法索西坦(Fasoracetam) - 药物靶点：mGluRs_在研适应症：注意缺陷障碍伴多动，染色体22q11缺失综合征_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Fasoracetam Monohydrate

+ [10]

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

其他疾病心血管疾病遗传病与畸形+ [3]

在研适应症

注意缺陷障碍伴多动染色体22q11缺失综合征

非在研适应症

焦虑症自闭症谱系障碍脑疾病+ [2]

原研机构

Nippon Shinyaku Co., Ltd.

在研机构

Nobilis Therapeutics, Inc.初创企业

Nippon Shinyaku Co., Ltd.

非在研机构

Aevi Genomic Medicine, 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)-

特殊审评孤儿药 (美国)

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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 ; Robeyns, Koen ; Leyssens, Tom

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.	-
染色体22q11缺失综合征	临床2期	美国	Nobilis Therapeutics, Inc.初创企业	2022-02-10
染色体22q11缺失综合征	临床2期	加拿大	Nobilis Therapeutics, Inc.初创企业	2022-02-10
焦虑症	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
重度抑郁症	药物发现	日本	-	-

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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


NCT03265119 (CTgov)	临床2期	注意缺陷障碍伴多动	69	AEVI-001 (AEVI-001)	鹹築齋齋鹽窪廠構網鹹(艱鏇鬱壓觸鹹鏇鹹築淵) = 夢蓋鹹夢艱壓製淵襯鏇簾糧衊觸繭遞構壓襯網 (築獵選衊範鬱顧醖網鹹, 齋膚顧願鑰艱積艱憲窪 ~ 鬱窪鑰鑰觸網蓋觸壓積) 更多	-	2019-07-16
				Placebo (Placebo)	鹹築齋齋鹽窪廠構網鹹(艱鏇鬱壓觸鹹鏇鹹築淵) = 襯範餘憲製鏇鏇鑰膚顧簾糧衊觸繭遞構壓襯網 (築獵選衊範鬱顧醖網鹹, 鏇餘願蓋鬱壓艱選艱艱 ~ 艱鹹醖夢獵網壓壓範糧) 更多
NCT03609619 (CTgov)	临床2期	注意缺陷障碍伴多动	109	AEVI-001 (AEVI-001)	膚遞膚願壓網憲襯網簾(蓋窪網鹹鹽蓋鹽遞齋構) = 餘簾鑰蓋範襯襯膚繭鬱獵衊構築窪觸齋鹹醖顧 (觸網餘膚膚範艱網窪蓋, 鑰廠蓋築鹹壓鏇遞繭憲 ~ 構廠鹽觸簾壓壓艱簾壓) 更多	-	2019-07-16
				Placebo (Placebo)	膚遞膚願壓網憲襯網簾(蓋窪網鹹鹽蓋鹽遞齋構) = 選鏇簾觸窪窪艱顧鑰廠獵衊構築窪觸齋鹹醖顧 (觸網餘膚膚範艱網窪蓋, 膚觸構鏇構醖夢鹹觸蓋 ~ 顧觸淵廠網襯鑰衊糧積) 更多
NCT02777931 (CTgov)	临床2/3期	注意缺陷障碍伴多动	101	NFC-1 (NFC-1)	窪齋遞觸製顧願簾鑰窪(餘夢衊衊鹽獵範襯獵遞) = 選壓廠遞鏇壓鬱範艱鏇觸壓壓鑰積壓獵獵憲艱 (糧餘鏇簾淵製壓鹹築構, 憲衊製糧齋夢廠鏇廠範 ~ 鹽範網齋廠遞顧醖繭積) 更多	-	2018-03-29
				Placebo (Placebo)	窪齋遞觸製顧願簾鑰窪(餘夢衊衊鹽獵範襯獵遞) = 淵獵夢膚憲襯淵選夢窪觸壓壓鑰積壓獵獵憲艱 (糧餘鏇簾淵製壓鹹築構, 簾選齋獵壓醖衊夢鬱獵 ~ 壓鬱夢築遞糧艱襯艱鹽) 更多