Tesofensine Capsules
30 hard gelatin capsules labelled 500 mcg each of NS2330, a small-molecule triple monoamine reuptake inhibitor and not a peptide. Each lot is tested in the manufacturer’s own laboratory.
| Compound | Tesofensine (NS-2330), phenyltropane; small molecule |
|---|---|
| CAS number | 195875-84-4 |
| Molecular formula | C17H23Cl2NO |
| Form | Hard gelatin capsules containing the active substance blended with microcrystalline cellulose, packed in a sealed bottle |
| Storage, sealed | Store at room temperature (15–25 °C) in the tightly closed original container, dry and protected from light |
| Format | Capsules in a sealed bottle |
Sizes and lots
- 500 mcg × 30 · 1 bottle — $198.99
- 500 mcg × 30 · Kit of 10 — $1769.02
Tesofensine, development code NS2330, is a small-molecule inhibitor of the reuptake of noradrenaline, dopamine and serotonin. It is a phenyltropane of about 328 Da, not a peptide. This listing is a bottle of 30 hard gelatin capsules, each labelled 500 mcg of tesofensine in a microcrystalline cellulose fill. NeuroSearch developed the compound for Parkinson's and Alzheimer's disease, and its human literature is a set of randomised trials in those diseases followed by one phase II trial in obesity.
What is in each capsule
Each capsule is labelled to contain 500 mcg of tesofensine, blended with microcrystalline cellulose inside a gelatin shell, and the bottle holds 30. The safety data sheet identifies the active ingredient by the free-base formula, C17H23Cl2NO, and CAS number 195875-84-4, and classifies neither tesofensine nor the filler and shell as hazardous. The bottle is stored tightly closed in its original container at 15 to 25 °C, dry and away from light.
With this compound the form behind a label figure matters. Tesofensine is also sold as a tartrate salt, which the tesofensine guide puts at 478.36 g/mol against 328.3 g/mol for the free base, so 500 mcg of the tartrate would contain only about 343 mcg of tesofensine itself. Any conversion of the label amount into moles should start from the form given on the safety data sheet.
What the research covers
Mechanism and the Parkinson's trial
Tesofensine inhibits reuptake of dopamine, serotonin and noradrenaline, and it was tried in Parkinson's disease because dopamine reuptake inhibitors had reversed parkinsonian signs in lesioned marmosets1. Hauser and colleagues randomly assigned 261 people with early Parkinson's disease, none on dopaminergic treatment, to one of three tesofensine arms or placebo for 14 weeks1. No arm beat placebo on the total disease rating scale at week 14; the highest arm was ahead at week 6, but the difference did not last1. Constipation, insomnia and dry mouth were the commonest adverse events, and lower body weight and a raised heart rate were common in the highest arm1.
Body weight as an end point
That observation led to a pooled analysis of four randomised, double-blind 14-week trials, two in Parkinson's and two in Alzheimer's disease, with 740 people on tesofensine, 228 on placebo and no weight-management program2. Body weight fell more with tesofensine than with placebo and the effect grew with the amount given, while heart rate rose by up to 6.8 beats per minute and blood pressure did not change2. A phase II randomised, placebo-controlled trial in 203 adults with obesity followed, with everyone on an energy-restricted diet and percentage change in body weight over 24 weeks as the primary outcome3. Every tesofensine arm lost more weight than diet plus placebo; dry mouth, nausea, constipation, diarrhoea and insomnia were the commonest adverse events, and heart rate rose by 7.4 beats per minute in the middle arm3. The authors wrote that the findings needed confirmation in phase III trials3.
What is not established
Frequently asked questions
Is tesofensine a peptide?
No. Tesofensine is a phenyltropane, a small molecule of about 328 Da with no amino acids and no peptide bonds. People search for it as a peptide because peptide suppliers sell it, but it acts on the transporters for noradrenaline, dopamine and serotonin, not on any peptide receptor.
Is the 500 mcg on the label free base or tartrate?
The safety data sheet identifies the active ingredient by the free-base formula and CAS number. The question matters because the tartrate salt is about 1.46 times heavier, so a 500 mcg label figure for the salt would mean only about 343 mcg of tesofensine.
How should the bottle be stored?
Tightly closed in its original container at 15 to 25 °C, dry and protected from light. Tesofensine is a stable small molecule, so the capsules need no refrigeration, freezing or other cold-chain handling.
Is tesofensine an approved drug?
No. It has been through phase II trials but is not approved by the FDA, the European Medicines Agency or Mexico's regulator. These capsules are sold for laboratory research only. They are not a supplement and must not be swallowed by, or given to, people or animals.
References
- Hauser RA, Salin L, Juhel N, et al. Randomized trial of the triple monoamine reuptake inhibitor NS 2330 (tesofensine) in early Parkinson's disease. Mov Disord. 2007;22(3):359-65. DOI · PubMed
- Astrup A, Meier DH, Mikkelsen BO, et al. Weight loss produced by tesofensine in patients with Parkinson's or Alzheimer's disease. Obesity (Silver Spring). 2008;16(6):1363-9. DOI · PubMed
- Astrup A, Madsbad S, Breum L, 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(9653):1906-1913. DOI · PubMed
For laboratory research use only. Not for human or veterinary consumption. Products have not been evaluated by the U.S. Food and Drug Administration and are not intended to diagnose, treat, cure or prevent any disease.