Intepirdine

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]

Intepirdine

Clinical data
Other names	SB-742457, RVT-101
Routes of administration	Oral
ATC code	none
Legal status
Legal status	Investigational/abandoned
Identifiers
IUPAC name 3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline
CAS Number	607742-69-8^Y
PubChem CID	11256720
ChemSpider	9431746^N
UNII	2IOB2M82HY
KEGG	D10942
ChEMBL	ChEMBL1083390^N
CompTox Dashboard (EPA)	DTXSID30976249
ECHA InfoCard	100.158.094
Chemical and physical data
Formula	C19H19N3O2S
Molar mass	353.44 g·mol^−1
3D model (JSmol)	Interactive image
SMILES C3CNCCN3c1cccc(c1nc4)cc4S(=O)(=O)c2ccccc2
InChI 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
^NY (what is this?)  (verify)

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". 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.