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AXS-05

Axsome Therapeutics, Inc. · FDA-approved active Small molecule

AXS-05 is a combination of dextromethorphan and bupropion that enhances serotonergic and noradrenergic neurotransmission while modulating NMDA receptor activity.

AXS-05 is a combination of dextromethorphan and bupropion that enhances serotonergic and noradrenergic neurotransmission while modulating NMDA receptor activity. Used for Major depressive disorder.

At a glance

Generic nameAXS-05
Also known asBupropion/dextromethorphan
SponsorAxsome Therapeutics, Inc.
Drug classCombination antidepressant (NMDA antagonist + norepinephrine-dopamine reuptake inhibitor)
TargetSigma-1 receptor, NMDA receptor, norepinephrine transporter, dopamine transporter
ModalitySmall molecule
Therapeutic areaPsychiatry/Neurology
PhaseFDA-approved

Mechanism of action

The drug combines dextromethorphan (a sigma-1 receptor agonist and NMDA antagonist) with bupropion (a norepinephrine-dopamine reuptake inhibitor). This combination is designed to provide rapid-acting antidepressant effects through multiple mechanisms: bupropion increases norepinephrine and dopamine levels, while dextromethorphan acts on sigma-1 receptors and NMDA receptors to enhance neuroplasticity and reduce depressive symptoms more quickly than traditional antidepressants.

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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