Incretin & metabolic research compounds

Tesofensine

Also known as NS2330

A triple monoamine (noradrenaline, dopamine, serotonin) reuptake inhibitor that reduced weight in a phase 2 obesity trial.

Research referenceNot stocked4 PubMed citations

In 60 seconds

Phase 2 obesity data (2008); further development has been limited. Cardiovascular and psychiatric effects are the main questions for monoamine reuptake inhibitors; an abuse-potential study was run in recreational stimulant users.

  • A phase 2 trial measured body-weight change and safety with tesofensine in obesity.
  • In obese rats, tesofensine’s appetite suppression involved α1-adrenoceptor and D1 pathways.
  • A randomised study assessed tesofensine’s abuse potential in recreational stimulant users.

Mechanism

By blocking reuptake of three monoamines, tesofensine suppresses appetite; animal work implicates α1-adrenoceptor and dopamine D1 pathways and silencing of GABAergic hypothalamic neurons.

Research status

Phase 2 obesity data (2008); further development has been limited. Not approved.

Key studies

  1. A phase 2 trial measured body-weight change and safety with tesofensine in obesity.

    Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial — Lancet, 2008 · PMID 18950853

  2. In obese rats, tesofensine’s appetite suppression involved α1-adrenoceptor and D1 pathways.

    Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of alpha1 adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat — Neuropsychopharmacology, 2010 · PMID 20200509

  3. A randomised study assessed tesofensine’s abuse potential in recreational stimulant users.

    Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users — Clin Pharmacol Ther, 2010 · PMID 20520602

  4. Found tesofensine silences GABAergic neurons in the hypothalamus.

    Tesofensine, a novel antiobesity drug, silences GABAergic hypothalamic neurons — PLoS One, 2024 · PMID 38656972

Safety signals in the literature

Cardiovascular and psychiatric effects are the main questions for monoamine reuptake inhibitors; an abuse-potential study was run in recreational stimulant users.

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Comparisons

Questions

What is Tesofensine?

A triple monoamine (noradrenaline, dopamine, serotonin) reuptake inhibitor that reduced weight in a phase 2 obesity trial. By blocking reuptake of three monoamines, tesofensine suppresses appetite; animal work implicates α1-adrenoceptor and dopamine D1 pathways and silencing of GABAergic hypothalamic neurons.

What is the research status of Tesofensine?

Phase 2 obesity data (2008); further development has been limited. Not approved.

What safety signals are reported for Tesofensine?

Cardiovascular and psychiatric effects are the main questions for monoamine reuptake inhibitors; an abuse-potential study was run in recreational stimulant users.

Does Living Water Labs stock Tesofensine?

Not at present. Tesofensine is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Approved incretin medicines are prescription-only (scheduled) in South Africa and available only through a prescriber; research-grade material is not a medicine and is not for human use.

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Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.

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