Educational Guide

What Is Tesofensine?

A neutral, research-backed overview of Tesofensine — its mechanism of action, published evidence, and current safety profile. This guide is designed for educational purposes and does not constitute medical advice.

20 cited studies
Updated: 2026-05-27
Small Molecule

Overview

Tesofensine is classified as a small molecule peptide. Extreme fat loss and appetite suppression without GLP-1 side effects.

Triple monoamine reuptake inhibitor (inhibits reuptake of serotonin, noradrenaline, and dopamine). Originates as an Alzheimer's/Parkinson's drug but abandoned due to massive weight loss profiles.

Also known as: NS2330

Category

Small Molecule

Half-Life

216h

Route

Oral

FDA Status

Not Approved

How Does Tesofensine Work?

Triple monoamine reuptake inhibitor (inhibits reuptake of serotonin, noradrenaline, and dopamine). Originates as an Alzheimer's/Parkinson's drug but abandoned due to massive weight loss profiles.

At the molecular level, Tesofensine operates through pathways characteristic of the Small Molecule class, interacting with target receptors and downstream signaling cascades to produce its observed effects.

Published Research

The following studies are indexed from PubMed and peer-reviewed journals:

[1]Tesofensine induces profound weight loss

Phase 2 Lancet study showing 12.8 kg (10.6%) weight loss over 24 weeks at 1mg dose.

Evidence: strong

[2]Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13.

A study published in Expert opinion on investigational drugs investigating the effects and mechanisms.

Evidence: moderate

[3]Weight loss produced by tesofensine in patients with Parkinson's or Alzheimer's disease.

A study published in Obesity (Silver Spring, Md.) investigating the effects and mechanisms.

Evidence: moderate

[4]Tesofensine and weight loss.

A study published in Lancet (London, England) investigating the effects and mechanisms.

Evidence: preclinical

[5]A quantitative enterohepatic circulation model: development and evaluation with tesofensine and meloxicam.

A study published in Clinical pharmacokinetics investigating the effects and mechanisms.

Evidence: preclinical

[6]Expression of concern--effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial.

A study published in Lancet (London, England) investigating the effects and mechanisms.

Evidence: moderate

[7]Tesofensine, a novel antiobesity drug, silences GABAergic hypothalamic neurons.

A study published in PloS one investigating the effects and mechanisms.

Evidence: preclinical

[8]Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial.

A study published in Lancet (London, England) investigating the effects and mechanisms.

Evidence: moderate

[9]New and emerging drug molecules against obesity.

A study published in Journal of cardiovascular pharmacology and therapeutics investigating the effects and mechanisms.

Evidence: preclinical

[10]Quantitative pharmacology approach in Alzheimer's disease: efficacy modeling of early clinical data to predict clinical outcome of tesofensine.

A study published in The AAPS journal investigating the effects and mechanisms.

Evidence: moderate

[11]Structural basis for pharmacotherapeutic action of triple reuptake inhibitors.

A study published in Nature communications investigating the effects and mechanisms.

Evidence: preclinical

[12]Future Pharmacotherapy for Obesity: New Anti-obesity Drugs on the Horizon.

A study published in Current obesity reports investigating the effects and mechanisms.

Evidence: preclinical

[13]Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine.

A study published in European journal of pharmacology investigating the effects and mechanisms.

Evidence: preclinical

[14]Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users.

A study published in Clinical pharmacology and therapeutics investigating the effects and mechanisms.

Evidence: preclinical

[15]Contribution of the active metabolite M1 to the pharmacological activity of tesofensine in vivo: a pharmacokinetic-pharmacodynamic modelling approach.

A study published in British journal of pharmacology investigating the effects and mechanisms.

Evidence: preclinical

[16][The effect of tesofensine on body weight and body composition in obese subjects--secondary publication].

A study published in Ugeskrift for laeger investigating the effects and mechanisms.

Evidence: preclinical

[17]Tesofensine induces appetite suppression and weight loss with reversal of low forebrain dopamine levels in the diet-induced obese rat.

A study published in Pharmacology, biochemistry, and behavior investigating the effects and mechanisms.

Evidence: preclinical

[18]Anti-hypertensive treatment preserves appetite suppression while preventing cardiovascular adverse effects of tesofensine in rats.

A study published in Obesity (Silver Spring, Md.) investigating the effects and mechanisms.

Evidence: preclinical

[19]Population pharmacokinetic modelling of NS2330 (tesofensine) and its major metabolite in patients with Alzheimer's disease.

A study published in British journal of clinical pharmacology investigating the effects and mechanisms.

Evidence: moderate

[20]Anti-obesity drugs: a review about their effects and their safety.

A study published in Expert opinion on drug safety investigating the effects and mechanisms.

Evidence: moderate

Safety Profile

Research-only. Potent CNS stimulant. Can cause insomnia, elevated heart rate, and dry mouth. Half-life is extremely long, leading to accumulation in the system.

Side EffectIncidenceSeverity
Insomnia~15% of usersmoderate
Dry Mouth~20% of usersmild
Elevated Heart Rate~12% of usersmoderate

Sourcing Tesofensine for Research

If you're looking to source Tesofensine for laboratory research, our vendor directory compares pricing, purity testing, and COA verification from independently vetted suppliers.

* Research vendor — verify your regional regulations before purchase.

Full Research Profile

Tesofensine — dosing, interactions, timelines & more

Comprehensive compound profile with sourcing information, stacking synergies, and outcome timelines.

Last updated: 2026-05-27 · Educational Hub · Editorial Standards