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venlafaxine XR + aripiprazole
- Development stage
- Phase 4
- 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 XR
- Other names
- venlafaxine extended-release + aripiprazolevenlafaxine XR and aripiprazole combination
02
Targets
ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)DRD4 (Dopamine D4 Receptor)DAT (Dopamine plasma membrane transport protein)HRH1 (Histamine H1 Receptor)NET (Norepinephrine Transporter)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR2C (5-hydroxytryptamine 2C receptor)HTR7 (5-hydroxytryptamine receptor 7)SERT (Sodium-dependent serotonin transporter)
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