Intepirdine

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Intepirdine
SB-742457-structure.png
Clinical data
Synonyms SB-742457, RVT-101
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
ECHA InfoCard 100.158.094
Chemical and physical data
Formula C19H19N3O2S
Molar mass 353.44 g/mol
3D model (JSmol)
 NYesY (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]

Results of a phase III clinical trial were reported in September 2017.[9][10] The trial showed no improvement over control group.[11] Axovant lost 70% of its value upon the announcement of the trial results.[12]

It is also in a phase 2 trial for dementia with Lewy bodies.[13]

References[edit]

  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. ^ [1]
  12. ^ https://www.statnews.com/2017/09/26/axovant-intepirdine-trial/
  13. ^ Study Evaluating Intepirdine (RVT-101) in Subjects With Dementia With Lewy Bodies: The HEADWAY-DLB Study