Eplivanserin

Eplivanserin

Eplivanserin
Systematic (IUPAC) name
(Z,E)-1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime
Clinical data
Legal status
?
Routes Oral
Identifiers
CAS number
130580-02-8 (fumarate)
ATC code None
PubChem
ChemSpider
UNII  YesY
KEGG  YesY
Chemical data
Formula C19H21FN2O2 
Mol. mass 328.381 g/mol
 YesY   

Eplivanserin (SR-46,349; planned trade name Ciltyri) was an experimental drug for the treatment of insomnia which was being developed by Sanofi Aventis.[1]

Sanofi Aventis announced in December 2009 that it was withdrawing its application for approval of eplivanserin from both the U.S. Food and Drug Administration and the European Medicines Agency.[2]

Mechanism of action

Eplivanserin is an inverse agonist on the serotonin receptor subtype 5-HT2A. In contrast to older sedating drugs acting on 5-HT2A receptors (e.g., mirtazapine, clozapine, risperidone), eplivanserin has practically no affinity to dopamine, histamine and adrenergic receptors.[3]

Study results

In a placebo controlled Phase II clinical trial with 351 subjects, eplivanserin reduced the sleep latency by 39 minutes (versus 26 minutes under placebo).[3]

See also

References

  1. ^ "Future Treatments for Depression, Anxiety, Sleep Disorders, Psychosis, and ADHD -- Neurotransmitter.net". 
  2. ^ Spencer, Mimosa; Berton, Elena (21 December 2009). "Sanofi-Aventis Discontinues Eplivanserin For Insomnia". Dow Jones & Co. Retrieved 27 January 2010. 
  3. ^ a b Teergarden, BR; Al Shamma, H, Xiong, Y (2008). "5-HT2A Inverse-Agonists for the Treatment of Insomnia". Current Topics in Medicinal Chemistry 8 (11): 969–976.