Bupropion/dextromethorphan

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Bupropion/dextromethorphan
Bupropion.svg
Bupropion
Dextromethorphan.svg
Dextromethorphan
Combination of
BupropionNorepinephrine reuptake inhibitor and nicotinic acetylcholine receptor antagonist
DextromethorphanSigma-1 receptor agonist, NMDA receptor antagonist, serotonin-norepinephrine reuptake inhibitor
Clinical data
Other namesAXS-05; Bupropion/DXM
Routes of
administration		Oral
Legal status
Legal status
  • US: Investigational New Drug
Identifiers
CAS Number

Bupropion/dextromethorphan (developmental code name AXS-05) is a combination of bupropion and dextromethorphan (DXM) which is under development by Axsome Therapeutics for the treatment of treatment-resistant major depressive disorder (MDD), agitation in Alzheimer's disease, and smoking withdrawal.[1][2][3] Bupropion is a norepinephrine–dopamine reuptake inhibitor (NDRI) and nicotinic acetylcholine receptor (nAChR) antagonist, while dextromethorphan (DXM) is a σ1 receptor agonist, NMDA receptor antagonist, and serotonin–norepinephrine reuptake inhibitor (SNRI).[1] Bupropion, similarly to another drug known as quinidine, is also a potent inhibitor of CYP2D6.[4] This is the major enzyme responsible for metabolism of DXM—specifically into its active metabolite dextrorphan (DXO)—and by inhibiting it, bupropion increases DXM exposure and reduces the ratio of DXM to DXO in the body.[4][5][6][7] As of August 2021, bupropion/dextromethorphan is in pre-registration for depression, phase III clinical trials for agitation, and phase II trials for smoking withdrawal.[1]

See also[]

  • Bupropion/naltrexone
  • Dextromethorphan/quinidine
  • List of investigational antidepressants § Combinations

References[]

  1. ^ a b c "Bupropion/dextromethorphan - Axsome Therapeutics". Adis Insight. Springer Nature Switzerland AG.
  2. ^ Wilkinson ST, Sanacora G (February 2019). "A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems". Drug Discovery Today. 24 (2): 606–615. doi:10.1016/j.drudis.2018.11.007. PMC 6397075. PMID 30447328.
  3. ^ "Axsome depression drug meets late-stage study goal, shares soar 56%". Reuters. 16 December 2019 – via www.reuters.com.
  4. ^ a b Jefferson JW, Pradko JF, Muir KT (November 2005). "Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations". Clin Ther. 27 (11): 1685–95. doi:10.1016/j.clinthera.2005.11.011. PMID 16368442.
  5. ^ Stahl SM (October 2019). "Dextromethorphan/Bupropion: A Novel Oral NMDA (N-methyl-d-aspartate) Receptor Antagonist with Multimodal Activity". CNS Spectr. 24 (5): 461–466. doi:10.1017/S1092852919001470. PMID 31566163. S2CID 203607617.
  6. ^ Majeed A, Xiong J, Teopiz KM, Ng J, Ho R, Rosenblat JD, Phan L, Cao B, McIntyre RS (March 2021). "Efficacy of dextromethorphan for the treatment of depression: a systematic review of preclinical and clinical trials". Expert Opin Emerg Drugs. 26 (1): 63–74. doi:10.1080/14728214.2021.1898588. ISSN 1472-8214. PMID 33682569. S2CID 232141396.
  7. ^ Schoedel KA, Morrow SA, Sellers EM (2014). "Evaluating the safety and efficacy of dextromethorphan/quinidine in the treatment of pseudobulbar affect". Neuropsychiatr Dis Treat. 10: 1161–74. doi:10.2147/NDT.S30713. PMC 4079824. PMID 25061302.

External links[]



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