Drug intelligence / Profile preview

esbupropion

Development stage
Unknown
Lead developer
Axsome Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Esbupropion, also known as S-bupropion or S-BUP, is the S-enantiomer of the aminoketone antidepressant bupropion. It is being developed by Axsome Therapeutics primarily as a component of AXS-09, a fixed-dose combination therapy that pairs esbupropion with dextromethorphan. Esbupropion acts as a norepinephrine and dopamine reuptake inhibitor (NDRI) and is a potent inhibitor of the CYP2D6 enzyme. In the AXS-09 formulation, esbupropion serves a dual purpose: it provides independent antidepressant activity and pharmacokinetically enhances dextromethorphan by inhibiting its metabolism, thereby increasing its bioavailability and extending its half-life. This combination is being investigated for the treatment of central nervous system disorders, most notably treatment-resistant depression (TRD).

Other names
(S)-bupropiondexbupropion(+)-bupropion
02

Targets

CYP2D6 (Cytochrome P450 2D6)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)

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