Tesofensine
Triple monoamine reuptake inhibitor, an investigational anti-obesity agent with strong appetite suppression.
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Pharmacology
Contents
WHAT IS TESOFENSINE?
Detailed overview
Tesofensine (NS2330) is a triple monoamine reuptake inhibitor: it blocks the dopamine, norepinephrine and serotonin transporters at the same time, prolonging the presence of all three neurotransmitters in the synapse. It was originally developed for Parkinson's and Alzheimer's disease, but the striking weight loss seen in trials redirected interest toward obesity. In the 2008 phase 2 trial (TIPO-1) the middle and higher doses produced mean weight loss of roughly 9 to 11 percent over 24 weeks, about twice that of previously approved obesity drugs. Its half-life is unusually long, around 8 days, so it is dosed once daily in the morning. It has been studied in humans up to phase 2 but is not approved for obesity anywhere; a combination called Tesomet (with metoprolol to blunt the heart-rate rise) is in development for rare satiety and eating disorders.
Mechanism
Triple monoamine reuptake inhibitor (DAT/NET/SERT)
Half-life
About 8 days (once-daily morning dose)
Legal status
In development, not approved
Receptor profile
- Dopamine / norepinephrine / serotonin transporters (DAT/NET/SERT)Strong
- Satiety and energy expenditure (hypothalamus)Strong
- Hypothalamic GABAergic tone (indirect)Moderate
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Dry mouth, the most common and dose-dependent complaint
- Insomnia and disrupted sleep, especially with late dosing
- Increased heart rate and modest blood pressure rise (about 7 bpm on average)
- Constipation and gastrointestinal discomfort
- Restlessness, tremor and agitation from monoaminergic overstimulation
- Mood changes, irritability and anxiety at higher doses
Contraindications · 5
- Cardiovascular disease, arrhythmia, uncontrolled hypertension: due to the heart-rate and blood-pressure raising effect
- Concurrent MAO inhibitors or serotonergic drugs: risk of serotonin syndrome
- Anxiety disorder, panic disorder or mood disorder: the stimulant effect may worsen them
- Pregnancy and breastfeeding: safety not established, avoid
- Not an approved medicine: not recommended without clinical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial
Astrup A, Madsbad S, Breum L, Jensen TJ, Kroustrup JP, Larsen TM
The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men
Sjödin A, Gasteyger C, Nielsen AL, Raben A, Mikkelsen JD, Jensen JK, Meier D, Astrup A
The novel triple monoamine reuptake inhibitor tesofensine induces sustained weight loss and improves glycemic control in the diet-induced obese rat
Hansen HH, Hansen G, Tang-Christensen M, Larsen PJ, Axel AM, Raben A, Mikkelsen JD
Randomized controlled trial of Tesomet for weight loss in hypothalamic obesity
Huynh K, Klose M, Krogsgaard K, Drejer J, Byberg S, Madsbad S, Feldt-Rasmussen U
Centrally Acting Agents for Obesity: Past, Present, and Future
Perdomo CM, Cohen RV, Sumithran P, Clément K, Frühbeck G
FAQ
FAQ
Triple monoamine reuptake inhibitor, an investigational anti-obesity agent with strong appetite suppression.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.