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28 March 2013 - Just published: pharmacology of the antidepressant Levomilnacipran

The most frequently prescribed antidepressant drugs are selective serotonin reuptake inhibitors (SSRIs) such as citalopram and fluoxetine. Although well tolerated, SSRIs show limitations such as modest response rates (about a third of depressed patients fail to improve) and extended delay of therapeutic onset (several weeks). One strategy to improve  therapeutic efficacy, at least in some patient populations, is to develop drugs such as levomilnacipran that act on both the serotonergic and noradrenergic systems (SNRIs). Levomilnacipran is the active enantiomer of milnacipran (commercialized as an antidepressant in France and Japan) and is intended for commercialisation in the USA.

The present publication characterises the in vitro and in vivo pharmacological activity of levomilnacipran and shows that it has accentuated noradrenergic vs serotonergic activity, unlike the other SNRIs, duloxetine and venlafaxine. The distinctive balance of activity of levomilnacipran may translate to a different therapeutic profile in clinical use. Levomilnacipran was developed in the USA by Forest laboratories is currently awaiting FDA approval.

Adrian Newman-Tancredi participated in the characterisation of levomilnacipran and has extensive experience of drug discovery of novel antidepressants. For more information, Contact.

 

Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety.

Auclair AL, Martel JC, Assié MB, Bardin L, Heusler P, Cussac D, Marien M, Newman-Tancredi A, O'Connor J, Depoortère R.
Neuropharmacology. 2013 Jul;70:338-47. doi: 10.1016/j.neuropharm.2013.02.024. Epub 2013 Mar 13.