Edivoxetine

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	1194508-25-2 1194374-05-4 (hydrochloride)
PubChem CID	11186829
ChemSpider	9361913
UNII	3W9N3F4JOO
KEGG	D09890
CompTox Dashboard (EPA)	DTXSID70152464
Chemical and physical data
Formula	C18H26FNO4
Molar mass	339.407 g·mol−1
3D model (JSmol)	Interactive image
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

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]}

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

• Esreboxetine

References

1. Jun Yan (March 2012). "Pipeline for new antidepressants flowing slowly" . Psychiatric News. 47 (5): 1b–29. doi:10.1176/pn.47.5.psychnews_47_5_1-b . Retrieved 2012-04-27– via American Psychiatric Association.
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".