Triple monoamine reuptake inhibitor

Tesofensine in Canada

Also known as NS2330 · NS 2330 · Tesomet (tesofensine + metoprolol)

Tesofensine is not a peptide. It is a small synthetic molecule — a tropane-based inhibitor of noradrenaline, dopamine and serotonin reuptake — that a Danish neuroscience company developed for Parkinson's and Alzheimer's disease, failed with, and then repurposed when trial participants lost weight. Its 2008 Phase 2 obesity trial in The Lancet reported placebo-subtracted weight loss of about 10% at the highest dose, roughly twice what the approved drugs of that era achieved, alongside a rise in heart rate and blood pressure that has shaped everything since. Canada Peptides carries research-grade tesofensine, priced and shipped in CAD for laboratory and research use only. It has no approval in Canada, the United States or Europe.

Quick facts

Class: Synthetic small molecule; triple monoamine reuptake inhibitor (NET, DAT, SERT)
Structure: Tropane (8-azabicyclo[3.2.1]octane) scaffold · C17H23Cl2NO · ~328 Da · not a peptide
Half-life: Roughly 9 days (about 220 hours) for the parent; longer for the active metabolite NS2360; steady state takes weeks
Route in research: Oral, once daily, in every published human trial
Cadence in research: Once daily for 14–24 weeks in the obesity trials
Storage: Dry powder: cool, dry, dark, tightly sealed; stock solutions in organic solvent frozen in aliquots
Status in Canada

Tesofensine FAQ

Is Tesofensine for sale in Canada?

Yes. Research-grade tesofensine is available in Canada from Canada Peptides, priced and shipped in CAD. It is supplied strictly for laboratory and research use, not for human consumption, and it has no Health Canada approval.

What is tesofensine?

Tesofensine is a small-molecule triple monoamine reuptake inhibitor — it blocks the transporters for noradrenaline, dopamine and serotonin. It was developed by NeuroSearch for Parkinson's and Alzheimer's disease, failed in those trials, and was repurposed for obesity after participants lost weight.

Is tesofensine a peptide?

No. It is a synthetic tropane-based small molecule of about 328 daltons, taken orally in every human trial. It is stocked in the metabolic category because of what it was studied for, and it handles like a small molecule, not like a lyophilised peptide.

What did the tesofensine trials show?

The 2008 Phase 2 trial in The Lancet reported placebo-subtracted weight loss of about 4.5%, 9.2% and 10.6% at 0.25, 0.5 and 1.0 mg daily over 24 weeks. The sponsor has since reported positive Phase 3 results from a program in Mexico. There is no long-term outcome data.

What is the half-life of tesofensine?

About nine days — roughly 220 hours — for the parent compound, and longer for its active metabolite NS2360. Steady state takes several weeks to reach and effects persist for weeks after the last dose.

How was tesofensine dosed in studies?

Orally, once daily, at 0.25, 0.5 or 1.0 mg in the obesity Phase 2 trial and 0.25 or 0.5 mg in Phase 3. The 1.0 mg dose was dropped over blood-pressure effects. Tesofensine is unapproved in Canada; these are facts about clinical trials, not recommendations, and the material sold here is for research use only.

What side effects does tesofensine research report?

Dry mouth, nausea, constipation, insomnia and mood changes, all dose-related, plus a consistent rise in heart rate of around seven to eight beats per minute and, at 1.0 mg, a rise in blood pressure. No long-term cardiovascular-outcome data exists, which is the largest gap in its safety record.

Is tesofensine legal in Canada?

Tesofensine is not a controlled substance in Canada, but it has no Health Canada approval for human use and no DIN. It may be sold for laboratory research, which is how it is sold here. It is not named on the WADA list but may fall under the S6 stimulant catch-all.

Tesofensine in Canada

Quick facts

Tesofensine — for sale in Canada

What is Tesofensine?

Evidence at a glance

Pharmacology

Identity and chemistry

Storage and stability

Research indications

Research protocols

Interactions and stacking in research

Reconstitution and handling

Side effects and safety signals

Regulatory status in Canada

Further reading

Tesofensine FAQ

Research references