Landipirdine

Landipirdine

Clinical data
Other names	RO-5025181; RO5025181; SYN-120; SYN120
Drug class	Serotonin 5-HT2A receptor antagonist; Serotonin 5-HT6 receptor antagonist
ATC code	None
Identifiers
IUPAC name [(1R)-6-(3-fluorophenyl)sulfonyl-1,2,3,4-tetrahydronaphthalen-1-yl]methylurea
CAS Number	1000308-25-7
PubChem CID	46220503
DrugBank	DB16214
UNII	J0NX985GDI
KEGG	D11157
ChEMBL	ChEMBL1082508
Chemical and physical data
Formula	C18H19FN2O3S
Molar mass	362.42 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1C[C@H](C2=C(C1)C=C(C=C2)S(=O)(=O)C3=CC=CC(=C3)F)CNC(=O)N
InChI InChI=1S/C18H19FN2O3S/c19-14-5-2-6-15(10-14)25(23,24)16-7-8-17-12(9-16)3-1-4-13(17)11-21-18(20)22/h2,5-10,13H,1,3-4,11H2,(H3,20,21,22)/t13-/m0/s1 Key:MTTHRRVVGMPYQG-ZDUSSCGKSA-N

Landipirdine (INN Tooltip International Nonproprietary Name, USAN Tooltip United States Adopted Name; developmental code names RO-5025181 and SYN-120) is a serotonin 5-HT_2A and 5-HT₆ receptor antagonist which was under development for the treatment of dementia and cognition disorders but was never marketed. ^{[1] [2] [3]} It is taken orally. ^[1] The drug was developed by Roche, Accorda Therapeutics, and Biotie Therapies. ^[1] It reached phase 2 clinical trials for dementia and phase 1 trials for cognition disorders prior to the discontinuation of its development in 2020. ^{[1] [2]} Landipirdine was first described in the scientific literature by at least 2010. ^{[4] [5]}

References

1. "Acorda Therapeutics". AdisInsight. 9 March 2020. Retrieved 18 January 2026.
2. Wicke K, Haupt A, Bespalov A (2015). "Investigational drugs targeting 5-HT6 receptors for the treatment of Alzheimer's disease". Expert Opinion on Investigational Drugs. 24 (12): 1515–1528. doi:10.1517/13543784.2015.1102884. PMID   26548316.
3. Fernandez HH, Weintraub D, Macklin E, Litvan I, Schwarzschild MA, Eberling J, et al. (September 2023). "Safety, tolerability, and preliminary efficacy of SYN120, a dual 5-HT6/5-HT2A antagonist, for the treatment of Parkinson disease dementia: A randomized, controlled, proof-of-concept trial". Parkinsonism & Related Disorders. 114 105511. doi:10.1016/j.parkreldis.2023.105511. PMID   37532622.
4. Ivachtchenko AV, Ivanenkov YA, Tkachenko SE (September 2010). "5-hydroxytryptamine subtype 6 receptor modulators: a patent survey". Expert Opinion on Therapeutic Patents. 20 (9): 1171–1196. doi:10.1517/13543776.2010.494661. PMID   20716023.
5. Rossé G, Schaffhauser H (2010). "5-HT6 receptor antagonists as potential therapeutics for cognitive impairment". Current Topics in Medicinal Chemistry. 10 (2): 207–221. doi:10.2174/156802610790411036. PMID   20166958.