Delving into the Latest Updates on Edonerpic with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Edonerpic maleate

Target

σ1 receptor

Mechanism

σ1 receptor agonists(Sigma opioid receptor agonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication

StrokeAlzheimer DiseaseMild cognitive disorder

Inactive Indication

Liver Injury

Originator Organization

Toyama Chemical Co., Ltd.

Active Organization

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

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC20H25NO6S

InChIKeyRLUCYBFCLXANSO-BTJKTKAUSA-N

CAS Registry519187-97-4

View All Structures (2)

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

Start Date24 Dec 2019

Sponsor / Collaborator

FUJIFILM Toyama Chemical Co., Ltd.

JPRN-jRCT2080224564 / CompletedPhase 2

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

Start Date05 Jun 2019

Sponsor / Collaborator

FUJIFILM Toyama Chemical Co., Ltd.

100 Clinical Results associated with Edonerpic

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100 Translational Medicine associated with Edonerpic

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100 Patents (Medical) associated with Edonerpic

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10

Literatures (Medical) associated with Edonerpic

01 Nov 2022·Ageing Research Reviews

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

Review

Author: 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.

01 Jan 2022·Folia Pharmacologica Japonica

CRMP2 binding compound accelerates functional recovery from central nervous system damage

Article

Author: 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.

04 May 2021·Expert Opinion on Therapeutic TargetsQ2 · MEDICINE

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

Q2 · MEDICINE

Review

Author: 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 Deals associated with Edonerpic

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05938

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Stroke	Phase 2	JP	FUJIFILM Pharmaceuticals USA, Inc.	30 Jan 2022
Mild cognitive disorder	Phase 2	CZ	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	IE	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	GB	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	NL	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	DE	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	ES	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Mild cognitive disorder	Phase 2	HU	FUJIFILM Toyama Chemical Co., Ltd.	24 Dec 2019
Alzheimer Disease	Phase 2	US	FUJIFILM Toyama Chemical Co., Ltd.	01 Apr 2008
Alzheimer Disease	Phase 2	CA	FUJIFILM Toyama Chemical Co., Ltd.	01 Apr 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02079909 (CTgov)	Phase 2	Alzheimer Disease	482	T-817MA-H (T-817MA-H)	ekworcwokl(ihcnckyeal) = qpalzqxghr qxovpzwzqj (rkmrmaoibw, perftlzqsx - grgjtsjfpa) View more	-	09 Aug 2018
NCT02079909 (CTgov)	Phase 2	Alzheimer Disease	482	T-817MA-L (T-817MA-L)	ekworcwokl(ihcnckyeal) = gpdluwqzkm qxovpzwzqj (rkmrmaoibw, cfrbdawqli - dkqqfyllms) View more	-	09 Aug 2018
AAIC2015	Not Applicable	-	-	T-817MA	yhnikoyjsq(gonzfmtucn) = fwpnbnxqxv bwsffxdbjm (agwckgmnun )	-	01 Jul 2015