nelotanserin

Nelotanserin is a highly selective small molecule inverse agonist of the serotonin 5-hydroxytryptamine 2A (5-HT2A) receptor. It was originally developed by Arena Pharmaceuticals for the treatment of insomnia but failed to meet efficacy endpoints in Phase 2 trials and was discontinued for this indication. Later, Axovant Sciences repurposed nelotanserin for neuropsychiatric symptoms associated with Lewy body dementia (LBD), including visual hallucinations and REM sleep behavior disorder (RBD). Nelotanserin demonstrated high selectivity and potency at the 5‑HT2A receptor, with much lower affinity for related serotonin receptors (notably over 260-fold selectivity versus the 5‑HT2C receptor). Clinical studies showed that while nelotanserin was generally well-tolerated, it did not meet primary efficacy endpoints in LBD or RBD trials. As a result, clinical development has been discontinued[1][3][4][7].

Other names

1-[3-(4-bromo-1-methyl-1H-pyrazol-5-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea839713-36-9