Propriétés pharmacologiques de la vortioxetine et leurs conséquences pré-cliniques

Feb 17, 2016L'Encephale

Drug effects of vortioxetine and their early lab results

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Abstract

Vortioxetine is a novel multi-target antidepressant drug approved by the FDA and European Medicines Agency.

Vortioxetine differs from traditional SSRIs by not only inhibiting serotonin reuptake but also antagonizing and partially agonizing various serotonin receptors.
It may enhance the effectiveness of treatment for major depressive disorder by targeting specific serotonin receptors associated with anxiolytic and antidepressant effects.
Studies in animal models suggest that vortioxetine improves cognitive functions such as working memory, episodic memory, cognitive flexibility, and spatial memory.
Cognitive dysfunction is commonly associated with major depressive disorder, making vortioxetine's cognitive benefits particularly relevant.
Further investigation is needed, particularly regarding its efficacy for patients who do not respond adequately to existing antidepressants.

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Selective Serotonin Reuptake Inhibitors (SSRIs) are extensively used for the treatment of major depressive disorder (MDD). SSRIs are defined as indirect receptor agonists since the activation of postsynaptic receptors is a consequence of an increase in extracellular concentrations of serotonin (5-HT) mediated by the blockade of serotonin transporter. The activation of some serotoninergic receptors (5-HT1A, post-synaptic, 5-HT1B post-synaptic, 5-HT2B, and 5-HT4), but not all (5-HT1A, pre-synaptic, 5-HT1B pre-synaptic, 5-HT2A, 5-HT2C, 5-HT3, and probably 5-HT6), induces anxiolytic/antidepressive - like effects. Targetting specifically some of them could potentially improve the onset of action and/or efficacy and/or prevent MD relapse. Vortioxetine (Brintellix, 1- [2-(2,4-dimethylphenyl-sulfanyl)-phenyl]-piperazine) is a novel multi-target antidepressant drug approved by the Food and Drug Administration (FDA) and by European Medicines Agency. Its properties are markedly different from the extensively prescribed SSRIs. Compared to the SSRIs, vortioxetine is defined as a multimodal antidepressant drug since it is not only a serotonin reuptake inhibitor, but also a 5-HT1D, 5-HT3, 5-HT7 receptor antagonist, 5-HT1B receptor partial agonist and 5-HT1A receptor agonist. This specific pharmacological profile enables vortioxetine to affect not only the serotoninergic and noradrenergic systems, but also the histaminergic, cholinergic, gamma-butyric acid (GABA) ergic and glutamatergic ones. Thus, vortioxetine not only induces antidepressant-like or anxiolytic-like activity but also improves cognitive parameters in several animal models. Indeed, vortioxetine was shown to improve working memory, episodic memory, cognitive flexibility and spatial memory in young adult rodents and also in old animal models. These specific effects of the vortioxetine are of interest considering that cognitive dysfunction is a common comorbidity to MDD. Altogether, even though this molecule still needs to be investigated further, especially in the insufficient-response to antidepressant drugs, vortioxetine is already an innovative therapeutic option for the treatment of major depression.

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Propriétés pharmacologiques de la vortioxetine et leurs conséquences pré-cliniques

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