Chemistry:Intepirdine

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Short description: Chemical compound
Intepirdine
Intepirdine.svg
Clinical data
Other namesSB-742457, RVT-101
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational/abandoned
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC19H19N3O2S
Molar mass353.44 g·mol−1
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Intepirdine (INN; developmental codes SB-742457, RVT-101)[1] is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects.[2][3] It was under development by GlaxoSmithKline for the treatment of Alzheimer's disease and demonstrated some preliminary efficacy in phase II clinical trials.[3] GSK chose not to continue development and sold the rights to Axovant Sciences for $5 million in December 2014.[4]

Results of a phase III clinical trial for the treatment of Alzheimer's disease were reported in September 2017.[5] The trial showed no improvement over control group and Axovant lost 70% of its value upon the announcement of the trial results.[6]

Intepirdine also entered clinical trials for dementia with Lewy bodies, also with negative results.[7] Consequently, Axovant announced in 2018 that it has discontinued development of this drug.[7]

References

  1. ↑ "Intepirdine - Axovant Sciences / GlaxoSmithKline" (in en). AdisInsight. http://adisinsight.springer.com/drugs/800020107. 
  2. ↑ "5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease". Neurotherapeutics 5 (3): 458–69. July 2008. doi:10.1016/j.nurt.2008.05.008. PMID 18625457. 
  3. ↑ 3.0 3.1 "5-HT(6) Receptor Antagonists as Potential Therapeutics for Cognitive Impairment". Current Topics in Medicinal Chemistry 10 (2): 207–21. February 2010. doi:10.2174/156802610790411036. PMID 20166958. 
  4. ↑ Lowe, Derek (12 May 2015). "An Alzheimer's IPO, Because Why Not". In the Pipeline. https://www.science.org/content/blog-post/alzheimer-s-ipo-because-why-not. 
  5. ↑ Fiore, Kristina (27 September 2016). "NeuroBreak: Alzheimer's Drug Bombs; Elephant Tranquilizer ODs" (in en). MedPage Today. https://www.medpagetoday.com/Neurology/GeneralNeurology/60482. 
  6. ↑ Garde, Damian (26 September 2017). "Another Alzheimer's failure: Axovant's drug flops in late-stage trial". STAT. https://www.statnews.com/2017/09/26/axovant-intepirdine-trial/. 
  7. ↑ 7.0 7.1 Taylor, Phil (Jan 8, 2018). "Axovant slumps as it dumps lead drug intepirdine". Fierce Biotech. https://www.fiercebiotech.com/biotech/axovant-slumps-as-it-dumps-lead-drug-intepirdine. 



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