E-2027(E-2027) - 药物靶点：PDE9A_在研适应症：帕金森病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Irsenontrine、Irsenontrine maleate

+ [5]

靶点

PDE9A

作用机制

PDE9A抑制剂(磷酸二酯酶9A抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

最高研发阶段临床3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C26H26N4O7

InChIKeyAFKSGMDXSLTKSU-DASCVMRKSA-N

CAS号1630083-70-3

关联

6

项与 E-2027 相关的临床试验

NCT04764669 / Completed临床2期

An Open-Label Study To Evaluate the Pharmacodynamic Effects, Efficacy, Safety, and Tolerability of E2027 in Subjects With Dementia With Lewy Bodies or Parkinson's Disease Dementia With or Without Amyloid Copathology

The purpose of study is to demonstrate the pharmacodynamic (PD) effects of E2027 on cerebrospinal fluid (CSF) cyclic guanosine monophosphate (cGMP) in participants with DLB and PDD with and without amyloid copathology after 9 weeks of treatment.

开始日期2021-02-25

申办/合作机构

Eisai, Inc.

NCT04023877 / Completed临床1期

An Open-Label, Single-Dose Study to Determine the Metabolism and Elimination of [14C]E2027 in Healthy Male Subjects

The primary objective of the study is to achieve mass balance recovery of [14C]-radiolabel in urine and feces and to identify and quantify the main elimination pathways of E2027.

开始日期2019-07-18

申办/合作机构

Eisai, Inc.

NCT03467152 / Completed临床2期

A Placebo-Controlled, Double-Blind, Parallel-Group, Randomized, Study To Evaluate the Efficacy, Safety and Tolerability of E2027 in Subjects With Dementia With Lewy Bodies

This study will be conducted to compare Irsenontrine to placebo on the cognitive endpoint of Montreal Cognitive Assessment (MoCA) and the global clinical endpoint of Clinician's Interview Based Impression of Change Plus (CIBIC-Plus) Caregiver Input in participants with dementia with Lewy bodies after 12 weeks of treatment.

开始日期2018-05-04

申办/合作机构

Eisai, Inc.

100 项与 E-2027 相关的临床结果

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100 项与 E-2027 相关的转化医学

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100 项与 E-2027 相关的专利（医药）

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3

项与 E-2027 相关的文献（医药）

2023-10-01·Current Neurology and Neuroscience Reports

Lewy Body Dementia: An Overview of Promising Therapeutics

Review

作者: Sha, Sharon J ; Skylar-Scott, Irina A

PURPOSE OF REVIEWLewy body dementia (LBD) encompasses dementia with Lewy bodies (DLB) and Parkinson's disease dementia (PDD). This article will emphasize potential disease-modifying therapies as well as investigative symptomatic treatments for non-motor symptoms including cognitive impairment and psychosis that can present a tremendous burden to patients with LBD and their caregivers.RECENT FINDINGSWe review 11 prospective disease-modifying therapies (DMT) including four with phase 2 data (neflamapimod, nilotinib, bosutinib, and E2027); four with some limited data in symptomatic populations including phase 1, open-label, registry, or cohort data (vodabatinib, ambroxol, clenbuterol, and terazosin); and three with phase 1 data in healthy populations (Anle138b, fosgonimeton, and CT1812). We also appraise four symptomatic therapies for cognitive impairment, but due to safety and efficacy concerns, only NYX-458 remains under active investigation. Of symptomatic therapies for psychosis recently investigated, pimavanserin shows promise in LBD, but studies of nelotanserin have been suspended. Although the discovery of novel symptomatic and disease-modifying therapeutics remains a significant challenge, recently published and upcoming trials signify promising strides toward that aim.

2019-04-01·Drugs & Aging3区 · 医学

Pharmacological Management of Dementia with Lewy Bodies

3区 · 医学

Review

作者: Hershey, Linda A ; Coleman-Jackson, Rhonda

Dementia with Lewy bodies (DLB) is a complex disease that involves a variety of cognitive, behavioral and neurological symptoms, including progressive memory loss, visual hallucinations, parkinsonism, cognitive fluctuations and rapid eye movement sleep behavior disorder (RBD). These symptoms may appear in varying combinations and levels of severity in each patient who is seen in the clinic, making diagnosis and treatment a challenge. DLB is the third most common of all the neurodegenerative diseases behind both Alzheimer's disease and Parkinson's disease (PD). The median age of onset for DLB (76.3 years) is younger than that seen in PD dementia (81.4 years). New pathological studies have shown that most DLB patients have variable amounts of Alzheimer's changes in their brains, explaining the wide variability in this disease's clinical presentation and clinical course. This review discusses the three cholinesterase inhibitors that have been shown to be effective in managing the cognitive and behavioral symptoms of DLB: rivastigmine, galantamine and donepezil. Memantine is able to improve clinical global impression of change in those with mild to moderate DLB. Levodopa can treat the parkinsonism of some DLB patients, but the dose is often limited due to the fact that it can cause agitation or worsening of visual hallucinations. A recent phase 2 clinical trial showed the benefit of zonisamide when it is added as an adjunct to levodopa for treating DLB parkinsonism. While atypical antipsychotic drugs may not always be helpful as monotherapy in managing the agitation associated with DLB, low doses of valproic acid can be effective when added as an adjunct to drugs like quetiapine. Pimavanserin may prove to be a useful treatment for psychosis in DLB patients, but like other antipsychotic drugs that are used in dementia patients, there is a small increased risk of mortality. RBD, which is a common core clinical feature of DLB, can be managed with either melatonin or clonazepam. Two agents targeting alpha-synuclein (NPT200-11 and ambroxol) currently hold promise as disease-modifying therapies for DLB, but they are yet to be tested in clinical trials. An agent (E2027) that offers hope of neuroprotection by increasing central cyclic guanosine monophosphate (cGMP) levels is currently being examined in clinical trials in DLB patients.

Annals of Medicine & Surgery

Insights into the management of Lewy body dementia: a scoping review

Review

作者: Shah, Rajat ; Kausar, Huma ; Rauniyar, Vivek K ; Khan, Sadab ; Gautam, Sakshyam ; Luitel, Anish ; Khan, Sajjad Ahmed ; Parajuli, Surya Bahadur ; Khan, Moien A B

Lewy body dementia (LBD) is situated at the convergence of neurodegenerative disorders, posing an intricate and diverse clinical dilemma. The accumulation of abnormal protein in the brain, namely, the Lewy body causes disturbances in typical neural functioning, leading to a range of cognitive, motor, and mental symptoms that have a substantial influence on the overall well-being and quality of life of affected individuals. There is no definitive cure for the disease; however, several nonpharmacological and pharmacological modalities have been tried with questionable efficacies. The aim of this study is to figure out the role of different interventional strategies in the disease. Donepezil, rivastigmine, memantine, and galantamine were the commonly used drugs for LBD. Together with that, levodopa, antipsychotics, armodafinil, piracetam, and traditional medications like yokukansan were also used, when indicated. Talking about nonpharmacological measures, exercise, physical therapy, multicomponent therapy, occupational therapy, psychobehavioral modification, transcranial stimulation, and deep brain stimulation have been used with variable efficacies. Talking about recent advances in the treatment of LBD, various disease-modifying therapies like ambroxol, neflamapimod, irsenontrine, nilotinib, bosutinib, vodobatinib, clenbuterol, terazosin, elayta, fosgonimeton, and anle138b are emerging out. However, there drugs are still in the different phases of clinical trials and are not commonly used in clinical practice. With the different pharmacological and nonpharmacological modalities we have for treatment of LBD, all of them offer symptomatic relief only. Being a degenerative disease, definite cure of the disease can only be possible with regenerative measures.

100 项与 E-2027 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
帕金森病	临床3期	-	Eisai Co., Ltd.	-
帕金森病所致痴呆	临床2期	美国	Eisai, Inc.	2021-02-25
帕金森病所致痴呆	临床2期	加拿大	Eisai, Inc.	2021-02-25
路易体病	临床2期	意大利	Eisai Co., Ltd.	2018-04-19

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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


NCT04764669 (CTgov)	临床2期	帕金森病所致痴呆 \| 路易体病 \| 帕金森病	34	E2027 (DLB Without Amyloid Copathology)	窪糧獵憲餘顧壓選獵築(簾製鑰齋構憲鹽鹽築繭) = 選範糧糧鬱製餘顧夢鏇築積醖餘築顧鹽觸顧繭 (鏇顧鹽遞齋鹹蓋獵窪蓋, 製鬱醖繭醖顧糧醖憲淵 ~ 襯願獵築艱衊鑰窪製鹹) 更多	-	2022-09-26
NCT04764669 (CTgov)	临床2期	帕金森病所致痴呆 \| 路易体病 \| 帕金森病	34	E2027 (DLB With Amyloid Copathology)	窪糧獵憲餘顧壓選獵築(簾製鑰齋構憲鹽鹽築繭) = 繭艱蓋壓憲簾鏇窪糧構築積醖餘築顧鹽觸顧繭 (鏇顧鹽遞齋鹹蓋獵窪蓋, 鏇製衊鏇夢鑰製顧憲窪 ~ 窪鑰衊鹹衊觸壓簾餘顧) 更多	-	2022-09-26
E2027 (AAIC2018)	N/A	路易体病	-	E2027 100 mg	選齋鏇艱製憲願廠觸窪(壓壓簾獵衊選願憲積願) = 築餘鹹顧襯糧製繭鏇艱衊鬱鹹簾鑰觸觸選襯製 (築製艱鬱醖繭淵顧鹽簾 )	-	2018-07-01