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Drug intelligence / Profile preview
dextromethorphan + bupropion
- Development stage
- Approved
- Lead developer
- Axsome Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Dextromethorphan + bupropion is an oral, fixed-dose extended-release small-molecule combination marketed in the United States as **Auvelity** and developed by Axsome as AXS-05. Dextromethorphan is an uncompetitive N-methyl-D-aspartate receptor antagonist and sigma-1 receptor agonist, while bupropion inhibits cytochrome P450 2D6 to increase dextromethorphan exposure and also inhibits norepinephrine and dopamine reuptake. Auvelity is approved for major depressive disorder in adults and for agitation associated with dementia due to Alzheimer's disease. ([axsome.com](https://www.axsome.com/wp-content/uploads/2024/11/auvelity-prescribing-information.pdf))
- Brand names
- Auvelity
- Other names
- dextromethorphan and bupropiondextromethorphan hydrobromide + bupropion hydrochloridedextromethorphan-bupropiondextromethorphan/bupropion
02
Targets
CYP2D6 (Cytochrome P450 2D6)DAT (Dopamine plasma membrane transport protein)NMDAR (Glutamate receptor ionotropic, NMDA)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)α4β2 nAChR (Nicotinic acetylcholine receptor alpha4 beta2 subtype)MOR (Mu opioid receptor)
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