Tesofensine

also known as: NS2330

A triple-monoamine reuptake inhibitor (SNDRI) with Phase 2 anti-obesity data showing up to ~12% weight loss at 1.0 mg/day — development stalled over cardiovascular concerns; not a peptide and included here for cross-reference only.

A small-molecule serotonin, noradrenaline, and dopamine triple-reuptake inhibitor originally developed by NeuroSearch for Alzheimer's and Parkinson's disease; repurposed as an appetite suppressant after unexpectedly large weight loss was observed in early neurology trials, with a Phase 2 obesity program showing weight loss at the high end of the stimulant class but cardiovascular safety signals that blunted further development.

Mechanism of action

Blocks the presynaptic reuptake of serotonin, noradrenaline, and dopamine, producing central appetite suppression and increased resting metabolic rate analogous to stimulant-class anorectics but with a longer duration of action than classical agents like phentermine. The monoaminergic mechanism drives the cardiovascular side-effect profile — elevations in heart rate and blood pressure are the primary tolerability and safety limitation.

Primary uses

Research into obesity pharmacotherapy
Historical research in Alzheimer's and Parkinson's disease (deprioritized)

Typical dosing

0.25–1.0 mg daily (oral)

Phase 2 obesity trials used 0.25, 0.5, and 1.0 mg/day for 24 weeks. Not a community research-chemical target — sold online as a research reference compound only.

Regulatory status

Not FDA-approved. In 2023, a tesofensine formulation (Tesomet) was approved in Mexico (COFEPRIS) for obesity in a low-dose combination with metoprolol; approval in other regions has not followed. Western Phase 3 development has not advanced due to persistent concerns about blood pressure and heart rate elevation.

References

[pubmed] Astrup A, et al. "Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial." Lancet, 2008;372:1906-1913.
[pubmed] Sjödin A, et al. "The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men." Int J Obes, 2010;34:1634-1643.

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Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.