Tesofensine (Capsule)

Tesofensine (NS2330)

A triple monoamine reuptake inhibitor with potent appetite suppression and weight loss effects.
100% 50% · t½ Time → Serum level
Molecular Weight Not specified
Half-Life Varies
Typical Dose One capsule
Cycle Length 12–24 weeks

Description

Tesofensine (NS2330) is a triple monoamine reuptake inhibitor originally developed by NeuroSearch for the treatment of Parkinson’s and Alzheimer’s disease, where it showed cognitive benefits but was ultimately repurposed for obesity after Phase II trials demonstrated remarkable weight loss. In a landmark 2008 Phase II trial published in The Lancet, Tesofensine at 0.5 mg produced 10.6% body weight reduction over 24 weeks — the highest weight loss ever reported for an oral weight loss drug at that time, significantly exceeding the efficacy of then-available obesity medications. Tesofensine works through a fundamentally different mechanism than GLP-1 agonists: rather than acting on gut hormones, it directly enhances central monoamine signaling to reduce appetite and increase metabolic rate. The compound is currently in Phase III trials for obesity in some regions and has been used in research settings for its combination of weight loss and cognitive enhancement properties.

Key Characteristics

Molecular Formula

Molecular Formula

Half-Life

Administration Routes

Oral capsule

Typical Dose

One capsule (per prescriber guidance)

Frequency

Once daily (morning)

Investigated Benefits

* Benefits based on preclinical/animal research unless otherwise noted.

Mechanism of Action

“A triple monoamine reuptake inhibitor with potent appetite suppression and weight loss effects.”

Tesofensine inhibits the reuptake transporters for dopamine (DAT), serotonin (SERT), and norepinephrine (NET) simultaneously, increasing the synaptic concentrations of all three monoamines in the central nervous system. This triple monoamine reuptake inhibition produces several metabolic effects: dopamine enhancement in the hypothalamus reduces appetite through reward pathway modulation; norepinephrine enhancement activates the sympathetic nervous system to increase metabolic rate and thermogenesis; serotonin enhancement contributes to satiety signaling and mood stabilization. Unlike amphetamines, which cause monoamine release, Tesofensine only blocks reuptake, producing a more controlled and sustained effect. The compound also has some cholinesterase inhibitory activity, which may contribute to its cognitive enhancement effects and explains its original development for neurodegenerative diseases. Morning dosing is essential as the stimulant and noradrenergic effects will significantly disrupt sleep if taken later in the day.

Administration Routes

Oral capsule

Key Characteristics

Typical Dose

One capsule (per prescriber guidance)

Frequency

Once daily (morning)

Cycle Length

12–24 weeks

Administration

Oral capsule

Protocol Notes

Morning dosing only — stimulant effects will disrupt sleep. Start with 0.25 mg to assess tolerance. Monitor heart rate and blood pressure.

Reconstitution Guide

Storage Information

Store at room temperature, away from light and moisture.

Quality & Sourcing Standards

When sourcing Tesofensine (Capsule) for research purposes, the following quality benchmarks should be verified before use.

Purity:

>98% (verified by HPLC)

Certificate of Analysis (COA):

Must be provided by supplier

Endotoxin Testing:

<0.1 EU/mg (prevents bacterial contamination)

GMP Compliance:

Manufactured in cGMP-certified facility

Third-Party Testing:

Independent lab verification preferred

Storage Information

Store at room temperature, away from light and moisture.

FDA Disclaimer

The statements made within this website have not been evaluated by the US Food and Drug Administration. The products and information provided are not intended to diagnose, treat, cure, or prevent any disease. This website is intended for educational and research purposes only. Many peptides described on this site are not approved by the FDA for human therapeutic use and are classified as research chemicals. Nothing on this site constitutes medical advice.

Research Highlights

1

Phase II: 10.6% weight loss at 0.5 mg — highest for oral drug at time of trial

2

Significant appetite suppression demonstrated

3

Phase III trials for obesity ongoing in some regions

Evidence Level

Multiple animal studies and/or early human trials. Reasonable confidence in mechanism, but human data is limited.

Compatible Peptides

Peptides commonly used alongside Tesofensine (Capsule) for synergistic effects.

5-Amino-1MQ (Capsule)

A small molecule NNMT inhibitor that promotes fat loss and metabolic health by raising cellular NAD+ levels.

SLU-PP-332 (Capsule)

An ERRα/γ agonist that mimics the metabolic effects of endurance exercise at the molecular level.

Quick Reference

Category

Metabolic & Weight
 

Status

Research Only
 

Dose

One capsule (per prescriber guidance)
 

Frequency

Once daily (morning)
 

Cycle

12–24 weeks