What Is Tesofensine?
Tesofensine is a triple monoamine reuptake inhibitor originally developed by NeuroSearch for the treatment of Parkinson’s and Alzheimer’s disease, which later attracted significant research interest for its effects on metabolic and body weight regulation. It inhibits the reuptake of serotonin, dopamine, and norepinephrine, producing appetite-suppressing effects through central nervous system pathways distinct from GLP-1 receptor agonists.
Unlike injectable peptide compounds, tesofensine is an oral small molecule. This delivery advantage has made it a subject of ongoing research particularly among researchers studying central obesity mechanisms and CNS-mediated appetite regulation. The compound remains in active research and has not received regulatory approval for any indication as of 2026.
Tesofensine Mechanism of Action
Tesofensine works primarily through presynaptic inhibition of monoamine transporters:
- Serotonin reuptake inhibition: Elevates synaptic serotonin, contributing to appetite suppression and mood modulation in research models
- Dopamine reuptake inhibition: Increases dopaminergic tone, associated with reduced reward-driven feeding behavior in animal models
- Norepinephrine reuptake inhibition: Activates the sympathetic nervous system, contributing to increased energy expenditure and thermogenesis
This triple inhibition profile produces a combined anorectic and metabolic effect that researchers have studied in the context of both obesity and neurodegenerative disease models.
Tesofensine Research Data
A Phase 2 randomized controlled trial (Lancet, 2008) studied tesofensine in 203 obese participants over 24 weeks. Key published findings:
- At 0.5mg/day, participants achieved a mean weight loss of 12.8 kg (approximately 11.3% of body weight)
- At 1.0mg/day, mean weight loss was 14.1 kg over 24 weeks
- All active treatment arms significantly outperformed placebo (1.0 kg loss)
- Favorable changes in waist circumference and fasting lipid profiles were observed
Subsequent research has explored tesofensine in combination with other metabolic compounds, and its dose-response relationship continues to be investigated in preclinical models.
Tesofensine Dosage Reference
| Study Phase | Daily Oral Dose | Mean Weight Loss (24 Weeks) |
|---|---|---|
| Placebo | — | −1.0 kg |
| Low dose | 0.25mg | −6.7 kg |
| Mid dose | 0.5mg | −12.8 kg |
| High dose | 1.0mg | −14.1 kg |
Data from published Phase 2 trial. Provided for research reference only — not dosing guidance for human use.
Side Effects from Trial Data
Adverse events in published trials were primarily sympathomimetic and CNS-related:
- Dry mouth (most commonly reported)
- Nausea and constipation
- Heart rate increase (dose-dependent, ~7–8 bpm at 1mg)
- Elevated blood pressure at higher doses
- Insomnia and mood changes in some participants
Tesofensine vs. GLP-1 Agonists — Research Comparison
| Parameter | Tesofensine | Semaglutide (GLP-1) |
|---|---|---|
| Mechanism | Triple monoamine reuptake inhibition | GLP-1 receptor agonism |
| Route | Oral | Subcutaneous injection |
| Primary site of action | CNS (appetite/reward) | Peripheral + CNS |
| Thermogenic effect | Yes (NE pathway) | Indirect |
| Regulatory status (2026) | Research only | Approved (Ozempic/Wegovy) |
Where to Buy Tesofensine for Research
Researchers sourcing tesofensine should look for suppliers providing documented purity testing and identity verification. Essential supplier criteria:
- HPLC purity documentation (≥99% preferred)
- Mass spectrometry confirmation of compound identity
- Independent third-party laboratory COA
- Clear research-use-only documentation
Core Power Peptides supplies Tesofensine (KLOW) 80mg at ≥99% purity, third-party tested with COA available on request. For research and laboratory use only.
Research Disclaimer: All content on this page is for educational and scientific reference purposes only. Tesofensine is not approved for human use. This product is sold strictly for in vitro research and laboratory use only. Not for human consumption. Not medical advice.