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/abandoned
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
ECHA InfoCard 100.158.094 Edit this at Wikidata
Chemical and physical data
Formula C19H19N3O2S
Molar mass 353.44 g/mol
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[edit]

  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 : the Journal of the American Society for Experimental NeuroTherapeutics. 5 (3): 458–69. doi:10.1016/j.nurt.2008.05.008. PMID 18625457. 
  3. ^ 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. 
  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. ^ a b Taylor, Phil (Jan 8, 2018). "Axovant slumps as it dumps lead drug intepirdine". Fierce Biotech.