Delving into the Latest Updates on Fasoracetam with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fasoracetam Monohydrate

+ [10]

Target

mGluRs

Action

agonists

Mechanism

mGluRs agonists(Metabotropic glutamate receptor agonists)

Therapeutic Areas

Other DiseasesCardiovascular DiseasesCongenital Disorders+ [3]

Active Indication

Attention Deficit Disorder With HyperactivityDiGeorge Syndrome

Inactive Indication

Anxiety DisordersAutism Spectrum DisorderBrain Diseases+ [1]

Originator Organization

Nippon Shinyaku Co., Ltd.

Active Organization

Nobilis Therapeutics, Inc.

Nippon Shinyaku Co., Ltd.

Inactive Organization

Aevi Genomic Medicine, Inc.

License Organization-

Drug Highest PhasePhase 3

First Approval Date-

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC10H16N2O2

InChIKeyGOWRRBABHQUJMX-MRVPVSSYSA-N

CAS Registry110958-19-5

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.

Start Date17 Aug 2018

Sponsor / Collaborator

Aevi Genomic Medicine, Inc.

NCT03265119

/ CompletedPhase 2

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.

Start Date28 Aug 2017

Sponsor / Collaborator

Aevi Genomic Medicine, Inc.

100 Clinical Results associated with Fasoracetam

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100 Translational Medicine associated with Fasoracetam

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100 Patents (Medical) associated with Fasoracetam

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36

Literatures (Medical) associated with Fasoracetam

05 Jun 2024·ACS Chemical Neuroscience

Identifying Substructures That Facilitate Compounds to Penetrate the Blood–Brain Barrier via Passive Transport Using Machine Learning Explainer Models

Article

Author: Rosa, Lucca Caiaffa Santos ; Nascimento, Cayque Monteiro Castro ; Pimentel, Andre Silva ; Argolo, Caio Oliveira

The local interpretable model-agnostic explanation (LIME) method was used to interpret two machine learning models of compounds penetrating the blood-brain barrier. The classification models, Random Forest, ExtraTrees, and Deep Residual Network, were trained and validated using the blood-brain barrier penetration dataset, which shows the penetrability of compounds in the blood-brain barrier. LIME was able to create explanations for such penetrability, highlighting the most important substructures of molecules that affect drug penetration in the barrier. The simple and intuitive outputs prove the applicability of this explainable model to interpreting the permeability of compounds across the blood-brain barrier in terms of molecular features. LIME explanations were filtered with a weight equal to or greater than 0.1 to obtain only the most relevant explanations. The results showed several structures that are important for blood-brain barrier penetration. In general, it was found that some compounds with nitrogenous substructures are more likely to permeate the blood-brain barrier. The application of these structural explanations may help the pharmaceutical industry and potential drug synthesis research groups to synthesize active molecules more rationally.

01 May 2024·Pesticide Biochemistry and Physiology

Influence of Bacillus subtilis strain Z-14 on microbial ecology of cucumber rhizospheric vermiculite infested with fusarium oxysporum f. sp. cucumerinum

Article

Author: Sun, Shangyi ; Fan, Chenxi ; Gao, Tongguo ; Zhang, Dongdong ; Sun, Yanheng ; An, Xutong ; Liu, Zhaosha ; Zhang, Jizong

Fusarium oxysporum (FO) is a typical soil-borne pathogenic fungus, and the cucumber wilt disease caused by F. oxysporum f. sp. cucumerinum (FOC) seriously affects crop yield and quality. Vermiculite is increasingly being used as a culture substrate; nevertheless, studies exploring the effectiveness and mechanisms of biocontrol bacteria in this substrate are limited. In this study, vermiculite was used as a culture substrate to investigate the control effect of Bacillus subtilis strain Z-14 on cucumber wilt and the rhizospheric microecology, focusing on colonization ability, soil microbial diversity, and rhizosphere metabolome. Pot experiments showed that Z-14 effectively colonized the cucumber roots, achieving a controlled efficacy of 61.32% for wilt disease. It significantly increased the abundance of Bacillus and the expression of NRPS and PKS genes, while reducing the abundance of FO in the rhizosphere. Microbial diversity sequencing showed that Z-14 reduced the richness and diversity of the rhizosphere bacterial community, increased the richness and diversity of the fungal community, and alleviated the effect of FO on the community structure of the cucumber rhizosphere. The metabolomics analysis revealed that Z-14 affected ABC transporters, amino acid synthesis, and the biosynthesis of plant secondary metabolites. Additionally, Z-14 increased the contents of phenylacetic acid, capsidol, and quinolinic acid, all of which were related to the antagonistic activity in the rhizosphere. Z-14 exhibited a significant control effect on cucumber wilt and influenced the microflora and metabolites in rhizospheric vermiculite, providing a theoretical basis for further understanding the control effect and mechanism of cucumber wilt in different culture substrates.

01 Mar 2024·3 Biotech

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

Article

Author: 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.

100 Deals associated with Fasoracetam

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Fasoracetam	-	DB16163

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Attention Deficit Disorder With Hyperactivity	Phase 3	-	Nippon Shinyaku Co., Ltd.	-
DiGeorge Syndrome	Phase 2	United States	Nobilis Therapeutics, Inc.	10 Feb 2022
DiGeorge Syndrome	Phase 2	Canada	Nobilis Therapeutics, Inc.	10 Feb 2022
Depressive Disorder, Major	Phase 2	Japan	-	-
Anxiety Disorders	Preclinical	United States	Aevi Genomic Medicine, Inc.	28 Nov 2016
Autism Spectrum Disorder	Preclinical	United States	Aevi Genomic Medicine, Inc.	28 Nov 2016
Brain Diseases	Preclinical	United States	Aevi Genomic Medicine, Inc.	28 Nov 2016

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05290493 (CTgov)	Phase 2	22q11 Deletion Syndrome \| DiGeorge Syndrome	37	NB-001 (NB-001)	mmvtttfxkc(ewkvmfxrfb) = bhqlnzjuto xjxordgpqd (kneqduxqso, kipujfauve - igkfffiayu) View more	-	10 Feb 2025
				Placebo (Placebo)	mmvtttfxkc(ewkvmfxrfb) = taaueqnaov xjxordgpqd (kneqduxqso, cxfgrypmcg - ibdbnicylb) View more
NCT03265119 (CTgov)	Phase 2	Attention Deficit Disorder With Hyperactivity	69	AEVI-001 (AEVI-001)	tnpxztbouq(stlmeicssb) = xasrpvjadc qrsrzbcwuz (tgzexspudj, upkjpidali - tvzeuotrju) View more	-	16 Jul 2019
				Placebo (Placebo)	tnpxztbouq(stlmeicssb) = zcakzcnhma qrsrzbcwuz (tgzexspudj, cvrklpdjkv - gfnllbrsxv) View more
NCT03609619 (CTgov)	Phase 2	Attention Deficit Disorder With Hyperactivity	109	AEVI-001 (AEVI-001)	tztlwqxwkz(bxottbzulj) = zwgzmnosek xbayksrycs (abgjiyfrou, dwukzhmvfh - hhrjjsrqhi) View more	-	16 Jul 2019
				Placebo (Placebo)	tztlwqxwkz(bxottbzulj) = vlmqvzizof xbayksrycs (abgjiyfrou, jrpvgotwlc - rffepsnupr) View more
NCT02777931 (CTgov)	Phase 2/3	Attention Deficit Disorder With Hyperactivity	101	NFC-1 (NFC-1)	jaouttlbqk(ibmzpqjrgk) = yesuycwifk yydynkpnhd (qkrspiwdov, lmfkpdfjho - sftuimecyz) View more	-	29 Mar 2018
				Placebo (Placebo)	jaouttlbqk(ibmzpqjrgk) = pqiazqzlyo yydynkpnhd (qkrspiwdov, jvkqmnyzas - kqdhqhywod) View more