SingleMetabolic & Weight

Tesofensine 0.5mg

An investigational oral triple monoamine reuptake inhibitor researched in Phase II clinical trials for weight regulation and appetite suppression.

Mechanism

Tesofensine functions as a triple monoamine reuptake inhibitor that concurrently blocks transporters for dopamine, noradrenaline, and serotonin to prolong central neurotransmitter signaling.

Dosing

Published experimental trials initiated research arms at 0.25 mg taken orally once daily before evaluating higher concentrations.

Reconstitution

Tesofensine is formulated as an oral solid preparation that requires no reconstitution or dilution with bacteriostatic water.

Storage

Keep oral capsules sealed in their original dry container at controlled room temperature, shielded from moisture, direct sunlight, and excessive heat.

Mix & measure Tesofensine 0.5mg

Pre-filled with this protocol's recommended BAC water and documented starting dose — edit any field to run your own numbers.

Mix & measure Tesofensine 0.5mg

Vial strength → BAC water → target dose

Vial strength

BAC water

Target dose

Concentration—

Draw volume—

On the syringe—

Total doses in vial: —

100u80u60u40u20u0

U-100 syringe: 100 units = 1 mL

Reconstitution math only — not dosing advice. U-100 syringe: 100 units = 1 mL. Advanced calculator →

Dosing Chart

Phase / Day(s)	Dose & Frequency	Volume (U-100 units / mL)
Lowest active arm	0.25 mg (1× daily, oral)	N/A (Oral Capsule)
Balance-point arm	0.5 mg (1× daily, oral)	N/A (Oral Capsule)
Highest active arm	1.0 mg (1× daily, oral)	N/A (Oral Capsule)

Reconstitution Steps

1
Inspect the packaging to confirm capsule identity, intact seals, and documented milligram potency.
2
Prepare clean laboratory measurement tools or dispense the intact oral pre-formulated capsule directly.
3
No liquid mixing is required; do not introduce bacteriostatic water, antimicrobial diluents, or syringe needles.
4
Store remaining capsules tightly sealed with a desiccant pack in a dry, room-temperature environment.

Supplies Needed

Peptide Vial

Provides pre-metered tesofensine oral capsules for laboratory research analysis.

Insulin Syringes (U-100)

Not required for oral solid-dose investigational compounds.

Bacteriostatic Water

Not required; tesofensine does not undergo aqueous reconstitution.

Alcohol Swabs

Used for sanitizing laboratory prep surfaces and equipment handling areas.

Why researchers study it

Obesity and weight management investigations

Hypothalamic appetite suppression and satiety signaling

Syndromic obesity models including Prader-Willi research

Neurodegenerative pathways and monoaminergic modulation

These describe what is being studied, not proven benefits, approved uses, or promised results.

Overview

Tesofensine (NS2330) is an investigational small molecule belonging to the phenyltropane chemical class rather than a true peptide structure. Originally explored for potential neuroprotective roles in Parkinson's and Alzheimer's disease research, it was subsequently pivoted toward metabolic science following observations of robust appetite modulation and substantial weight loss in preclinical and clinical models. Unlike conventional metabolic peptides that interface with peripheral incretin receptors, tesofensine operates directly within the central nervous system to alter neurotransmitter dynamics. Its pharmacokinetic profile is defined by an unusually sustained elimination half-life of roughly nine days, which results in cumulative systemic exposure across several weeks before a steady-state concentration is achieved in experimental subjects. Because of its small-molecule formulation, tesofensine is supplied and evaluated in oral solid-dosage preparations, bypassing the sterile reconstitution procedures required for injectable research peptides. Scientific evaluation focuses on balancing central satiety stimulation against sympathetic activation markers such as heart rate and arterial pressure.

References

1.Astrup et al., The Lancet, 2008 — 24-week randomised, double-blind, placebo-controlled Phase II trial of tesofensine for bodyweight loss in obese patients
2.Sjödin et al., International Journal of Obesity, 2010 — effect of tesofensine on energy metabolism and appetite in overweight and moderately obese men
3.Gilbert et al., Obesity (Silver Spring), 2011 — tesofensine effects on appetite sensations and satiety mechanisms
4.Bello & Zahner, Current Opinion in Investigational Drugs, 2009 — review of tesofensine mechanism, pharmacology, and cardiovascular signals
5.Lehr et al., British Journal of Clinical Pharmacology, 2007 — population pharmacokinetic modelling of NS2330 demonstrating long half-life and accumulation
6.Schoedel et al., Clinical Pharmacology & Therapeutics, 2010 — subjective and objective effects of tesofensine in recreational stimulant users assessing abuse liability
7.Hauser et al., Movement Disorders, 2007 — randomised trial of NS 2330 in early Parkinson's disease neurodegeneration research
8.ClinicalTrials.gov, Tesomet Trials, 2021 — registered studies combining tesofensine and metoprolol in hypothalamic obesity and Prader-Willi syndrome