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Esreboxetine is a highly selective and potent norepinephrine reuptake inhibitor (NRI), specifically the (S,S)-(+)-enantiomer of reboxetine. It acts by inhibiting the sodium-dependent noradrenaline transporter (SLC6A2), thereby increasing norepinephrine levels in the synaptic cleft and enhancing noradrenergic neurotransmission. Esreboxetine was originally developed by Pfizer for neuropathic pain and fibromyalgia but was discontinued after failing to show significant benefit over existing treatments. More recently, Axsome Therapeutics has been developing esreboxetine under the code name AXS-14 as an investigational oral therapy for fibromyalgia, with ongoing Phase III clinical trials as of early 2025[1][4][5][7]. The drug is administered orally.
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