Tesofensine dosage

What Tesofensine is

Tesofensine is an investigational small-molecule inhibitor of noradrenaline, dopamine and serotonin reuptake, not a peptide, originally developed for Parkinson's and Alzheimer's disease and then studied for obesity. A 24-week phase 2 obesity trial reported dose-related body-weight change with increases in heart rate, and that trial report later received an expression of concern from The Lancet. It is not FDA-approved and is named as a prohibited stimulant by WADA; this entry is for research reference only.

Tesofensine inhibits presynaptic reuptake of noradrenaline, dopamine and serotonin ^1. Pharmacokinetics A population model from 320 patients with Alzheimer's disease described low apparent clearance and large apparent volumes of distribution, giving half-lives of about 234 hours for tesofensine and 374 hours for its main metabolite M1; creatinine clearance and sex had the largest effects on steady-state exposure… How it works →

Schedules by time period

study arms from registered trials, laid out week by week. Each bar is what the label states or what investigators gave participants; none is a recommendation.

Doses given in human trials

• In the phase 2 obesity trial (NCT00394667), after a 2-week run-in, 203 adults on an energy-restricted diet were randomized to tesofensine 0.25 mg, 0.5 mg or 1.0 mg, or placebo, once daily for 24 weeks ^1.
• In the four pooled Parkinson's and Alzheimer's trials, patients received oral tesofensine 0.125, 0.25, 0.5 or 1.0 mg or placebo once daily for 14 weeks without a weight-loss programme ^4.
• In ADVANS (NCT00148512), patients with advanced Parkinson's disease received tesofensine 0.125, 0.25, 0.5 or 1 mg or placebo tablets once daily for 14 weeks ^5.
• In the hypothalamic obesity trial, 21 adults were randomized to Tesomet (tesofensine 0.5 mg with metoprolol 50 mg) or placebo for 24 weeks with diet and lifestyle counselling ^6.
• In NCT02737891, 60 adults with type 2 diabetes received oral tesofensine 0.5 mg plus metoprolol 100 mg or matching placebo; outcomes were assessed from baseline to day 90 ^9.

How long did human studies run?

• Obesity phase 2: 24 weeks; neurology phase 2: 14 weeks ^1,4.
• Tesomet in hypothalamic obesity: 24 weeks ^6.

Who was excluded from the studies

• The obesity phase 2 trial enrolled adults with BMI 30 to 40 ^1.
• No label exists, so no formal contraindications are defined ^10.

Side effects reported in studies

• Dry mouth, nausea, constipation, hard stools, diarrhoea, insomnia
  Most common adverse events (rates not given in the abstract) · Phase 2 obesity trial, 24 weeks ¹
• Heart-rate increase
  +7.4 bpm with 0.5 mg vs placebo at 24 weeks · Phase 2 obesity trial ¹
• Heart-rate increase
  +2.1 to +6.8 bpm across doses vs -0.4 placebo · Pooled Parkinson's and Alzheimer's trials, 14 weeks ⁴
• Sleep disturbances (with metoprolol)
  50% vs 13% placebo · Hypothalamic obesity, 24 weeks ⁶
• Dry mouth (with metoprolol)
  43% vs 0% placebo · Hypothalamic obesity, 24 weeks ⁶
• Headache (with metoprolol)
  36% vs 0% placebo · Hypothalamic obesity, 24 weeks ⁶
• Gastrointestinal and neuropsychiatric adverse events
  More frequent than placebo, especially at higher doses · Advanced Parkinson's disease, 14 weeks ⁵

Tesofensine draw calculator

Pick the vial strength and the water added, enter an amount, and see the concentration, the units to draw and how many draws the vial holds. Arithmetic only.

1 · Vial strength

2 mg5 mg10 mg

2 · Water added

1 mL2 mL3 mL5 mL

3 · Amount per draw

mcgmg

4 · Syringe

30u50u100u

Your mix

10 mg + 2 mL water = 5 mg/mL

10 units holds 0.5 mg (500 mcg)

Draw toEnter an amount in step 3

U-100 syringe · 100 units = 1 mL

Computed from your inputs. Not a dose or a recommendation.

Compare water volumes for this vialShow

More water = lower concentration = a larger, easier-to-measure draw. Tap a row to use it.

Water	mg/mL	Draw
0.5 mL	20	—
1 mL	10	—
1.5 mL	6.667	—
2 mL	5	—
2.5 mL	4	—
3 mL	3.333	—
5 mL	2	—

Supplies and handling

• Lyophilized vial
  Sealed vial with the freeze-dried cake. Check the label, lot and the certificate of analysis before opening.
• Sterile diluent
  The diluent named on the product documentation. Bacteriostatic water contains benzyl alcohol; sterile water does not.
• Graduated syringes
  Sized to the volume being measured. U-100 insulin syringes are graduated in units where 100 units = 1 mL.
• Alcohol prep pads
  For wiping vial stoppers before each puncture.
• Nitrile gloves
  Clean gloves for aseptic handling.
• Sharps container
  Puncture-resistant container for used needles.

Storage

No approved-product storage instructions exist. Research material should be handled according to the supplier's documentation.

• Lyophilized (unmixed) vials: typically stored cold and dry, away from light, as the documentation directs. Many are stable longer frozen.
• Reconstituted vials: typically refrigerated (about 2–8 °C), protected from light and not frozen.
• Bacteriostatic water contains benzyl alcohol, which inhibits bacterial growth in multi-use vials; sterile water has no preservative.

Handling mistakes and troubleshooting

Added the wrong volume of diluent

The concentration changes, not the amount of compound in the vial. Recalculate with the volume actually added and relabel the vial.

Shook the vial and it foamed

Let it settle in the refrigerator. Foam is a sign of agitation; some peptides aggregate when shaken. Note it on the label.

The solution is cloudy or has particles

Do not use it. Cloudiness can indicate incomplete dissolution, contamination or degradation. Record the lot and contact the supplier with the certificate of analysis.

The powder cake looks melted or shrunken before reconstitution

This can indicate the vial was exposed to heat or moisture. Record the lot and condition on arrival.

Liquid sprayed back when the needle was removed

Pressure built up in the vial. Withdraw a small volume of air while adding diluent to keep pressure neutral.

Regulatory status

Status

Not approved by the FDA; an openFDA Drugs@FDA query returned no application record ^10. Phase 2 trials have been completed and registered on ClinicalTrials.gov, including Tesomet trials with posted results ^9. No phase 3 results or national approvals were confirmed in the allowed sources reviewed.

United States (FDA)

Not approved; an openFDA Drugs@FDA query for tesofensine returned no application record ^10. Tesofensine does not appear in any category of FDA's May 14, 2026 503A bulk drug substances list ^11.

Sport (WADA)

Prohibited in competition. Tesofensine is named in section S6.B, specified stimulants, of the WADA 2026 Prohibited List ^13.

Status varies by country and changes over time. How we describe regulatory status.

Tesofensine compared with related compounds

Frequently asked questions

References

1. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial Lancet. 2008
2. 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 Lancet. 2013
3. Under-reporting of adverse effects of tesofensine Lancet. 2013
4. Weight loss produced by tesofensine in patients with Parkinson's or Alzheimer's disease Obesity (Silver Spring). 2008
5. Tesofensine (NS 2330), a monoamine reuptake inhibitor, in patients with advanced Parkinson disease and motor fluctuations: the ADVANS Study Arch Neurol. 2008
6. Randomized controlled trial of Tesomet for weight loss in hypothalamic obesity Eur J Endocrinol. 2022
7. Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users Clin Pharmacol Ther. 2010
8. Population pharmacokinetic modelling of NS2330 (tesofensine) and its major metabolite in patients with Alzheimer's disease Br J Clin Pharmacol. 2007
9. Safety and Efficacy Study of Tesofensine/Metoprolol Treatment in Subjects With Type 2 Diabetes Mellitus (NCT02737891), registry record with posted results ClinicalTrials.gov. 2017
10. Drugs@FDA application data queried through openFDA for tesofensine (no matching application record returned on 23 October 2026) openFDA / Drugs@FDA. 2026
11. Bulk Drug Substances Nominated for Use in Compounding Under Section 503A of the FD&C Act (categories 1, 2 and 3; updated May 14, 2026) FDA. 2026
12. PubChem compound record for tesofensine (CID 11370864; CAS 195875-84-4) PubChem. 2026
13. International Standard: Prohibited List 2026 World Anti-Doping Agency. 2026