NXT-10796(NXT-10796) - 药物靶点：EP4_在研适应症：炎症性肠病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

EP4

作用机制

EP4激动剂(前列腺素EP4受体激动剂)

治疗领域

消化系统疾病

在研适应症

炎症性肠病

非在研适应症-

原研机构

Inception Sciences, Inc.

在研机构

Inception Sciences, Inc.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 NXT-10796 相关的临床结果

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100 项与 NXT-10796 相关的转化医学

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100 项与 NXT-10796 相关的专利（医药）

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1

项与 NXT-10796 相关的文献（医药）

2023-07-15·Bioorganic & medicinal chemistry letters

Discovery of NXT-10796, an orally active, intestinally restricted EP4 agonist prodrug for the treatment of inflammatory bowel disease.

Article

作者: Fader, Lee D ; Chefson, Amandine ; Percival, M David ; Dorich, Stephane ; St-Onge, Miguel ; Burch, Jason ; Caron-Duval, Édouard ; Cox, Jennifer ; Dumais, Valerie ; Caron, Alex ; Therien, Alex G ; Wu, Joyce

A property-focused optimization strategy was employed to modify the carboxylic acid head group of a class of EP4 agonists in order to minimize its absorption upon oral administration. The resulting oxalic acid monohydrazide-derived carboxylate isostere demonstrated utility as a class of prodrug showing colon-targeted delivery of parent agonist 2, with minimal exposure observed in the plasma. Oral administration of NXT-10796 demonstrated tissue specific activation of the EP4 receptor through modulation of immune genes in the colon, without modulation of EP4 driven biomarkers in the plasma compartment. Although further in depth understanding of the conversion of NXT-10796 is required for further assessment of the developability of this series of prodrugs, using NXT-10796 as a tool molecule has allowed us to confirm that tissue-specific modulation of an EP4-modulated gene signature is possible, which allows for further evaluation of this therapeutic modality in rodent models of human disease.

100 项与 NXT-10796 相关的药物交易

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