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Tesofensine

NS2330

2 min read · Updated July 27, 2026 · 7 references

Curated by PeptideInfo Wikilast reviewed how we verify

Explored forWeight management
In brief · TL;DR
Limited/early human data — not approved

Tesofensine is a monoamine-reuptake inhibitor with phase 2 obesity data; it is not FDA-approved, and the principal monotherapy publication carries an expression of concern.

Evidence: Only small/early human studies; not approved.

  • Human weight-loss signals come mainly from one phase 2 programme
  • The main publication has an expression of concern
  • Current development focuses on a tesofensine–metoprolol combination
↓ Read the full referenced entry below

Tesofensine is a monoamine-reuptake inhibitor with phase 2 obesity data; it is not FDA-approved, and the principal monotherapy publication carries an expression of concern.

Overview

Tesofensine (NS2330) is a synthetic monoamine-reuptake inhibitor investigated for obesity and earlier neurological programmes. Human efficacy signals exist, but the evidence is not equivalent to an approved medicine. The principal 2008 obesity publication later received an expression of concern.

Investigational, not approved

An orphan-drug designation for tesofensine plus metoprolol is not FDA marketing approval; FDA’s own record says the combination is not approved for that orphan indication.

Identity and chemistry

PropertyVerified value
PubChem CID11370864
Molecular formulaC17H23Cl2NO
Molecular weight328.3 g/mol
CAS number195875-84-4

These values describe tesofensine free base. Tesofensine citrate is a separate salt record with different formula and mass and must not be mixed into this identity.

Mechanism

Tesofensine inhibits presynaptic reuptake of noradrenaline, dopamine and serotonin. That pharmacology can influence appetite and autonomic variables, but a plausible mechanism does not establish a favourable clinical risk–benefit balance.

Phase 2 monotherapy evidence

NCT00394667 randomised 203 adults with obesity to placebo or three once-daily tesofensine doses alongside an energy-restricted diet for 24 weeks. The publication reported greater mean weight loss than placebo and 161 participants completed the study. Common adverse effects included dry mouth, nausea, constipation, diarrhoea and insomnia; heart rate increased by 7.4 beats/min in the 0.5 mg group. The publication’s later expression of concern must remain attached to any interpretation.

Combination development

Later work has focused on Tesomet, a fixed combination of tesofensine and metoprolol. A small randomised trial in 21 adults with hypothalamic obesity reported weight-loss signals and included anxiety, sleep disturbance, dry mouth and headache among safety findings. NCT05147415 studies several Tesomet doses. Evidence for the combination does not automatically validate tesofensine monotherapy.

Regulatory context

FDA granted orphan designation in 2021 to the fixed tesofensine–metoprolol combination for hypothalamic obesity. The same FDA record explicitly states that it is not FDA-approved for the orphan indication. Designation supports development; it is not evidence of marketing authorisation.

Safety and dosing

The monoamine mechanism and observed heart-rate and neuropsychiatric findings make cardiovascular, psychiatric and interaction assessment central to development. Trial doses document what researchers tested; they are not an approved regimen.

No established clinical dose

This page does not convert phase 2 or combination-study doses into treatment advice.

Evidence conclusion

Tesofensine has genuine human trial data, but the monotherapy evidence is limited, its central publication carries an integrity warning, and current development uses a combination product. Confirmation in rigorous trials and regulatory review remain necessary.

References

  1. 1.
    PubChem Compound Summary: Tesofensine (CID 11370864) source
  2. 2.
    ClinicalTrials.gov: NCT00394667 source
  3. 3.
    Phase 2 obesity trial publication source
  4. 4.
    Lancet expression of concern source
  5. 5.
    Tesomet hypothalamic-obesity randomized trial source
  6. 6.
    ClinicalTrials.gov: NCT05147415 Tesomet source
  7. 7.
    FDA orphan designation record: tesofensine plus metoprolol source

Frequently asked questions

What is Tesofensine?
Tesofensine is a monoamine-reuptake inhibitor with phase 2 obesity data; it is not FDA-approved, and the principal monotherapy publication carries an expression of concern.
Is Tesofensine approved as a medicine, and where?
No. Tesofensine is not an approved medicine anywhere. It is handled as a research chemical, with only limited or early-stage human data.
What is Tesofensine studied for?
Tesofensine is most often discussed in the context of weight management. Being studied for an area does not mean it is proven or approved for it.
Does Tesofensine have human clinical trials?
Only to a limited extent. A small number of early-stage human studies exist, but the evidence is preliminary and Tesofensine is not approved.

Educational disclaimer. This article summarizes published research for informational purposes and is not medical advice. Tesofensine is a research chemical not approved for human use. Consult a qualified healthcare professional before making health decisions.

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