法索西坦(Fasoracetam) - 药物靶点：mGluRs_在研适应症：注意缺陷障碍伴多动_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [6]

靶点

mGluRs

作用机制

mGluRs激动剂(代谢型谷氨酸受体激动剂)

治疗领域

其他疾病

在研适应症

注意缺陷障碍伴多动

非在研适应症

焦虑自闭症谱系障碍自闭症+ [4]

原研机构

Nippon Shinyaku Co., Ltd.

在研机构

Aevi Genomic Medicine, Inc.

Nippon Shinyaku Co., Ltd.

非在研机构

Avalo Therapeutics, Inc.

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-

结构

分子式C10H16N2O2

InChIKeyGOWRRBABHQUJMX-MRVPVSSYSA-N

CAS号110958-19-5

关联

7

项与法索西坦相关的临床试验

NCT05290493 / Completed临床2期

A Randomized, Placebo-Controlled Crossover Trial to Assess the Safety and Efficacy of NB-001 in Children and Adolescents With 22q11 Deletion Syndrome

This is a Phase 2, randomized, placebo-controlled crossover trial to assess the safety and efficacy of NB-001 in children and adolescents with 22q11DS that manifest commonly associated neuropsychiatric conditions.

开始日期2022-02-10

申办/合作机构

Nobilis Therapeutics, Inc.初创企业

NCT03609619 / Completed临床2期

A Multicenter, 2-Part, 6-Week, Double-blind, Randomized, Placebo-controlled, Parallel-design Study to Assess the Efficacy and Safety of AEVI-001 in Children and Adolescents (Ages 6-17 Years) With Attention Deficit Hyperactivity Disorder and With or Without Copy Number Variants in Specific Genes Implicated in Glutamatergic Signaling and Neuronal Connectivity

This is PART B of a 2-part, 6-week, double-blind, dose-optimization, parallel-group study in children and adolescents (ages 6-17 years) with ADHD with and without CNVs in specific genes implicated in glutamatergic signaling and neuronal activity. PART B will assess subjects who do not have CNVs in any of the specific gene mutation(s) implicated in glutamatergic signaling and neuronal connectivity.

开始日期2018-08-17

申办/合作机构

Aevi Genomic Medicine, Inc.

NCT03265119 / Completed临床2期

A Multicenter, 2-Part, 6-Week, Double-blind, Randomized, Placebo-controlled, Parallel-design Study to Assess the Efficacy and Safety of AEVI-001 in Children and Adolescents (Ages 6-17 Years) With Attention Deficit Hyperactivity Disorder and With or Without Copy Number Variants in Specific Genes Implicated in Glutamatergic Signaling and Neuronal Connectivity

This is PART A of a 2-part, 6-week, double-blind, dose-optimization, parallel-group study in children and adolescents (ages 6-17 years) with ADHD with and without CNVs in specific genes implicated in glutamatergic signaling and neuronal activity. Parts A will include subjects determined to have a specific gene mutations implicated in glutamatergic signaling and neuronal connectivity.

开始日期2017-08-28

申办/合作机构

Aevi Genomic Medicine, Inc.

100 项与法索西坦相关的临床结果

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100 项与法索西坦相关的转化医学

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100 项与法索西坦相关的专利（医药）

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13

项与法索西坦相关的文献（医药）

2024-03-01·3 Biotech

Molecular authentication, metabolite profiling and in silico–in vitro cytotoxicity screening of endophytic Penicillium ramusculum from Withania somnifera for breast cancer therapeutics

Article

作者: Haldar, Niladri ; Rajeshkumar, K C ; Shaikh, Aazam ; Jisha, M S ; Varghese, Sherin ; Gajbhiye, Virendra

In the present study, we isolated a potent endophytic fungus from the roots of Withania somnifera. The endophytic fungal strain was authenticated as Penicillium ramusculum SVWS3 based on morphological and molecular sequencing using four gene data and phylogenetic analyses. In vitro cytotoxicity studies unveiled the remarkable cytotoxic potential of the crude extract derived from P. ramusculum, exhibiting dose-dependent effects on MDA-MB-468 and MCF-7 cells. At a concentration of 100 µg/mL, the crude extract resulted in cell viability of 29.78% for MDA-MB-468 cells and 14.61% for MCF-7 cells. The IC₅₀ values were calculated as 62.83 ± 0.93 µg/mL and 17.23 ± 1.43 µg/mL, respectively for MDA-MB-468 and MCF-7 cells. Caspase activation assay established the underlying mechanism of the crude extract depicting the activation of caspases 3 and 7, indicating the induction of apoptosis in MCF-7 cells. Chemotaxonomic profiling elucidated the ability of P. ramusculum to synthesize a diverse array of bioactive compounds, including Fasoracetam, Tryprostatin B, Odorinol, Thyronine, Brevianamide F, Proglumide, Perlolyrine, Tyrphostin B48, Baptifoline, etc. Molecular docking studies inferred that Baptifoline, Brevianamide F, Odorinol, Perlolyrine, Thyronine, Tryphostin B48, and Tryprostatin B were the lead compounds that could effectively interact with the five selected target receptors of breast cancer, further surpassing the positive controls analyzed. Pharmacokinetic profiling revealed that Baptifoline, Odorinol, and Thyronine depicted an excellent therapeutic profile of druggability. These findings collectively substantiate the anticancer activity of bioactive metabolites synthesized by P. ramusculum SVWS3. Hence, the endophytic P. ramusculum SVWS3 can be an authentic source for developing novel chemotherapeutic drug formulations.Supplementary InformationThe online version contains supplementary material available at 10.1007/s13205-023-03906-3.

2019-07-03·Expert Review of Neurotherapeutics3区 · 医学

Beyond stimulants: a systematic review of randomised controlled trials assessing novel compounds for ADHD

3区 · 医学

Review

作者: Cortese, Samuele ; Nageye, Fatuma

Introduction: Despite stimulants being highly efficacious in short-term randomized controlled trials (RCTs), not all patients respond or can successfully tolerate them. A number of novel non-stimulant options are currently in the pipeline for the treatment of attention-deficit/hyperactivity disorder (ADHD). Areas covered: The authors conducted a systematic review of RCTs registered in ClinicalTrials.gov in the past 5 years (January 2014 and February 2019), supplemented by searches in PubMed, Web of Science, and drug manufacturer websites to find recent RCTs on novel non-stimulant ADHD medications. Expert opinion: The authors found 28 pertinent RCTs of compounds acting on a variety of biological targets, including Dasotraline, Viloxazine (SPN-812), Centanafadine SR (CTN SR), OPC-64005, Fasoracetam (NFC-1, AEVI-001), Metadoxine (MDX), Vortioxetine, Tipepidine Hibenzate, Oxytocin, Sativex (delta-9-tetrahydrocannabinol (THC) plus cannabidiol), Mazindol, and Molindone hydrochloride (SPN-810). Given the high effect size found in RCTs of stimulants in terms of efficacy on ADHD core symptoms, it is unlikely that these novel agents will show better efficacy than stimulants, at the group level. However, they may offer comparable or better tolerability. Additionally, agents acting on etiopathophysiological targets disrupted in specific subgroups of patients with ADHD will move forward the pharmacotherapy of ADHD from a 'one size fits all' to a 'precision medicine' approach.

2017-05-01·Journal of Pharmaceutical Sciences3区 · 医学

A Study of Fasoracetam’s Solid State Forms: A Potential Anti-Alzheimer Pharmaceutical

3区 · 医学

Article

作者: Harmsen, Bram ; Wouters, Johan ; Leyssens, Tom ; Robeyns, Koen

Different solid state forms of the research chemical fasoracetam, which counters the effects of Alzheimer's disease, have been subjected to a thermal and structural analysis. Single crystals were obtained from solution evaporation and from the melt. Single-crystal X-ray analyses of the crystals show the existence of 2 hydrated and 1 non-hydrated crystalline form of fasoracetam. Under ambient conditions, the hydrate form I is found to be the most stable form, showing a melting point of 57C. This low melting point, combined with possible water losses could cause problems when formulating the hydrated form and impact the storage conditions of the compound.

100 项与法索西坦相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	法索西坦	-	DB16163

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
注意缺陷障碍伴多动	临床3期	-	Nippon Shinyaku Co., Ltd.	-
注意缺陷障碍伴多动	临床3期	-	Aevi Genomic Medicine, Inc.	-
重度抑郁症	临床2期	日本	-	-
焦虑	临床前	美国	Aevi Genomic Medicine, Inc.	2016-11-28
自闭症谱系障碍	临床前	美国	Aevi Genomic Medicine, Inc.	2016-11-28
脑疾病	临床前	美国	Aevi Genomic Medicine, Inc.	2016-11-28
迪格奥尔格综合征	临床前	美国	Aevi Genomic Medicine, Inc.	2016-11-28
自闭症	临床前	美国	Avalo Therapeutics, Inc.	-
认知障碍	临床前	日本	-	-

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临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03609619 (CTgov)	临床2期	注意缺陷障碍伴多动	109	AEVI-001 (AEVI-001)	淵鹽襯鹹鹽繭顧鬱糧夢(鏇壓願壓夢餘鬱網淵窪) = 廠積鹽願鹽獵積襯襯餘鹹膚齋簾夢簾衊餘壓鏇 (鑰鹹蓋蓋獵選廠簾鹹積, 遞鹹糧鹽鑰願觸廠鏇餘 ~ 醖獵製鑰範淵簾鏇簾鹹) 更多	-	2019-07-16
				placebo (Placebo)	淵鹽襯鹹鹽繭顧鬱糧夢(鏇壓願壓夢餘鬱網淵窪) = 鏇艱蓋膚獵鏇觸壓壓築鹹膚齋簾夢簾衊餘壓鏇 (鑰鹹蓋蓋獵選廠簾鹹積, 淵鹹艱積糧鏇廠顧構壓 ~ 鹽遞窪遞顧蓋夢鹽衊糧) 更多
NCT03265119 (CTgov)	临床2期	注意缺陷障碍伴多动	69	AEVI-001 (AEVI-001)	築積積繭憲壓襯獵艱簾(醖壓醖鬱鏇遞膚範遞窪) = 選艱鏇選鬱鏇窪繭鑰遞膚鏇憲餘淵網膚築餘選 (繭餘餘醖鏇襯顧壓淵鹹, 鏇選壓窪膚窪蓋範鏇衊 ~ 鏇積衊齋衊蓋壓窪餘夢) 更多	-	2019-07-16
				placebo (Placebo)	築積積繭憲壓襯獵艱簾(醖壓醖鬱鏇遞膚範遞窪) = 鹽齋繭衊襯艱廠鬱鏇鑰膚鏇憲餘淵網膚築餘選 (繭餘餘醖鏇襯顧壓淵鹹, 範繭觸鑰壓顧選廠繭鏇 ~ 憲範糧範網窪構艱簾觸) 更多
NCT02777931 (CTgov)	临床2/3期	注意缺陷障碍伴多动	101	NFC-1 (NFC-1)	範淵簾簾觸鹹觸窪鹹築(選築蓋憲壓鬱獵餘襯積) = 範製範範遞鹹艱鑰選鹽膚鬱網醖窪廠蓋窪選鹽 (餘憲憲壓顧顧製選鬱醖, 網襯簾膚窪憲蓋餘構夢 ~ 餘選選獵繭鏇艱淵鏇簾) 更多	-	2018-03-29
				Placebo (Placebo)	範淵簾簾觸鹹觸窪鹹築(選築蓋憲壓鬱獵餘襯積) = 淵餘齋觸鏇膚衊鹽膚壓膚鬱網醖窪廠蓋窪選鹽 (餘憲憲壓顧顧製選鬱醖, 齋膚餘衊襯遞範繭壓選 ~ 憲範鬱衊獵醖網鬱積糧) 更多