 V) showed a gain in sensitivity of about 10 using electrochemical detection (ED) for the determination of CBS-113 A in human plasma. Linearity range, precision and accuracy were calculated and showed the potential application of HPLC-ED to pharmacokinetic studies of CBS-113 A in plasma.

1991-11-01·Eye3区 · 医学

A randomised double blind trial comparing the treatment of episcleritis with topical 2-(2-hydroxy-4-methylphenyl) aminothiazole hydrochloride 0.1% (CBS 113A) and placebo

3区 · 医学

Article

作者: P G Watson ; S Ramirez-Florez ; C S C Liu

A randomised double blind trial of 2-(2-Hydroxy-4-methylphenyl) Aminothiazole Hydrochloride 0.1% (CBS 113A) versus placebo was carried out in 43 eyes with episcleritis. Our results show that CBS 113A is effective in reducing the signs of conjunctival and episcleral inflammation in mild episcleritis within the first week of administration of the drug (Day 3: Total Score p = 0.0013, Conjunctival Injection p = 0.017, Episcleral Injection p = 0.0018 and Day 7: Total Score p = 0.01, Conjunctival Injection p = 0.014, Episcleral Injection p = 0.027). CBS 113A was not effective against severe episcleritis. No significant side effects were found apart from a stinging sensation. There was no effect on intraocular pressure. The potential use of this new drug is discussed.

1990-01-01·Journal of Ocular Pharmacology and Therapeutics

PAF-Induced Conjunctivitis in the Rabbit is Mediated by Peptido-Leukotrienes

Article

作者: Bonne, C. ; Meynier, F. ; Muller, A.

Platelet activating factor (PAF) released by many cell types is involved in several steps of inflammatory reactions in various organs including the eye. It has been reported that some effects of PAF could be mediated by arachidonic acid metabolites generated after PAF-receptor interaction. In the study we investigated the protective effect of CBS-113A, a dual inhibitor of 5-lipoxygenase/cyclooxygenase in PAF-induced conjunctivitis in the rabbit. Moreover, the characterization of the icosanoid potentially mediating the PAF activity has been performed by using specific pharmacological agents. Subconjunctival injection of PAF (10-1000 ng) provoked Evans' blue extravasation measured in tissues within 30 min. Simultaneous injection of a PAF antagonist (BN 50730) inhibited the dye leakage, showing specific PAF receptor-mediated vascular reaction. CBS-113A applied in eye drops also inhibited Evans' blue extravasation. By contrast, indometacin administered either topically or by subconjunctival injection was not effective in reducing the effect of PAF. These results suggesting the involvement of a 5-lipoxygenase metabolite were confirmed by the effectiveness of local injection of SKF 104353, a specific leukotriene D4 antagonist. The present study shows that PAF-induced plasma leakage in conjunctivitis is mediated by peptido-leukotrienes.

100 项与艾考度林相关的药物交易

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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
眼部疾病	临床3期	-	Chauvin Pharmaceuticals Ltd.	-
眼部疾病	临床3期	法国	Groupe Chauvin	-
皮肤疾病	临床3期	美国	-	-
皮肤疾病	临床3期	加拿大	-	-