西比奈肽(Cibinetide) - 药物靶点：EPO receptor_专利_临床

概要

基本信息

药物类型

合成多肽

别名

Cibinetide (USAN/INN)、pHBSP

+ [2]

靶点

EPO receptor

作用方式

激动剂

作用机制

EPO receptor激动剂(促红细胞生成素受体激动剂)

治疗领域

免疫系统疾病神经系统疾病心血管疾病+ [4]

在研适应症-

非在研适应症

2型糖尿病糖尿病性黄斑水肿葡萄糖耐受不良+ [3]

原研机构

Araim Pharmaceuticals, Inc.

在研机构-

非在研机构

Araim Pharmaceuticals, Inc.

最高研发阶段终止临床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/序列

分子式C51H84N16O21

InChIKeyWZTIQQBMSJTRBR-WYKNNRPVSA-N

CAS号1208243-50-8

Sequence Code 148592

来源: *****

关联

15

项与西比奈肽相关的临床试验

NCT06626971

/ Terminated临床2期IIT

A Phase II Clinical Trial on the Use of ARA 290 for the Treatment of Diabetic Macular Oedema

ARA 290-DMO is a prospective, open label, interventional, single centre, investigator led, phase II trial to examine the effect of ARA 290 on diabetic macular oedema in patients with type 1 or 2 diabetes.
The aim or primary objective of the study was to determine whether ARA 290 administered at a daily dose of 4mg subcutaneously for 12 weeks to patients with diabetes mellitus (DM) and DMO would have a beneficial effect on mean change in best corrected visual acuity (BCVA) from baseline values to week 12.

开始日期2016-04-01

申办/合作机构

Belfast Health & Social Care Trust

[+1]

EUCTR2015-001940-12-GB

/ Not yet recruiting临床2期IIT

A phase II Clinical Trial on the use of ARA 290 for the treatment of diabetic macular oedema (ARA 290-DMO) - The use of ARA 290 for the treatment of DMO (ARA 290-DMO) v1

开始日期2015-11-10

申办/合作机构

Belfast Health & Social Care Trust

NCT02039687

/ Completed临床2期

A Double Blind, Placebo Controlled Phase 2 Dose Ranging Study of the Effects of ARA 290 on Corneal Nerve Fiber Density and Neuropathic Symptoms of Subjects With Sarcoidosis

The purpose of this study is to determine whether ARA 290, a new class of compound, is effective in the treatment of the neuropathic symptoms of sarcoidosis. Brief interaction of ARA 290 with the innate repair receptor results in anti-apoptotic and anti-inflammatory activities in myriad of cells, tissues and organs throughout the body to activate repair mechanisms and accelerate healing, including the nerve damage that can be associated with sarcoidosis. In this study, subjects with sarcoidosis and symptoms of small fiber neuropathy will administered ARA 290 or placebo by subcutaneous injection daily for 28 days. In addition to monitoring the safety of the treatment, the symptoms of the subjects will be assessed with several questionnaires, function tests, and measurement of nerve fibers in their cornea and skin (via a non-invasive test and a biopsy, respectively). The total participation time for each patient will be 16 weeks.

开始日期2014-01-01

申办/合作机构

Araim Pharmaceuticals, Inc.

100 项与西比奈肽相关的临床结果

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100 项与西比奈肽相关的转化医学

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100 项与西比奈肽相关的专利（医药）

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93

项与西比奈肽相关的文献（医药）

2024-12-01·Neuroscience Bulletin

Microglial EPOR Contribute to Sevoflurane-induced Developmental Fine Motor Deficits Through Synaptic Pruning in Mice

Article

作者: Shi, Xiaotong ; Kuang, Fang ; Zhao, Youyi ; Cao, Shuhui ; He, Danyi ; Liu, Bing ; Zhang, Xiao ; Gao, Zhenzhen ; Liang, Lirong ; Fan, Ze ; Ma, Sanxing ; Zhang, Hui

AbstractClinical researches including the Mayo Anesthesia Safety in Kids (MASK) study have found that children undergoing multiple anesthesia may have a higher risk of fine motor control difficulties. However, the underlying mechanisms remain elusive. Here, we report that erythropoietin receptor (EPOR), a microglial receptor associated with phagocytic activity, was significantly downregulated in the medial prefrontal cortex of young mice after multiple sevoflurane anesthesia exposure. Importantly, we found that the inhibited erythropoietin (EPO)/EPOR signaling axis led to microglial polarization, excessive excitatory synaptic pruning, and abnormal fine motor control skills in mice with multiple anesthesia exposure, and those above-mentioned situations were fully reversed by supplementing EPO-derived peptide ARA290 by intraperitoneal injection. Together, the microglial EPOR was identified as a key mediator regulating early synaptic development in this study, which impacted sevoflurane-induced fine motor dysfunction. Moreover, ARA290 might serve as a new treatment against neurotoxicity induced by general anesthesia in clinical practice by targeting the EPO/EPOR signaling pathway.

2024-09-01·International Immunopharmacology

The protective effect of erythropoietin and its novel derived peptides in peripheral nerve injury

Review

作者: Xu, Shuo ; Wang, Xiao ; Tang, Lei ; Jiang, Suli ; Li, Wei ; Zhang, Bei ; Liang, Jie ; Yang, Zijie ; Song, Meiying ; Liu, Guixian ; Liu, Xiaoli ; Du, Qiaochu ; Wang, Luoyang ; Meng, Haining ; Zhou, Mengting ; Zhang, Li ; Yang, Yanyan

Peripheral nerve injury seriously endangers human life and health, but there is no clinical drug for the treatment of peripheral nerve injury, so it is imperative to develop drugs to promote the repair of peripheral nerve injury. Erythropoietin (EPO) not only has the traditional role of promoting erythropoiesis, but also has a tissue-protective effect. Over the past few decades, researchers have confirmed that EPO has neuroprotective effects. However, side effects caused by long-term use of EPO limited its clinical application. Therefore, EPO derivatives with low side effects have been explored. Among them, ARA290 has shown significant protective effects on the nervous system, but the biggest disadvantage of ARA290, its short half-life, limits its application. To address the short half-life issue, the researchers modified ARA290 with thioether cyclization to generate a thioether cyclized helical B peptide (CHBP). ARA290 and CHBP have promising applications as peptide drugs. The neuroprotective effects they exhibit have attracted continuous exploration of their mechanisms of action. This article will review the research on the role of EPO, ARA290 and CHBP in the nervous system around this developmental process, and provide a certain reference for the subsequent research.

2024-03-01·CNS Neuroscience & Therapeutics

Erythropoietin‐derived peptide ARA290 mediates brain tissue protection through the β‐common receptor in mice with cerebral ischemic stroke

Article

作者: Wang, Rong‐Liang ; Huang, Yu‐You ; Hu, Yue ; Fan, Jun‐Fen ; Li, Si‐Jie ; Yang, Zhen‐Hong ; Zhao, Hai‐Ping ; Wang, Yi‐Lin ; Tao, Zhen ; Luo, Yu‐Min ; Zheng, Yang‐Min ; Han, Zi‐Ping ; Yan, Feng

AbstractAimTo explore the neuroprotective effects of ARA290 and the role of β‐common receptor (βCR) in a mouse model of middle cerebral artery occlusion (MCAO).MethodsThis study included male C57BL/6J mice that underwent MCAO and reperfusion. The neuroprotective effect of ARA290 on MCAO‐induced brain injury was investigated using neurological function tests (Longa and modified neurological severity score). Cerebral infarction was examined by 2, 3, 5‐triphenyl tetrazolium chloride staining, neuronal apoptosis was assessed by immunofluorescence staining, blood parameters were measured using a flow cytometry‐based automated hematology analyzer, liquid chromatography with tandem mass spectrometry was used to identify the serum metabolomics signature, inflammatory cytokines and liver index were detected by commercially available kits, and the protein levels of the erythropoietin (EPO) receptor and βCR were measured by western blot.ResultsARA290 exerted a qualitatively similar neuroprotective effect after MCAO as EPO. ARA290 significantly reduced neuronal apoptosis and the level of inflammatory cytokines in the brain tissue. However, ARA290's neuroprotective effect was significantly suppressed following the injection of siRNA against βCR.ConclusionARA290 provided a neuroprotective effect via βCR in cerebral ischemic mice without causing erythropoiesis. This study provides novel insights into the role of ARA290 in ischemic stroke intervention.

100 项与西比奈肽相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11218	-	-	DB13006

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
糖尿病性黄斑水肿	临床2期	英国	Araim Pharmaceuticals, Inc.	2016-04-01
神经结节病	临床2期	美国	Araim Pharmaceuticals, Inc.	2014-01-01
神经结节病	临床2期	荷兰	Araim Pharmaceuticals, Inc.	2014-01-01
疼痛	临床2期	美国	Araim Pharmaceuticals, Inc.	2014-01-01
疼痛	临床2期	荷兰	Araim Pharmaceuticals, Inc.	2014-01-01
2型糖尿病	临床2期	瑞典	Araim Pharmaceuticals, Inc.	2013-10-01
葡萄糖耐受不良	临床2期	瑞典	Araim Pharmaceuticals, Inc.	2013-10-01
糖尿病前期	临床2期	瑞典	Araim Pharmaceuticals, Inc.	2013-10-01

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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


NCT02039687 (CTgov)	临床2期	疼痛 \| 神经结节病	64	ARA 290 (1 mg Per Day ARA 290)	窪顧範窪艱築淵簾網鑰(蓋網選鹹選襯鬱願憲淵) = 餘齋積構淵齋鹹壓憲鏇鏇襯顧鹽廠壓範構積襯 (糧願壓鏇顧選鹽淵築鬱, 選淵遞壓積簾簾鬱繭選 ~ 艱齋選醖齋範網窪淵鹹) 更多	-	2017-01-18
				ARA 290 (4 mg Per Day ARA 290)	窪顧範窪艱築淵簾網鑰(蓋網選鹹選襯鬱願憲淵) = 窪繭鏇構鏇壓簾餘簾窪鏇襯顧鹽廠壓範構積襯 (糧願壓鏇顧選鹽淵築鬱, 廠鏇壓淵艱鬱製襯獵願 ~ 鹽範築鑰廠築醖襯顧壓) 更多
PS 045 (EASD2013)	N/A	2型糖尿病	-	ARA290	製餘夢繭鏇糧網繭築顧(憲遞艱醖蓋構淵築糧糧) = 選選鏇艱鑰網壓廠夢齋蓋遞蓋鑰窪餘憲選淵鏇 (網憲夢壓壓艱構網艱構 ) 更多	积极	2013-09-25
				Placebo	製餘夢繭鏇糧網繭築顧(憲遞艱醖蓋構淵築糧糧) = 鹽製餘願餘廠選範鏇願蓋遞蓋鑰窪餘憲選淵鏇 (網憲夢壓壓艱構網艱構 ) 更多