Bupropion/dextromethorphan (developmental code name AXS-05) is a combination drug of bupropion (Wellbutrin), a norepinephrine-dopamine reuptake inhibitor (NDRI) and nicotinic acetylcholine receptor (nAChR) antagonist, and dextromethorphan (DXM), a sigma-1 receptor agonist, NMDA receptor antagonist, and serotonin-norepinephrine reuptake inhibitor (SNRI), which is under development by Axsome Therapeutics for the treatment of treatment- resistant major depressive disorder (MDD) and agitation in Alzheimer's disease.[1][2][3] Via inhibition of CYP2D6, similarly to quinidine, bupropion slows the metabolism of DXM and thereby increases its levels. As of 2017, the combination is in phase III clinical trials for the aforementioned indications.[1]
抑郁症的发病机制至今仍未完全阐明。传统的抗抑郁药是基于单胺递质假说而开发的。近年来，除了单胺类外，谷氨酸系统、HPA轴等一些新的抑郁症治疗靶标逐渐成为研究
热点
AXS-05这个有点奇葩，一堆东西的混合，拭目以待看看FDA能批吗 08/22/2021
Bupropion/dextromethorphan (developmental code name AXS-05) is a combination drug of bupropion (Wellbutrin), a norepinephrine-dopamine reuptake
inhibitor (NDRI) and nicotinic acetylcholine receptor (nAChR) antagonist,
and dextromethorphan (DXM), a sigma-1 receptor agonist, NMDA receptor
antagonist, and serotonin-norepinephrine reuptake inhibitor (SNRI), which is under development by Axsome Therapeutics for the treatment of treatment-
resistant major depressive disorder (MDD) and agitation in Alzheimer's
disease.[1][2][3] Via inhibition of CYP2D6, similarly to quinidine,
bupropion slows the metabolism of DXM and thereby increases its levels. As
of 2017, the combination is in phase III clinical trials for the
aforementioned indications.[1]