Edivoxetine

Edivoxetine (INN; code name LY-2216684) is a drug which acts as a selective norepinephrine reuptake inhibitor and was under development by Eli Lilly for attention-deficit disorder (ADD) and as an antidepressant treatment.[1][2] It was in phase III clinical trials, in 2012, for major depressive disorder, but failed to get approval.[1][3]

Edivoxetine
Clinical data
ATC code
  • None
Legal status
Legal status
  • Development terminated
Identifiers
IUPAC name
  • (1R)-2-(5-fluoro-2-methoxyphenyl)-1-[(2S)-morpholin-2-yl]-1-(tetrahydro-2H-pyran-4-yl)ethanol
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H26FNO4
Molar mass339.407 g·mol−1
3D model (JSmol)
SMILES
  • COC1=C(C=C(C=C1)F)C[C@]([C@@H]2CNCCO2)(C3CCOCC3)O
InChI
  • InChI=1S/C18H26FNO4/c1-22-16-3-2-15(19)10-13(16)11-18(21,14-4-7-23-8-5-14)17-12-20-6-9-24-17/h2-3,10,14,17,20-21H,4-9,11-12H2,1H3/t17-,18+/m0/s1
  • Key:CPBHSHYQQLFAPW-ZWKOTPCHSA-N

Effectiveness

In a study published in 2010, edivoxetine succeeded to prove superiority over placebo, as measured by Hamilton Depression Rating Scale. However, effectiveness could be observed using the Self-Rated Quick Inventory of Depressive Symptomatology.[4]

In a study published in 2011, using the Montgomery–Åsberg Depression Rating Scale and the Sheehan Disability Scale, edivoxetine showed superiority over placebo, with higher response and remission rates.[5]

In December 2013, Eli Lilly announced that the clinical development of edivoxetine will be stopped due to lack of efficacy compared to SSRI alone in three separate clinical trials.[6]

Side effects

Side effects significantly associated with edivoxetine are headache, nausea, constipation, dry mouth and insomnia.[4]

The above-mentioned studies report increases of the cardiac rhythm, and one also increases of diastolic and systolic blood pressures.[4][5]

See also

References
  1. Jun Yan (March 2012). "Pipeline for new antidepressants flowing slowly". Psychiatric News. American Psychiatric Association. 47 (5): 1b–29. doi:10.1176/pn.47.5.psychnews_47_5_1-b. Retrieved 2012-04-27.
  2. "Statement on a nonproprietary name adopted by the USAN council - Edivoxetine" (PDF) (Press release). American Medical Association. 2012. Retrieved 2012-04-12.
  3. Chancellor D (November 2011). "The depression market". Nature Reviews. Drug Discovery. 10 (11): 809–10. doi:10.1038/nrd3585. PMID 22037032. S2CID 3194093.
  4. Dubé S, Dellva MA, Jones M, Kielbasa W, Padich R, Saha A, Rao P (April 2010). "A study of the effects of LY2216684, a selective norepinephrine reuptake inhibitor, in the treatment of major depression". Journal of Psychiatric Research. 44 (6): 356–363. doi:10.1016/j.jpsychires.2009.09.013. PMID 19909980.
  5. Pangallo P, Dellva MA, D'Souza DN, Essink B, Russell J, Goldberger C (June 2011). "A randomized, double-blind study comparing LY2216684 and placebo in the treatment of major depressive disorder". Journal of Psychiatric Research. 45 (6): 748–755. doi:10.1016/j.jpsychires.2011.03.014. PMID 21511276.
  6. "Lilly Announces Edivoxetine Did Not Meet Primary Endpoint of Phase III Clinical Studies as Add-On Therapy for Major Depressive Disorder | Eli Lilly and Company".
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