A triple monoamine reuptake inhibitor with potent appetite suppression and weight loss effects.
Tesofensine (NS2330) is a triple monoamine reuptake inhibitor originally developed by NeuroSearch for the treatment of Parkinson’s and Alzheimer’s disease, where it showed cognitive benefits but was ultimately repurposed for obesity after Phase II trials demonstrated remarkable weight loss. In a landmark 2008 Phase II trial published in The Lancet, Tesofensine at 0.5 mg produced 10.6% body weight reduction over 24 weeks — the highest weight loss ever reported for an oral weight loss drug at that time, significantly exceeding the efficacy of then-available obesity medications. Tesofensine works through a fundamentally different mechanism than GLP-1 agonists: rather than acting on gut hormones, it directly enhances central monoamine signaling to reduce appetite and increase metabolic rate. The compound is currently in Phase III trials for obesity in some regions and has been used in research settings for its combination of weight loss and cognitive enhancement properties.
* Benefits based on preclinical/animal research unless otherwise noted.
“A triple monoamine reuptake inhibitor with potent appetite suppression and weight loss effects.”
Tesofensine inhibits the reuptake transporters for dopamine (DAT), serotonin (SERT), and norepinephrine (NET) simultaneously, increasing the synaptic concentrations of all three monoamines in the central nervous system. This triple monoamine reuptake inhibition produces several metabolic effects: dopamine enhancement in the hypothalamus reduces appetite through reward pathway modulation; norepinephrine enhancement activates the sympathetic nervous system to increase metabolic rate and thermogenesis; serotonin enhancement contributes to satiety signaling and mood stabilization. Unlike amphetamines, which cause monoamine release, Tesofensine only blocks reuptake, producing a more controlled and sustained effect. The compound also has some cholinesterase inhibitory activity, which may contribute to its cognitive enhancement effects and explains its original development for neurodegenerative diseases. Morning dosing is essential as the stimulant and noradrenergic effects will significantly disrupt sleep if taken later in the day.
Protocol Notes: Morning dosing only — stimulant effects will disrupt sleep. Start with 0.25 mg to assess tolerance. Monitor heart rate and blood pressure.
Store at room temperature, away from light and moisture.
When sourcing Tesofensine (Capsule) for research purposes, the following quality benchmarks should be verified before use.
Store at room temperature, away from light and moisture.
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Moderate Evidence — Multiple animal studies and/or early human trials. Reasonable confidence in mechanism, but human data is limited.
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