Drug intelligence / Profile preview

brexpiprazole + venlafaxine XR

Development stage
Unknown
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy consisting of **brexpiprazole**, an atypical antipsychotic, and **venlafaxine XR**, an extended-release serotonin-norepinephrine reuptake inhibitor (SNRI). Brexpiprazole acts as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors, and as an antagonist at serotonin 5-HT2A and noradrenergic α1B/α2C receptors. Venlafaxine XR inhibits the reuptake of serotonin and norepinephrine, enhancing neurotransmission of these monoamines in the CNS. The combined use is investigated as an adjunctive treatment in major depressive disorder, with neurophysiological evidence supporting normalization of serotonin and norepinephrine activity and increased dopamine neuron population activity via AMPA receptor facilitation. This combination is used where monotherapy with an antidepressant is insufficient to produce remission[1][5][7].

02

Targets

ADRA2C (α2C)SERT (Sodium-dependent serotonin transporter)HTR2A (Serotonin receptor 5-HT2A)ADRA1B (α1B)DRD2 (Dopamine D2 Receptor)NET (Norepinephrine Transporter)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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