Drug intelligence / Profile preview

Lithium + aripiprazole

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

Overview

Lithium + aripiprazole is a combination therapy used primarily in the management of acute manic and mixed episodes associated with Bipolar I Disorder. Lithium is a classic mood stabilizer that modulates neurotransmitter activity and second messenger systems, while aripiprazole is an atypical antipsychotic that acts as a partial agonist at dopamine D2 receptors and serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptors. The combination has been shown to be effective and generally well-tolerated for patients who have not responded adequately to monotherapy with either agent. Aripiprazole’s mechanism involves dopamine system stabilization via partial agonism at presynaptic D2 autoreceptors (reducing dopamine release) and antagonism at postsynaptic D2 receptors[6]. This dual action may contribute to its efficacy in mood stabilization when combined with lithium[4][5]. The combination is FDA-approved for adjunctive use in acute treatment of manic or mixed episodes of Bipolar I Disorder[5].

02

Targets

DRD4 (Dopamine D4 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2C (5-hydroxytryptamine 2C receptor)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)IMPA1 (Inositol Monophosphatase)HTR7 (5-hydroxytryptamine receptor 7)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)

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