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Chemical compound
Intepirdine
Clinical data
Other namesSB-742457, RVT-101
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational/abandoned
Identifiers
  • 3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.158.094 Edit this at Wikidata
Chemical and physical data
FormulaC19H19N3O2S
Molar mass353.44 g·mol
3D model (JSmol)
  • C3CNCCN3c1cccc(c1nc4)cc4S(=O)(=O)c2ccccc2
  • InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2
  • Key:JJZFWROHYSMCMU-UHFFFAOYSA-N
  (what is: this?)  (verify)

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

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

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

References※

  1. ^ "Intepirdine - Axovant Sciences / GlaxoSmithKline". AdisInsight. Retrieved 9 January 2018.
  2. ^ Upton N, "Chuang TT," Hunter AJ, Virley DJ (July 2008). "5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease". Neurotherapeutics. 5 (3): 458–69. doi:10.1016/j.nurt.2008.05.008. PMC 5084247. PMID 18625457.
  3. ^ Rossé G, Schaffhauser H (February 2010). "5-HT(6) Receptor Antagonists as Potential Therapeutics for Cognitive Impairment". Current Topics in Medicinal Chemistry. 10 (2): 207–21. doi:10.2174/156802610790411036. PMID 20166958.
  4. ^ Lowe, Derek (12 May 2015). "An Alzheimer's IPO, Because Why Not". In the Pipeline.
  5. ^ Fiore, Kristina (27 September 2016). "NeuroBreak: Alzheimer's Drug Bombs; Elephant Tranquilizer ODs". MedPage Today.
  6. ^ Garde, Damian (26 September 2017). "Another Alzheimer's failure: Axovant's drug flops in late-stage trial". STAT.
  7. ^ Taylor, Phil (Jan 8, 2018). "Axovant slumps as it dumps lead drug intepirdine". Fierce Biotech.
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