Chemistry:Fasoracetam

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Fasoracetam
Fasoracetam.svg
Fasoracetam3d.png
Names
IUPAC name
(5R)-5-(Piperidine-1-carbonyl)pyrrolidin-2-one
Other names
(5R)-5-Oxo-D-prolinepiperidinamide monohydrate, NS-105, AEVI-001, LAM 105, MDGN-001, NFC 1[1][2]
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
Properties
C10H16N2O2
Molar mass 196.250 g·mol−1
Pharmacology
Oral
Legal status
  • AU: S4 (Prescription only)
  • US: Not FDA approved
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references
Tracking categories (test):

Fasoracetam is a research chemical of the racetam family.[3] It is a putative nootropic that failed to show sufficient efficacy in clinical trials for vascular dementia. It is currently being studied for its potential use for attention deficit hyperactivity disorder.[2][4]

Fasoracetam appears to agonize all three groups of metabotropic glutamate receptors and has improved cognitive function in rodent studies.[5] It is orally bioavailable and is excreted mostly unchanged via the urine.[6]

Fasoracetam was discovered by scientists at the Japanese pharmaceutical company Nippon Shinyaku, which brought it through Phase 3 clinical trials for vascular dementia, and abandoned it due to lack of efficacy.[5][7]

Scientists at Children's Hospital of Philadelphia led by Hakon Hakonarson have studied fasoracetam's potential use in attention deficit hyperactivity disorder.[5] Hakonarson's company neuroFix tried to bring the drug to market for this use; neuroFix acquired Nippon Shinyaku's clinical data as part of its efforts.[7][8] neuroFix was acquired by Medgenics in 2015.[8] Medgenics changed its name to Aevi Genomic Medicine in 2016.[9]

Clinical trials in adolescents with ADHD who also have mGluR mutations started in 2016.[8] While Fasoracetam may be effective in the treatment of ADHD in people with specific mGluR mutations, these represent around 10% of total ADHD cases, and Fasoracetam is likely ineffective in all other cases.[10][11] Studies showing improvements in cognitive function from Fasoracetam have exclusively been done on rodents.[10]

Legality

Australia

Fasoracetam is a schedule 4 substance in Australia under the Poisons Standard (February 2020).[12] A schedule 4 substance is classified as "Prescription Only Medicine, or Prescription Animal Remedy – Substances, the use or supply of which should be by or on the order of persons permitted by State or Territory legislation to prescribe and should be available from a pharmacist on prescription."[12]

See also

References

  1. ↑ FDA/NIH Substance registration system. Page accessed March 21, 2016
  2. ↑ 2.0 2.1 "Drug Profile Fasoracetam". http://adisinsight.springer.com/drugs/800003134. 
  3. ↑ "5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary". https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=198695. 
  4. ↑ "Recommended INN List 40". WHO Drug Information 12 (2). 1998. https://mednet-communities.net/inn/db/media/docs/r-innlist40.pdf. 
  5. ↑ 5.0 5.1 5.2 Connolly, J; Glessner, J; Kao, C; Elia, J; Hakonarson, H (2015). "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. PMID 26366330. 
  6. ↑ Malykh, AG; Sadaie, MR (12 February 2010). "Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders.". Drugs 70 (3): 287–312. doi:10.2165/11319230-000000000-00000. PMID 20166767. 
  7. ↑ 7.0 7.1 Moskowitz, D. H. (2017) (in en). Finding the Genetic Cause and Therapy for ADHD, Autism and 22q. BookBaby (self published). ISBN 9781483590981. https://books.google.com/books?id=LSrlDQAAQBAJ&pg=PT117. 
  8. ↑ 8.0 8.1 8.2 Sharma, B. (7 October 2016). "Medgenics: NFC-1 Could Be A Key Future Revenue Driver.". Seeking Alpha. https://seekingalpha.com/article/4010894-medgenics-nfcminus-1-key-future-revenue-driver. 
  9. ↑ "Press Release: Medgenics, Inc. Announces Name Change to Aevi Genomic Medicine, Inc.". Aevi via MarketWired. 16 December 2016. http://www.prnewswire.com/news-releases/medgenics-inc-announces-name-change-to-aevi-genomic-medicine-inc-300378599.html. 
  10. ↑ 10.0 10.1 Elia, Josephine; Ungal, Grace; Kao, Charlly; Ambrosini, Alexander; De Jesus-Rosario, Nilsa; Larsen, Lene; Chiavacci, Rosetta; Wang, Tiancheng et al. (2018-01-16). "Fasoracetam in adolescents with ADHD and glutamatergic gene network variants disrupting mGluR neurotransmitter signaling". Nature Communications 9 (1): 4. doi:10.1038/s41467-017-02244-2. ISSN 2041-1723. PMID 29339723. Bibcode: 2018NatCo...9....4E. 
  11. ↑ Tardner, P (2020-09-09). "Fasoracetam as a treatment for ADHD: A systematic review of available clinical data" (in en-US). International Journal of Environmental Science & Technology. https://www.ijest.org/fasoracetam-treatment-adhd-a-systematic-review/. 
  12. ↑ 12.0 12.1 Poisons Standard February 2020. comlaw.gov.au



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