TRINTELLIX® (vortioxetine) is indicated for the treatment of Major Depressive Disorder (MDD) in adults.

MOA

The story of TRINTELLIX

The first and only compound with this combination of pharmacologic activity:

Mechanism of action1

The mechanism of the antidepressant effect of TRINTELLIX is not fully understood, but it is thought to be related to its enhancement of serotonergic activity in the central nervous system through inhibition of the reuptake of serotonin (5-HT). It also has several other activities including 5-HT3 receptor antagonism and 5-HT1A receptor agonism. The contribution of these activities to the antidepressant effect of TRINTELLIX has not been established.

Pharmacodynamics1

TRINTELLIX strongly inhibits SERT and has strong affinities for 5 other serotonin receptors.* The clinical relevance of these activities is unknown.

TRINTELLIX (vortioxetine) Mechanism of Action (MOA)

*TRINTELLIX binds with high affinity to the human serotonin transporter (Ki=1.6 nM), but not to the norepinephrine (Ki=113 nM) or dopamine (Ki>1000 nM) transporters.1 TRINTELLIX potently and selectively inhibits reuptake of serotonin (IC50=5.4 nM). TRINTELLIX binds to 5‑HT3 (Ki=3.7 nM), 5-HT1A (Ki=15 nM), 5-HT7 (Ki=19 nM), 5‑HT1D (Ki=54 nM), and 5-HT1B (Ki=33 nM) receptors, and is a 5-HT3, 5-HT1D, and 5-HT7 receptor antagonist, 5-HT1B receptor partial agonist, and 5-HT1A receptor agonist.

Abbreviations: SERT, serotonin transporter.



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