Edonerpic(Edonerpic) - 药物靶点：σ1 receptor_在研适应症：脑卒中，阿尔茨海默症，轻度认知障碍_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Edonerpic maleate

靶点

σ1 receptor

作用机制

σ1 receptor激动剂(σ-阿片受体激动剂)

治疗领域

神经系统疾病心血管疾病其他疾病

在研适应症

脑卒中阿尔茨海默症轻度认知障碍

非在研适应症

肝损伤

原研机构

Toyama Chemical Co., Ltd.

在研机构

FUJIFILM Toyama Chemical Co., Ltd.FUJIFILM Pharmaceuticals USA, Inc.

非在研机构-

最高研发阶段临床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

分子式C20H25NO6S

InChIKeyRLUCYBFCLXANSO-BTJKTKAUSA-N

CAS号519187-97-4

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关联

12

项与 Edonerpic 相关的临床试验

JPRN-jRCTs031220728 / RecruitingN/AIIT

Exploratory study to compare AMPA receptors changes during rehabilitation with or without T-817MA measured with [11C]K-2 PET combined with Japic-104711 data - Additional T-817 AMPA-PET

开始日期2023-04-21

申办/合作机构-

NCT04191486 / Completed临床2期

A Phase 2 Multi-center, Randomized, Double-blind, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy and Safety of T-817MA in Patients With Mild Cognitive Impairment Due to Alzheimer's Disease or Mild Alzheimer's Disease

Primary objective is to evaluate the neuroprotective effect of T-817MA on Tau protein phosphorylated at threonine 181 (p-tau 181) in cerebrospinal fluid (CSF) compared with placebo in patients with a diagnosis of MCI due to AD or mild AD.
Secondary objectives are:
To evaluate in patients on T-817MA and placebo:
cognitive function measured by the Clinical Dementia Rating Scale Sum of Boxes (CDR-sb) and working memory and attention domain as measured by the Cognitive Functional Composite (CFC).
AD-related biomarkers in CSF and plasma
imaging analysis using volumetric magnetic resonance imaging (vMRI)
alpha/theta ratio of the electroencephalogram (EEG)
To evaluate the safety of T-817MA by clinical laboratory tests and adverse events (AEs).
To evaluate the pharmacokinetics of T-817MA

开始日期2019-12-24

申办/合作机构

FUJIFILM Toyama Chemical Co., Ltd.

JPRN-jRCT2080224564 / Completed临床2期

A Phase 2, Multi-center, Randomized, Double-blind, Placebo-controlled Study of T-817MA in Post-stroke Patients Undergoing Rehabilitation for Upper Limb Hemiplegia

开始日期2019-06-05

申办/合作机构

FUJIFILM Toyama Chemical Co., Ltd.

100 项与 Edonerpic 相关的临床结果

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100 项与 Edonerpic 相关的转化医学

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100 项与 Edonerpic 相关的专利（医药）

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10

项与 Edonerpic 相关的文献（医药）

2022-11-01·Ageing Research Reviews

A systematic review on drugs for synaptic plasticity in the treatment of dementia

Review

作者: Piscopo, P ; Lo Giudice, M ; Rivabene, R ; Corbo, M ; Vanacore, N ; Crestini, A ; Carbone, E ; Lacorte, E ; Ancidoni, A

The aim of the present systematic review (SR) was to provide an overview of all published and unpublished clinical trials investigating the safety and efficacy of disease-modifying drugs targeting synaptic plasticity in dementia. Searches on CT.gov and EuCT identified 27 trials (4 phase-1, 1 phase-1/2, 18 phase-2, 1 phase-2/3, 1 phase-3, 1 phase-4, and 1 not reported). Twenty of them completed, and seven are currently active or enrolling. The structured bibliographic searches yielded 3585 records. A total of 12 studies were selected on Levetiracetam, Masitinib, Saracatinib, BI 40930, Bryostatin 1, PF-04447943 and Edonerpic drugs. We used RoB tool for quality analysis of randomized studies. Efficacy was assessed as a primary outcome in all studies except one and the main scale used was ADAS-Cog (7 studies), MMSE and CDR (4 studies). Safety and tolerability were reported in eleven studies. The incidence of SAEs was similar between treatment and placebo. At the moment, only one molecule reached phase-3. This could suggest that research on these drugs is still preliminary. Of all, three studies reported promising results on Levetiracetam, Bryostatin 1 and Masitinib.

2022-01-01·Folia Pharmacologica Japonica

CRMP2 binding compound accelerates functional recovery from central nervous system damage

Article

作者: Jitsuki, Susumu

Brain injury causes temporary or permanent impairment of brain function due to an accident or circulation disorders. Even after rehabilitation training, there are often persistent functional impairments. Recent advances in our understanding of the repair mechanisms of neural circuits after brain injury have led to the possibility that these mechanisms may offer potential therapeutic targets for drugs that promote functional recovery after brain injury. Neuroplasticity is believed to be important for the recovery process after brain injury in the brain regions associated with injured region for compensation. The effectiveness of drugs for restoring brain function after stroke investigated in a variety of animal models and clinical trials has been focused on drugs that act on the monoamine system to modulate neuroplasticity, as well as other targets such as NMDA receptors and CCR5. Recently, we focused on novel small compound, edonerpic maleate, as a drug which facilitates experience-dependent synaptic delivery of AMPA receptor. We found that edonerpic maleate binds to Collapsin-response mediator protein 2, a downstream molecule of Semaphorin and enhance synaptic plasticity by facilitating synaptic delivery of AMPA receptors, thereby promoting functional recovery in a rehabilitation-dependent manner after brain injury in rodents and non-human primates. Further investigations is needed to seek more appropriate drug targets from both preclinical animal studies and clinical trials, and to translate preclinical results into successful clinical trials.

2021-05-04·Expert Opinion on Therapeutic Targets2区 · 医学

The emerging role of the sigma-1 receptor in autophagy: hand-in-hand targets for the treatment of Alzheimer’s

2区 · 医学

Review

作者: Prasanth, Mani Iyer ; Brimson, James Michael ; Tencomnao, Tewin ; Malar, Dicson Sheeja

INTRODUCTIONAutophagy is a cellular catabolic mechanism that helps clear damaged cellular components and is essential for normal cellular and tissue function. The sigma-1 receptor (σ-1R) is a chaperone protein involved in signal transduction, neurite outgrowth, and plasticity, improving memory, and neuroprotection. Recent evidence shows that σ-1R can promote autophagy. Autophagy activation by the σ-1Rs along with other neuroprotective effects makes it an interesting target for the treatment of Alzheimer's disease. AF710B, T-817 MA, and ANAVEX2-73 are some of the σ-1R agonists which have shown promising results and have entered clinical trials. These molecules have also been found to induce autophagy and show cytoprotective effects in cellular models.AREAS COVEREDThis review provides insight into the current understanding of σ-1R functions related to autophagy and their role in alleviating AD.EXPERT OPINIONWe propose a mechanism through which the activation of σ-1R and autophagy could alter amyloid precursor protein processing to inhibit amyloid-β production by reconstituting cholesterol and gangliosides in the lipid raft to offer neuroprotection against AD. Future AD treatment could involve the combined targeting of the σ-1R and autophagy activation. We suggest that future studies investigate the link between autophagy the σ-1R and AD.

100 项与 Edonerpic 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05938

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
脑卒中	临床2期	日本	FUJIFILM Pharmaceuticals USA, Inc.	2022-01-30
轻度认知障碍	临床2期	捷克	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	爱尔兰	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	英国	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	荷兰	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	德国	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	西班牙	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
轻度认知障碍	临床2期	匈牙利	FUJIFILM Toyama Chemical Co., Ltd.	2019-12-24
阿尔茨海默症	临床2期	美国	FUJIFILM Toyama Chemical Co., Ltd.	2008-04-01
阿尔茨海默症	临床2期	加拿大	FUJIFILM Toyama Chemical Co., Ltd.	2008-04-01

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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


NCT02079909 (CTgov)	临床2期	阿尔茨海默症	482	T-817MA-H (T-817MA-H)	壓窪齋網襯範壓鹽齋夢(艱範構繭願醖構願夢艱) = 鹹製蓋鑰選襯範範鏇餘範廠顧製遞餘網顧繭鏇 (觸淵艱積簾膚網鬱築淵, 獵壓構簾築遞製願構顧 ~ 選築衊鏇積廠鹽鹹範繭) 更多	-	2018-08-09
NCT02079909 (CTgov)	临床2期	阿尔茨海默症	482	T-817MA-L (T-817MA-L)	壓窪齋網襯範壓鹽齋夢(艱範構繭願醖構願夢艱) = 衊範鑰夢憲淵鏇蓋構衊範廠顧製遞餘網顧繭鏇 (觸淵艱積簾膚網鬱築淵, 鑰網鹹鬱醖餘遞製構選 ~ 襯憲餘鏇觸憲鏇壓獵餘) 更多	-	2018-08-09
AAIC2015	N/A	-	-	T-817MA	願廠窪選鹹鑰網鹽築淵(構壓蓋壓觸廠願願鏇製) = 窪鏇鏇衊簾淵網艱艱製醖艱願鹽顧鬱顧願襯繭 (蓋窪範範選淵範憲鑰憲 )	-	2015-07-01