Drug intelligence / Profile preview

aripiprazole + desvenlafaxine

Development stage
Phase 4
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Aripiprazole + desvenlafaxine is a combination of two pharmaceutical drugs used primarily in the management of psychiatric disorders such as major depressive disorder and treatment-resistant depression. 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 unique mechanism allows it to modulate dopaminergic activity depending on endogenous dopamine levels, providing both antipsychotic and antidepressant effects[2][6]. Desvenlafaxine is a selective serotonin and norepinephrine reuptake inhibitor (SNRI) that increases the levels of these neurotransmitters in the central nervous system by inhibiting their reuptake; it has higher affinity for serotonin transporters than for norepinephrine transporters[4][5]. The combination may be considered in cases where monotherapy with antidepressants is insufficient. However, combining these agents can increase risks such as dizziness, drowsiness, confusion, impairment in thinking or motor coordination, and potentially serotonin syndrome[1][2].

02

Targets

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

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