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Context, anatomy, and key evidence

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monoamine reuptake inhibitor

Tesofensine

Published evidence · coverage incomplete

Anatomy in the research

Anatomy evidence is still being assembled.

These are anatomical mentions in cited research—not established treatment targets or proof of benefit in people.

This publication has no anatomy passages that meet our source-linking checks yet. Read the available findings ↓

General anatomy view only. No peptide-specific structures are highlighted.

At a glance

What is it—and why does it matter?

Tesofensine is described as inhibiting reuptake of monoamine neurotransmitters. In this randomized trial, adding tesofensine (0.25 mg, 0.5 mg, or 1.0 mg) to an energy-restricted diet increased mean percentage weight loss versus diet plus placebo at 24 weeks. Metabolite profiling identified four principal metabolites, including three dealkylation products (M1–M3) and one hydroxylation plus glucuronidation product (M4).

Sources for this introduction: [1] [2] [3]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

Tesofensine has an alternative identifier, NS-2330, indicating the same pharmacologically active compound.

Sources[8]pubmedInvestigations Into the Metabolism and Elimination of Tesofensine in Human Urine.Tesofensine (NS-2330) is a pharmacologically active compound with weight-reducing effects in obese patients.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Tesofensine (NS-2330) is a pharmacologically active compound with weight-reducing effects in obese patients.”

    Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine. · Abstract

    pubmed:42320973:3ab20e2ff97c:3ab20e2ff97c

Identity

The molecular formula reported for tesofensine is C17H23Cl2NO.

Sources[1]chembl-moleculeTESOFENSINEMolecular formula: C17H23Cl2NO
Molecular / pharmacology evidence

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Molecular formula: C17H23Cl2NO”

    TESOFENSINE · Molecular properties

    chembl-molecule:chembl3989690:fb0bf293e01f:fb0bf293e01f

Identity

Tesofensine is described as a monoamine reuptake inhibitor with activity at norepinephrine, serotonin (5-HT), and dopamine transport processes.

Sources[6]pubmedTesofensine, 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.Tesofensine is a novel monoamine reuptake inhibitor that inhibits both norepinephrine, 5-HT, and dopamine (DA) reuptake function.
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Tesofensine is a novel monoamine reuptake inhibitor that inhibits both norepinephrine, 5-HT, and dopamine (DA) reuptake function.”

    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. · Abstract

    pubmed:20200509:4d0925aead96:4d0925aead96

Identity

Tesofensine (NS‐2330) is described as a pharmacologically active compound with weight-reducing effects in obese patients.

Sources[2]doiInvestigations Into the Metabolism and Elimination of Tesofensine in Human UrineTesofensine (NS‐2330) is a pharmacologically active compound with weight‐reducing effects in obese patients.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Tesofensine (NS‐2330) is a pharmacologically active compound with weight‐reducing effects in obese patients.”

    Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine · Abstract

    doi:10.1002/dta.70104:a833da5a75c3:a833da5a75c3

How does it work?

Target, response, and disposition.

Mechanism

In vitro assays reported potent inhibition of dopamine, norepinephrine, and serotonin reuptake by tesofensine.

Sources[5]pubmedTesofensine, a monoamine reuptake inhibitor for the treatment of obesity.In vitro, the compound potently blocked dopamine, norepinephrine and serotonin reuptake.
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “In vitro, the compound potently blocked dopamine, norepinephrine and serotonin reuptake.”

    Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity. · Abstract

    pubmed:19777399:76ddff3b8d7c:76ddff3b8d7c

Mechanism

The abstract attributes tesofensine-induced hypophagia in obese rats to indirect activation of alpha1-adrenergic and dopamine D1 receptor pathways.

Sources[6]pubmedTesofensine, 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.Hence, the mechanism underlying the suppression of feeding by tesofensine in the obese rat is dependent on the drug's ability to indirectly stimulate alpha(1) adrenoceptor and DA D(1) receptor function.
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Hence, the mechanism underlying the suppression of feeding by tesofensine in the obese rat is dependent on the drug's ability to indirectly stimulate alpha(1) adrenoceptor and DA D(1) receptor function.”

    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. · Abstract

    pubmed:20200509:4d0925aead96:4d0925aead96

Mechanism

Tesofensine is described as inhibiting reuptake of monoamine neurotransmitters.

Sources[3]pubmedEffect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial.We assessed the efficacy and safety of tesofensine-an inhibitor of the presynaptic uptake of noradrenaline, dopamine, and serotonin-in patients with obesity.[5]pubmedTesofensine, a monoamine reuptake inhibitor for the treatment of obesity.Tesofensine, a monoamine reuptake inhibitor, is under development by NeuroSearch A/S for the potential treatment of obesity.
Human research · design must be checked

2 cited sources · 1 linked study ID · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

2 cited passages across 2 source records. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “We assessed the efficacy and safety of tesofensine-an inhibitor of the presynaptic uptake of noradrenaline, dopamine, and serotonin-in patients with obesity.”

    Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. · BACKGROUND

    pubmed:18950853:924fbf541b41:924fbf541b41
  2. supports · Source-backed record
    “Tesofensine, a monoamine reuptake inhibitor, is under development by NeuroSearch A/S for the potential treatment of obesity.”

    Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity. · Abstract

    pubmed:19777399:76ddff3b8d7c:76ddff3b8d7c

Pharmacokinetics

MS/MS fragmentation/dissociation patterns were used to support the structural assignment of metabolites M1–M4.

Sources[2]doiInvestigations Into the Metabolism and Elimination of Tesofensine in Human UrineFour principal metabolites were identified: three dealkylated metabolites (M1–M3) and one hydroxylated and glucuronidated metabolite (M4), supported by MS/MS dissociation patterns.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Four principal metabolites were identified: three dealkylated metabolites (M1–M3) and one hydroxylated and glucuronidated metabolite (M4), supported by MS/MS dissociation patterns.”

    Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine · Abstract

    doi:10.1002/dta.70104:a833da5a75c3:a833da5a75c3

Pharmacokinetics

Metabolite profiling identified four principal metabolites, including three dealkylation products (M1–M3) and one hydroxylation plus glucuronidation product (M4).

Sources[2]doiInvestigations Into the Metabolism and Elimination of Tesofensine in Human UrineFour principal metabolites were identified: three dealkylated metabolites (M1–M3) and one hydroxylated and glucuronidated metabolite (M4), supported by MS/MS dissociation patterns.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Four principal metabolites were identified: three dealkylated metabolites (M1–M3) and one hydroxylated and glucuronidated metabolite (M4), supported by MS/MS dissociation patterns.”

    Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine · Abstract

    doi:10.1002/dta.70104:a833da5a75c3:a833da5a75c3

What has been studied?

What the evidence says.

Study findings

In a Phase II clinical trial in obese subjects, tesofensine was associated with significant body-weight loss at 26 weeks.

Sources[4]pubmedTesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13.After 26 weeks, tesofensine caused a significant weight loss, and may have a higher maximal ability to reduce weight than the presently available anti-obesity agents.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “After 26 weeks, tesofensine caused a significant weight loss, and may have a higher maximal ability to reduce weight than the presently available anti-obesity agents.”

    Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13. · RESULTS

    pubmed:19548858:b90f60025c49:b90f60025c49

Study findings

In obese patients, tesofensine is described as having weight-reducing effects (no magnitude or duration provided).

Sources[8]pubmedInvestigations Into the Metabolism and Elimination of Tesofensine in Human Urine.Tesofensine (NS-2330) is a pharmacologically active compound with weight-reducing effects in obese patients.
Human research · design must be checked

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Tesofensine (NS-2330) is a pharmacologically active compound with weight-reducing effects in obese patients.”

    Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine. · Abstract

    pubmed:42320973:3ab20e2ff97c:3ab20e2ff97c

Study findings

In this randomized trial, adding tesofensine (0.25 mg, 0.5 mg, or 1.0 mg) to an energy-restricted diet increased mean percentage weight loss versus diet plus placebo at 24 weeks.

Sources[3]pubmedEffect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial.After 24 weeks, the mean weight loss produced by diet and placebo was 2.0% (SE 0.60). Tesofensine 0.25 mg, 0.5 mg, and 1.0 mg and diet induced a mean weight loss of 4.5% (0.87), 9.2% (0.91), and 10.6% (0.84), respectively, greater than diet and placebo (p<0.0001).
Human research · design must be checked

1 cited source · 1 linked study ID

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “After 24 weeks, the mean weight loss produced by diet and placebo was 2.0% (SE 0.60). Tesofensine 0.25 mg, 0.5 mg, and 1.0 mg and diet induced a mean weight loss of 4.5% (0.87), 9.2% (0.91), and 10.6% (0.84), respectively, greater than diet and placebo (p<0.0001).”

    Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. · FINDINGS

    pubmed:18950853:924fbf541b41:924fbf541b41

Study findings

Repeated subcutaneous tesofensine dosing in DIO rats was associated with reduced body weight relative to vehicle, with changes attributed to hypophagia in the report.

Sources[6]pubmedTesofensine, 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.DIO rats treated with tesofensine (2.0 mg/kg, s.c.) for 16 days showed significantly lower body weights than vehicle-treated DIO rats, being reflected by a marked hypophagic response.
Animal / laboratory evidence

1 cited source · Study independence not established

Animal or laboratory findings do not establish benefit or safety in people.

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “DIO rats treated with tesofensine (2.0 mg/kg, s.c.) for 16 days showed significantly lower body weights than vehicle-treated DIO rats, being reflected by a marked hypophagic response.”

    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. · Abstract

    pubmed:20200509:4d0925aead96:4d0925aead96

Risks and interactions

Risks, organized for scanning.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Products and regulatory status

Same ingredient. Different records.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Administration context

The practical clinical context.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Additional research & classification gaps

3 archived statements are kept separate from drug-effect findings. Media studies, economic models, methods, and records with unresolved scope are not used as medical-effect evidence.

Inspect contextual research (3)
Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Tesofensine is classified as a small-molecule compound in ChEMBL (ID CHEMBL3989690).

Research context only—not evidence of a treatment effect.

  • TESOFENSINE
    ChEMBL ID: CHEMBL3989690 Preferred name: TESOFENSINE Molecule type: Small molecule
Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Synonymy in this record links tesofensine to multiple alternate names (NS 2330, NS-2330, Ns2330, Tesofensina, Tesofensine).

Research context only—not evidence of a treatment effect.

  • TESOFENSINE
    NS 2330; NS-2330; Ns2330; Tesofensina; Tesofensine
Research context · scope unclassified

1 cited source · Study independence not established

How to read this evidence

Sources and study IDs describe provenance, not clinical strength. Several articles can report the same study; one study can support several distinct findings. No clinical strength rating has been assigned here.

1 cited passage across 1 source record. 1 publication group(s) lack a resolved study identity.

Tesofensine is reported to stabilize the dopamine transporter (DAT) in an outward-facing conformation, indicating a specific transporter conformational preference when bound.

Research context only—not evidence of a treatment effect.

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: administration, contraindication, interaction, regulatory, safety
  • 129 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (46), assurance_score_below_0.72 (73), current_regulatory_source_required (49), extraction_ambiguity (55), high_risk_requires_regulatory_or_two_independent_sources (81), no_direct_support (115)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. TESOFENSINE ↗

    chembl-molecule · published 2026-08-30 · retrieved 2026-08-30T08:40:08Z

  2. Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine ↗

    doi · published 2026-06-19 · retrieved 2026-09-09T18:03:44Z

  3. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. ↗

    pubmed · published 2008-11-29 · retrieved 2026-09-04T22:25:11Z

  4. Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13. ↗

    pubmed · published 2009-07-01 · retrieved 2026-09-09T23:05:19Z

  5. Tesofensine, a monoamine reuptake inhibitor for the treatment of obesity. ↗

    pubmed · published 2009-10-01 · retrieved 2026-09-09T23:05:18Z

  6. 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. ↗

    pubmed · published 2010-06-01 · retrieved 2026-09-09T23:05:16Z

  7. Structural basis for pharmacotherapeutic action of triple reuptake inhibitors. ↗

    pubmed · published 2025-12-14 · retrieved 2026-08-30T08:40:08Z

  8. Investigations Into the Metabolism and Elimination of Tesofensine in Human Urine. ↗

    pubmed · published 2026-09-01 · retrieved 2026-09-07T08:44:20Z

Publication history and provenance

Version 2 · Automated assessment · 2026-09-09T23:05:19Z

cac1b8da38bfb2f90eeb566e4f55fe6f93cffd931c1b5eab3353f11f7fb137e5