BIO-203(BIO-203) - 药物靶点：PPARα_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

PPARα

作用机制

PPARα激动剂(过氧化物酶体增长因子活化受体α激动剂)

治疗领域

遗传病与畸形眼部疾病

在研适应症-

非在研适应症

干性年龄相关性黄斑病变

原研机构

Biophytis SA

在研机构-

非在研机构

Université Pierre et Marie Curie

Institut de la Vision

Biophytis 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 BIO-203 相关的临床结果

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100 项与 BIO-203 相关的转化医学

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100 项与 BIO-203 相关的专利（医药）

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1

项与 BIO-203 相关的文献（医药）

2023-03-10·International journal of molecular sciences

Anti-Inflammatory Effects and Photo- and Neuro-Protective Properties of BIO203, a New Amide Conjugate of Norbixin, in Development for the Treatment of Age-Related Macular Degeneration (AMD).

Article

作者: Latil, Mathilde ; Clatot, Justine ; Camelo, Serge ; Lafont, René ; Fontaine, Valérie ; Balducci, Christine ; Dinan, Laurence ; Monteiro, Elodie ; Nguyen, Vincent ; Sahel, José-Alain ; Veillet, Stanislas ; Fournié, Mylène ; Dilda, Pierre J ; Guibout, Louis ; Boumedine, Thinhinane

9'-cis-norbixin (norbixin/BIO201) protects RPE cells against phototoxicity induced by blue light and N-retinylidene-N-retinylethanolamine (A2E) in vitro and preserves visual functions in animal models of age-related macular degeneration (AMD) in vivo. The purpose of this study was to examine the mode of action and the in vitro and in vivo effects of BIO203, a novel norbixin amide conjugate. Compared to norbixin, BIO203 displays improved stability at all temperatures tested for up to 18 months. In vitro, BIO203 and norbixin share a similar mode of action involving the inhibition of PPARs, NF-κB, and AP-1 transactivations. The two compounds also reduce IL-6, IL-8, and VEGF expression induced by A2E. In vivo, ocular maximal concentration and BIO203 plasma exposure are increased compared to those of norbixin. Moreover, BIO203 administered systemically protects visual functions and retinal structure in albino rats subjected to blue-light illumination and in the retinal degeneration model of Abca4^-/- Rdh8^-/- double knock-out mice following 6 months of oral complementation. In conclusion, we report here that BIO203 and norbixin share similar modes of action and protective effects in vitro and in vivo. BIO203, with its improved pharmacokinetic and stability properties, could be developed for the treatment of retinal degenerative diseases such as AMD.

100 项与 BIO-203 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
干性年龄相关性黄斑病变	药物发现	法国	Université Pierre et Marie Curie	-
干性年龄相关性黄斑病变	药物发现	法国	Institut de la Vision	-
干性年龄相关性黄斑病变	药物发现	法国	Biophytis SA	-
干性年龄相关性黄斑病变	药物发现	法国	Université Pierre et Marie Curie	-
干性年龄相关性黄斑病变	药物发现	法国	Institut de la Vision	-
干性年龄相关性黄斑病变	药物发现	法国	Biophytis SA	-