Drug intelligence / Profile preview

brexpiprazole + duloxetine

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

Overview

**Brexpiprazole + duloxetine** is a combination of two approved psychiatric medications used for the treatment of major depressive disorder, typically where brexpiprazole acts as adjunctive therapy to other antidepressants. **Brexpiprazole** is a second-generation (atypical) antipsychotic and serotonin-dopamine activity modulator whose mechanism includes partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors, and antagonist activity at serotonin 5-HT2A, 5-HT2B, 5-HT7, and multiple adrenergic receptors. **Duloxetine** is a serotonin-norepinephrine reuptake inhibitor (SNRI) that increases levels of serotonin and norepinephrine by inhibiting their reuptake, with minor inhibition of dopamine reuptake. The combination is used to address symptoms of depression resistant to monotherapy, leveraging complementary mechanisms of action: brexpiprazole modulates monoaminergic receptor activity, while duloxetine raises monoamine levels in the synaptic cleft by blocking reuptake. There is a clinically significant drug interaction between the two, warranting careful monitoring for side effects such as serotonin syndrome and CNS effects[1][3][6][7].

Brand names
Rxulti
Other names
brexpiprazole + duloxetine
02

Targets

HTR2A (Serotonin receptor 5-HT2A)ADRA1B (α1B)SERT (Sodium-dependent serotonin transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA2C (α2C)DAT (Dopamine plasma membrane transport protein)HTR2B (5-Hydroxytryptamine Receptor 2B)DRD2 (Dopamine D2 Receptor)HTR7 (5-hydroxytryptamine receptor 7)DRD3 (Dopamine receptor D3)NET (Norepinephrine Transporter)

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