Drug intelligence / Profile preview

venlafaxine XR + aripiprazole

Development stage
Unknown
Lead developer
Otsuka Holdings
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral, Intramuscular
01

Overview

Venlafaxine XR + aripiprazole is a combination therapy consisting of two pharmaceutical agents used primarily in the management of major depressive disorder (MDD), particularly in cases resistant to monotherapy. Venlafaxine extended-release (XR) is a serotonin-norepinephrine reuptake inhibitor (SNRI) that increases synaptic concentrations of serotonin and norepinephrine by inhibiting their reuptake. Aripiprazole is an atypical antipsychotic that acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptors. This combination has been studied for its efficacy in treatment-resistant depression, chronic or recurrent MDD, and has also shown benefit in elderly patients with hard-to-treat depression. The regimen typically involves starting with venlafaxine XR followed by the addition of aripiprazole after initial titration[1][2][3][4][5]. The combination may also be considered for other psychiatric conditions such as excoriation disorder when standard treatments are ineffective[7].

Brand names
Effexor XRAbilify
Other names
venlafaxine extended-release + aripiprazolevenlafaxine XR and aripiprazole combination
02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)DAT (Dopamine plasma membrane transport protein)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)ADRA1A (α1A)HTR7 (5-hydroxytryptamine receptor 7)DRD2 (Dopamine D2 Receptor)HTR2B (5-Hydroxytryptamine Receptor 2B)DRD3 (Dopamine receptor D3)

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