Eplivanserin

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Eplivanserin
Eplivanserin structure.svg
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 130579-75-8
130580-02-8 (fumarate)
ATC code None
PubChem CID 5493160
ChemSpider 13267837
UNII 3CO94WO6DJ YesY
KEGG D10006 YesY
Chemical data
Formula C19H21FN2O2 
Mol. mass 328.381 g/mol
 YesY (what is this?)  (verify)

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[edit]

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[edit]

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[edit]

References[edit]

  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. doi:10.2174/156802608784936700. PMID 18673166.