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-HT2A and was under development for the treatment of insomnia.[1] It was shown to be effective and well-tolerated in clinical trials,[2][3] but development was halted in December 2008 because the substance did not meet the trial's effectiveness endpoints.[4] Research continues on newer analogues which may potentially be more successful.[5] More recently, nelotanserin has been repurposed for the treatment of Lewy body disease.[6] As of 2017, it is in phase II clinical trials for this indication.[6]

Clinical data
Other namesAPD-125
Routes of
ATC code
  • none
CAS Number
PubChem CID
CompTox Dashboard (EPA)
Chemical and physical data
Molar mass437.238 g/mol g·mol−1
3D model (JSmol)
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  1. Teegarden, B. R.; Li, H.; Jayakumar, H.; Strah-Pleynet, S.; Dosa, P. I.; Selaya, S. D.; Kato, N.; Elwell, K. H.; Davidson, J.; Cheng, K.; Saldana, H.; Frazer, J. M.; Whelan, K.; Foster, J.; Espitia, S.; Webb, R. R.; Beeley, N. R. A.; Thomsen, W.; Morairty, S. R.; Kilduff, T. S.; Al-Shamma, H. A. (2010). "Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2AInverse Agonists for the Treatment of Insomnia". Journal of Medicinal Chemistry. 53 (5): 1923–1936. doi:10.1021/jm9007328. PMID 20143782.
  2. Rosenberg, R; Seiden, DJ; Hull, SG; Erman, M; Schwartz, H; Anderson, C; Prosser, W; Shanahan, W; et al. (2008). "APD125, a selective serotonin 5-HT2A receptor inverse agonist, significantly improves sleep maintenance in primary insomnia". Sleep. 31 (12): 1663–71. doi:10.1093/sleep/31.12.1663. PMC 2603489. PMID 19090322.
  3. Al-Shamma, H. A.; Anderson, C.; Chuang, E.; Luthringer, R.; Grottick, A. J.; Hauser, E.; Morgan, M.; Shanahan, W.; Teegarden, B. R.; Thomsen, W. J.; Behan, D. (2009). "Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia". Journal of Pharmacology and Experimental Therapeutics. 332 (1): 281–290. doi:10.1124/jpet.109.160994. PMID 19841476.
  4. APD125 for Insomnia Archived 2009-08-26 at the Wayback Machine
  5. Xiong, Y.; Ullman, B.; Choi, J. S. K.; Cherrier, M.; Strah-Pleynet, S.; Decaire, M.; Dosa, P. I.; Feichtinger, K.; Teegarden, B. R.; Frazer, J. M.; Yoon, W. H.; Shan, Y.; Whelan, K.; Hauser, E. K.; Grottick, A. J.; Semple, G.; Al-Shamma, H. (2010). "Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine2A Receptor Antagonists for the Treatment of Insomnia". Journal of Medicinal Chemistry. 53 (15): 5696–5706. doi:10.1021/jm100479q. PMID 20684606.
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