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Drug intelligence / Profile preview
aripiprazole + fluvoxamine
- Development stage
- Preclinical
- Lead developer
- Otsuka Holdings
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of the atypical antipsychotic aripiprazole and the selective serotonin reuptake inhibitor (SSRI) fluvoxamine. Aripiprazole acts as a partial agonist at dopamine D2 receptors and serotonin 5-HT1A receptors, and an antagonist at 5-HT2A receptors. Fluvoxamine is an SSRI that also functions as a sigma-1 receptor agonist. This combination has been used to treat aripiprazole-induced akathisia, pathological gambling, and has been considered for Fragile X syndrome. The combination requires careful monitoring due to pharmacokinetic interactions, as fluvoxamine inhibits CYP3A4 enzymes that metabolize aripiprazole, potentially leading to increased aripiprazole blood levels and risk of side effects including hepatotoxicity.
02
Targets
DRD2 (Dopamine D2 Receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)
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