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'''Fasoracetam''' ('''NS-105''', '''5-oxo-<small>D</small>-prolinepiperidinamide monohydrate''')<ref>[http://fdasis.nlm.nih.gov/srs/ProxyServlet?mergeData=true&objectHandle=DBMaint&APPLICATION_NAME=fdasrs&actionHandle=default&nextPage=jsp/srs/ResultScreen.jsp&TXTSUPERLISTID=42O8UF5CJB&QV1=42O8UF5CJB FDA/NIH Substance registration system]. Page accessed March 21, 2016</ref> is a [[research chemical]] of the [[racetam]] family.<ref>{{cite web |url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=198695|title=5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary|accessdate=21 July 2013}}</ref> It is a [[nootropic]], and has been in a clinical trial for [[attention deficit hyperactivity disorder]].<ref>{{cite web |url=http://adisinsight.springer.com/drugs/800003134|title=Drug Profile Fasoracetam }}</ref>
'''Fasoracetam''' ('''NS-105''', '''5-oxo-<small>D</small>-prolinepiperidinamide monohydrate'''<ref>[http://fdasis.nlm.nih.gov/srs/ProxyServlet?mergeData=true&objectHandle=DBMaint&APPLICATION_NAME=fdasrs&actionHandle=default&nextPage=jsp/srs/ResultScreen.jsp&TXTSUPERLISTID=42O8UF5CJB&QV1=42O8UF5CJB FDA/NIH Substance registration system]. Page accessed March 21, 2016</ref>, '''AEVI-001''', '''LAM 105''', '''MDGN-001''', '''NFC 1'''<ref>{{cite web |url=http://adisinsight.springer.com/drugs/800003134|title=Drug Profile Fasoracetam }}</ref>) is a [[research chemical]] of the [[racetam]] family.<ref>{{cite web |url=http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=198695|title=5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary|accessdate=21 July 2013}}</ref> It is a [[nootropic]], and has been in a clinical trial for [[attention deficit hyperactivity disorder]].<ref>{{cite web |url=http://adisinsight.springer.com/drugs/800003134|title=Drug Profile Fasoracetam }}</ref>


In [[in vitro]] studies on mouse neurons, fasoracetam modulated [[mGluR]] II/III activity.<ref>{{cite journal |title=A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture. | pmid=9272724 | volume=356 | journal=Naunyn Schmiedebergs Arch Pharmacol | pages=189–96 | last1 = Oka | first1 = M | last2 = Itoh | first2 = Y | last3 = Tatsumi | first3 = S | last4 = Ma | first4 = FH | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1007/pl00005040}}.</ref> In studies in rats, it blocked memory disruptions caused by [[baclofen]], a [[GABAB receptor|GABA<sub>B</sub>]] agonist<ref name=study1>{{cite journal |title=Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. | pmid=10494996 | volume=64 | journal=Pharmacol Biochem Behav | pages=41–52 | last1 = Ogasawara | first1 = T | last2 = Itoh | first2 = Y | last3 = Tamura | first3 = M | last4 = Mushiroi | first4 = T | last5 = Ukai | first5 = Y | last6 = Kise | first6 = M | last7 = Kimura | first7 = K | doi=10.1016/s0091-3057(99)00108-2}}</ref> and [[upregulate]]d production of GABA<sub>B</sub> receptors after repeat dosing.<ref>{{cite journal |title=Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment. | pmid=9424016 | volume=338 | journal=Eur J Pharmacol | pages=225–32 | last1 = Shimidzu | first1 = T | last2 = Itoh | first2 = Y | last3 = Oka | first3 = M | last4 = Ishima | first4 = T | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1016/s0014-2999(97)81925-5}}</ref>
In [[in vitro]] studies on mouse neurons, fasoracetam modulated [[mGluR]] II/III activity.<ref>{{cite journal |title=A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture. | pmid=9272724 | volume=356 | journal=Naunyn Schmiedebergs Arch Pharmacol | pages=189–96 | last1 = Oka | first1 = M | last2 = Itoh | first2 = Y | last3 = Tatsumi | first3 = S | last4 = Ma | first4 = FH | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1007/pl00005040}}.</ref> In studies in rats, it blocked memory disruptions caused by [[baclofen]], a [[GABAB receptor|GABA<sub>B</sub>]] agonist<ref name=study1>{{cite journal |title=Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. | pmid=10494996 | volume=64 | journal=Pharmacol Biochem Behav | pages=41–52 | last1 = Ogasawara | first1 = T | last2 = Itoh | first2 = Y | last3 = Tamura | first3 = M | last4 = Mushiroi | first4 = T | last5 = Ukai | first5 = Y | last6 = Kise | first6 = M | last7 = Kimura | first7 = K | doi=10.1016/s0091-3057(99)00108-2}}</ref> and [[upregulate]]d production of GABA<sub>B</sub> receptors after repeat dosing.<ref>{{cite journal |title=Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment. | pmid=9424016 | volume=338 | journal=Eur J Pharmacol | pages=225–32 | last1 = Shimidzu | first1 = T | last2 = Itoh | first2 = Y | last3 = Oka | first3 = M | last4 = Ishima | first4 = T | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1016/s0014-2999(97)81925-5}}</ref>
==Clinical Trials==
Fasoracetam was originally developed for use in the treatment of dementia, but was abandoned in Phase 3 clinical trials.<ref>{{cite journal |title=ADHD & Pharmacotherapy: Past, Present and Future: A Review of the Changing Landscape of Drug Therapy for Attention Deficit Hyperactivity Disorder. | volume=49(5) | journal=Ther Innov Regul Sci | pages=632-642 | last1 = Connolly| first1 = J | last2 = Glessner | first2 = J | last3 = Kao | first3 = C | last4 = Elia | first4 = J | last5 = Hakonarson | first5 = H | doi=10.1177/2168479015599811}}</ref>
A Phase one safety study found a positive effect with 30 adolescents with ADHD and genetic disorders impacting [[metabotropic glutamate receptor]]s (mGluRs).<ref>{{cite web | title=Pediatric ADHD Study Shows Rare Genetic Mutation Underlies Condition in Some Patients. | url=http://scipol.duke.edu/content/pediatric-adhd-study-shows-rare-genetic-mutation-underlies-condition-some-patients | publisher=Duke Initiative for Science & Society}}</ref><ref>{{cite conference | title=Exploratory Dose-Escalation Study of NFC-1 in ADHD Adolescents With Glutamatergic Gene Network Variants. | conference=American Academy of Child and Adolescent Psychiatry | date=2015 | last1 = Jones | first1 = G | last2 = Dejesus-Rosario | first2 = N | last3 = Kao | first3 = C | last4 = Larsen | first4 = L | last5 = Chiavacci | first5 = R | last6 = Pallotto | first6 = A | last7 = Kurian | first7 = C | url=http://phx.corporate-ir.net/External.File?item=UGFyZW50SUQ9NTk5Mzk0fENoaWxkSUQ9MzEwMTg5fFR5cGU9MQ==&t=1}}</ref><ref>{{cite web | title=Efficacy and Safety of NFC-1 in Adolescents With Genetic Disorders Impacting mGluR and ADHD. | url=https://clinicaltrials.gov/ct2/show/NCT02777931 | author=ClinicalTrials.gov}} </ref> Aevi Genomic Medicine (formerly Medigenics<ref>{{cite web | title=Medgenics, Inc. Announces Name Change to Aevi Genomic Medicine, Inc. | url=http://http://www.prnewswire.com/news-releases/medgenics-inc-announces-name-change-to-aevi-genomic-medicine-inc-300378599.html | publisher=MarketWired}}</ref>), an emerging pharmaceutical firm, acquired the rights to develop this medication as of September, 2015. The company described fasoracetam as "a first-in-class non-stimulant, metabotropic glutamate receptor modulator."<ref>{{cite web | title=Medgenics: NFC-1 Could Be A Key Future Revenue Driver. | url=https://seekingalpha.com/article/4010894-medgenics-nfcminus-1-key-future-revenue-driver | author=Sharma, B.}} </ref> Medgenics announced a phase 2/3 clinical trial in June, 2016,<ref>{{cite web | title=Medgenics Announces Enrollment of First Patient in Phase 2/3 Clinical Trial of NFC-1 in Adolescents With mGluR Mutation Positive ADHD. | url=http://www.marketwired.com/press-release/medgenics-announces-enrollment-first-patient-phase-2-3-clinical-trial-nfc-1-adolescents-nyse-mdgn-2135254.htm | publisher=MarketWired}}</ref> from which results were released in March, 2017.<ref>{{cite web |url=http://adisinsight.springer.com/drugs/800003134|title=Drug Profile Fasoracetam }}</ref> In spite of what the market viewed as negative results,<ref>{{cite web | title=Why Aevi Genomic Medicine Got Crushed Today. | url=Why Aevi Genomic Medicine Got Crushed Today}}</ref> the company annonced plans for a Phase 2 clinical trial in the second half of 2017.<ref>{{cite web | title=MAevi Genomic Medicine Announces Plans to Initiate Phase 2 Clinical Trial to Confirm Genetic Responders to AEVI-001 and First Quarter 2017 Operating Results. | url=http://phx.corporate-ir.net/phoenix.zhtml?c=217925&p=irol-newsArticle&ID=2271808}}</ref>

==References==
==References==


Revision as of 22:00, 10 June 2017

Fasoracetam
Names
IUPAC name
(5R)-5-(piperidine-1-carbonyl) pyrrolidin-2-one
Other names
(5R)-5-oxo-D-prolinepiperidinamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
  • InChI=1S/C10H16N2O2/c13-9-5-4-8(11-9)10(14)12-6-2-1-3-7-12/h8H,1-7H2,(H,11,13)/t8-/m1/s1 checkY
    Key: GOWRRBABHQUJMX-MRVPVSSYSA-N checkY
  • InChI=1/C10H16N2O2/c13-9-5-4-8(11-9)10(14)12-6-2-1-3-7-12/h8H,1-7H2,(H,11,13)/t8-/m1/s1
    Key: GOWRRBABHQUJMX-MRVPVSSYBL
  • O=C(N1CCCCC1)[C@@H]2NC(=O)CC2
Properties
C10H16N2O2
Molar mass 196.250 g·mol−1
Pharmacology
Oral
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)

Fasoracetam (NS-105, 5-oxo-D-prolinepiperidinamide monohydrate[1], AEVI-001, LAM 105, MDGN-001, NFC 1[2]) is a research chemical of the racetam family.[3] It is a nootropic, and has been in a clinical trial for attention deficit hyperactivity disorder.[4]

In in vitro studies on mouse neurons, fasoracetam modulated mGluR II/III activity.[5] In studies in rats, it blocked memory disruptions caused by baclofen, a GABAB agonist[6] and upregulated production of GABAB receptors after repeat dosing.[7]

Clinical Trials

Fasoracetam was originally developed for use in the treatment of dementia, but was abandoned in Phase 3 clinical trials.[8] A Phase one safety study found a positive effect with 30 adolescents with ADHD and genetic disorders impacting metabotropic glutamate receptors (mGluRs).[9][10][11] Aevi Genomic Medicine (formerly Medigenics[12]), an emerging pharmaceutical firm, acquired the rights to develop this medication as of September, 2015. The company described fasoracetam as "a first-in-class non-stimulant, metabotropic glutamate receptor modulator."[13] Medgenics announced a phase 2/3 clinical trial in June, 2016,[14] from which results were released in March, 2017.[15] In spite of what the market viewed as negative results,[16] the company annonced plans for a Phase 2 clinical trial in the second half of 2017.[17]

References

  1. ^ FDA/NIH Substance registration system. Page accessed March 21, 2016
  2. ^ "Drug Profile Fasoracetam".
  3. ^ "5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary". Retrieved 21 July 2013.
  4. ^ "Drug Profile Fasoracetam".
  5. ^ Oka, M; Itoh, Y; Tatsumi, S; Ma, FH; Ukai, Y; Yoshikuni, Y; Kimura, K. "A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture". Naunyn Schmiedebergs Arch Pharmacol. 356: 189–96. doi:10.1007/pl00005040. PMID 9272724..
  6. ^ Ogasawara, T; Itoh, Y; Tamura, M; Mushiroi, T; Ukai, Y; Kise, M; Kimura, K. "Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer". Pharmacol Biochem Behav. 64: 41–52. doi:10.1016/s0091-3057(99)00108-2. PMID 10494996.
  7. ^ Shimidzu, T; Itoh, Y; Oka, M; Ishima, T; Ukai, Y; Yoshikuni, Y; Kimura, K. "Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment". Eur J Pharmacol. 338: 225–32. doi:10.1016/s0014-2999(97)81925-5. PMID 9424016.
  8. ^ Connolly, J; Glessner, J; Kao, C; Elia, J; Hakonarson, H. "ADHD & Pharmacotherapy: Past, Present and Future: A Review of the Changing Landscape of Drug Therapy for Attention Deficit Hyperactivity Disorder". Ther Innov Regul Sci. 49(5): 632–642. doi:10.1177/2168479015599811.
  9. ^ "Pediatric ADHD Study Shows Rare Genetic Mutation Underlies Condition in Some Patients". Duke Initiative for Science & Society.
  10. ^ Jones, G; Dejesus-Rosario, N; Kao, C; Larsen, L; Chiavacci, R; Pallotto, A; Kurian, C (2015). Exploratory Dose-Escalation Study of NFC-1 in ADHD Adolescents With Glutamatergic Gene Network Variants. American Academy of Child and Adolescent Psychiatry.
  11. ^ ClinicalTrials.gov. "Efficacy and Safety of NFC-1 in Adolescents With Genetic Disorders Impacting mGluR and ADHD".
  12. ^ "Medgenics, Inc. Announces Name Change to Aevi Genomic Medicine, Inc". MarketWired. {{cite web}}: Check |url= value (help)
  13. ^ Sharma, B. "Medgenics: NFC-1 Could Be A Key Future Revenue Driver".
  14. ^ "Medgenics Announces Enrollment of First Patient in Phase 2/3 Clinical Trial of NFC-1 in Adolescents With mGluR Mutation Positive ADHD". MarketWired.
  15. ^ "Drug Profile Fasoracetam".
  16. ^ [Why Aevi Genomic Medicine Got Crushed Today "Why Aevi Genomic Medicine Got Crushed Today"]. {{cite web}}: Check |url= value (help)
  17. ^ "MAevi Genomic Medicine Announces Plans to Initiate Phase 2 Clinical Trial to Confirm Genetic Responders to AEVI-001 and First Quarter 2017 Operating Results".


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