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Intepirdine

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Intepirdine
Clinical data
Other namesSB-742457, RVT-101
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
  • 3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.158.094 Edit this at Wikidata
Chemical and physical data
FormulaC19H19N3O2S
Molar mass353.44 g/mol g·mol−1
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 ☒N
  • Key:JJZFWROHYSMCMU-UHFFFAOYSA-N ☒N
 ☒NcheckY (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][4][5] It was under development by GlaxoSmithKline for the treatment of Alzheimer's disease and demonstrated some preliminary efficacy in phase II clinical trials;[4][5][6] however, GSK chose not to continue development and sold the rights to Axovant Sciences in December 2014.[7][8]

A phase 3 clinical trial for Alzheimer's is due to report in 2017.[9][10]

It is also in a phase 2 trial for dementia with Lewy bodies.[11]

References

  1. ^ "RVT-101". Axovant.
  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 : the Journal of the American Society for Experimental NeuroTherapeutics. 5 (3): 458–69. doi:10.1016/j.nurt.2008.05.008. PMID 18625457.
  3. ^ Idris N, Neill J, Grayson B, et al. (January 2010). "Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms". Psychopharmacology. 208 (1): 23–36. doi:10.1007/s00213-009-1702-5. PMID 19851757.
  4. ^ a b Maher-Edwards G, Zvartau-Hind M, Hunter AJ, et al. (December 2009). "Double-Blind, Controlled Phase II Study of a 5-HT6 Receptor Antagonist, SB-742457, in Alzheimer's Disease". Current Alzheimer Research. 7 (5): 374–85. PMID 20043816.
  5. ^ a b 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.
  6. ^ "Search of: SB-742457 - List Results - ClinicalTrials.gov".
  7. ^ "Axovant Acquires SB742457 from GlaxoSmithKline" (Press release). Axovant. December 23, 2014.[self-published source]
  8. ^ House, Douglas W. (June 5, 2015). "Axovant Sciences on deck for IPO". Seeking Alpha.
  9. ^ NeuroBreak: Alzheimer's Drug Bombs; Sept 2016
  10. ^ Study Evaluating Intepirdine (RVT-101) in Subjects With Mild to Moderate Alzheimer's Disease on Donepezil: MINDSET Study
  11. ^ Study Evaluating Intepirdine (RVT-101) in Subjects With Dementia With Lewy Bodies: The HEADWAY-DLB Study

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