Nelotanserin

Nelotanserin

File:Nelotanserin structure.png
Clinical data
Other names	APD-125
Routes of administration	Oral
ATC code	none
Identifiers
IUPAC name 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea
CAS Number	839713-36-9 checkY
PubChem CID	11683556
ChemSpider	9858284 ☒N
UNII	4ZA73QEW2P
KEGG	D09645
E number	{{#property:P628}}
CompTox Dashboard (EPA)	{{#property:P3117}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C18H15BrF2N4O2
Molar mass	437.245 g·mol−1
3D model (JSmol)	Interactive image
SMILES Brc1cnn(C)c1-c2cc(ccc2OC)NC(=O)Nc3ccc(F)cc3F
InChI InChI=1S/C18H15BrF2N4O2/c1-25-17(13(19)9-22-25)12-8-11(4-6-16(12)27-2)23-18(26)24-15-5-3-10(20)7-14(15)21/h3-9H,1-2H3,(H2,23,24,26) ☒N Key:COSPVUFTLGQDQL-UHFFFAOYSA-N ☒N
☒NcheckY (what is this?)  (verify)

Nelotanserin (former developmental code name APD-125) is a drug developed by Arena Pharmaceuticals which acts as an inverse agonist on the serotonin receptor subtype 5-HT_2A and was under development for the treatment of insomnia. It was shown to be effective and well tolerated in clinical trials, but development was halted in December 2008 because the substance did not meet the trial's effectiveness endpoints. Research continues on newer analogues which may potentially be more successful.

Usages

Later, nelotanserin was repurposed for the treatment of Lewy body dementia (LBD) by Axovant Sciences (now Sio Gene Therapies). In late 2018, the company announced that while nelotanserin was generally well-tolerated by LBD patients in a small Phase 2 clinical trial for the treatment of REM sleep behavior disorder (RBD) and there were positive indications on some secondary trial outcomes such as sleep diaries and some polysomnogram sleep parameters, the drug failed to meet its primary endpoint of reducing the frequency of RBD episodes and would be discontinued.