Drug intelligence / Profile preview

naltrexone + aripiprazole

Development stage
Preclinical
Lead developer
Endo International
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Naltrexone + aripiprazole is a combination therapy being investigated primarily for alcohol dependence treatment. Naltrexone is an opioid antagonist that blocks opioid receptors, reducing alcohol cravings and rewarding effects of alcohol. It's available as oral tablets and monthly injections (Vivitrol). Aripiprazole is an atypical antipsychotic that functions as a dopamine/serotonin system stabilizer, acting as a partial dopamine agonist that blocks dopamine at higher concentrations and augments it at lower concentrations. This combination targets multiple neurotransmitter systems involved in addiction, potentially enhancing efficacy compared to either medication alone.

02

Targets

DRD2 (Dopamine D2 Receptor)KOR (Kappa opioid receptor)ADRA1A (α1A)MOR (Mu opioid receptor)DRD3 (Dopamine receptor D3)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))DOR (Opioid Receptor Delta 1)HTR2A (Serotonin receptor 5-HT2A)

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