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Aripiprazole (BMS-337039)

Otsuka Pharmaceutical Development & Commercialization, Inc. · Phase 3 active Small molecule

Aripiprazole is a partial agonist at dopamine D2 and serotonin 5-HT1A receptors that modulates dopaminergic and serotonergic neurotransmission in the brain.

Aripiprazole is a partial agonist at dopamine D2 and serotonin 5-HT1A receptors that modulates dopaminergic and serotonergic neurotransmission in the brain. Used for Schizophrenia, Bipolar I disorder (acute manic and mixed episodes), Major depressive disorder (adjunctive treatment).

At a glance

Generic nameAripiprazole (BMS-337039)
SponsorOtsuka Pharmaceutical Development & Commercialization, Inc.
Drug classAtypical antipsychotic
TargetDopamine D2 receptor (partial agonist); Serotonin 5-HT1A receptor (partial agonist)
ModalitySmall molecule
Therapeutic areaPsychiatry
PhasePhase 3

Mechanism of action

Aripiprazole acts as a partial agonist rather than a full antagonist, meaning it can both activate and inhibit dopamine D2 receptors depending on baseline dopamine levels, providing a stabilizing effect on dopaminergic signaling. This unique mechanism, combined with 5-HT1A partial agonism, reduces both positive and negative symptoms of psychosis while potentially causing fewer extrapyramidal side effects than typical antipsychotics. The partial agonist activity allows for dopaminergic tone adjustment rather than complete blockade.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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