Tesofensine
Clinical TrialsTesofensine
A triple monoamine reuptake inhibitor originally researched for Parkinson's and Alzheimer's. Repurposed for obesity research showing significant weight loss in trials.
Dose
0.25 mg - 1 mg
Route
Oral
Cycle
Variable, typically 12-24 weeks in research settings
Storage
Not applicable (oral compound)
What is Tesofensine?
Tesofensine is a triple monoamine reuptake inhibitor that was initially investigated for its potential in treating neurological disorders such as Parkinson's and Alzheimer's disease. However, research later shifted to its potent effects on weight management. It works by inhibiting the reuptake of serotonin, norepinephrine, and dopamine in the central nervous system, leading to increased levels of these neurotransmitters in the synaptic cleft. This action is believed to reduce appetite, increase satiety, and enhance energy expenditure, ultimately promoting significant weight loss in research subjects.
Key Benefits
- Significant weight loss in trials
- Appetite suppression
- Increased energy expenditure
- Cognitive function research
Mechanism of Action
- Inhibits reuptake of serotonin, norepinephrine, and dopamine
- Reduces appetite via CNS mechanisms
- Increases metabolic rate
Best For
- Weight loss research
- Metabolic health
Body Systems
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Molecular Information
Molecular weight
331.3 g/mol
Length
Not applicable (small molecule)
Type
Small Molecule
Amino acid sequence
Not applicable (small molecule)
Tesofensine is a non-peptide small molecule.
Pharmacokinetics
Time to peak
1-2 hours
Half-life
220 h
Time to clear
Approximately 45-55 days (5-6 half-lives)
Relevant peer-reviewed pharmacokinetic studies.
Research Indications
Obesity
Tesofensine has demonstrated significant efficacy in reducing body weight and improving obesity-related parameters in clinical trials.
Appetite Suppression
Research indicates potent appetite-suppressing effects, contributing to reduced caloric intake.
Increased Energy Expenditure
Studies suggest an increase in metabolic rate and energy expenditure, which supports weight loss.
Research Protocols
| Goal | Dose | Frequency | Route |
|---|---|---|---|
| Obesity Research (Weight Loss) | 0.25 mg - 1 mg | Once daily | Oral |
| Appetite Regulation Studies | 0.5 mg | Once daily | Oral |
| Metabolic Rate Impact Assessment | 0.25 mg | Once daily | Oral |
| Long-term Weight Maintenance Research | 0.5 mg | Once daily | Oral |
Oral administration is typically once daily. Consistency in timing is commonly discussed in research protocols.
Peptide Interactions
- Avoid
Monoamine Oxidase Inhibitors (MAOIs)
Concomitant use is contraindicated due to the risk of hypertensive crisis and serotonin syndrome.
- Use Caution
Serotonin Reuptake Inhibitors (SSRIs) / Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)
Increased risk of serotonin syndrome or exacerbated noradrenergic side effects (e.g., increased heart rate, blood pressure, anxiety).
- Use Caution
Norepinephrine Reuptake Inhibitors (NRIs) / Stimulants
Potential for additive cardiovascular and CNS stimulant effects, leading to increased heart rate, blood pressure, and anxiety.
- Use Caution
Tricyclic Antidepressants (TCAs)
May enhance the effects of TCAs, leading to increased plasma concentrations and potential for adverse effects due to combined reuptake inhibition.
- Monitor Combination
Antihypertensive Medications
Tesofensine may increase blood pressure, potentially counteracting the effects of antihypertensive drugs; close monitoring is required.
- Monitor Combination
Alcohol
May enhance CNS depressant or stimulant effects and reduce tolerance; caution is advised.
How to Reconstitute
Taken orally — no reconstitution required.
What to Expect
- Weeks 1-4: Initial changes in appetite, possibly increased energy and reduced food cravings. Some subjects may report mild side effects like dry mouth or insomnia.
- Weeks 4-12: More noticeable reductions in body weight, often accompanied by continued appetite suppression. Metabolic rate changes may become more apparent.
- Weeks 12-24: Significant and sustained weight loss typically observed in research settings. Continued monitoring of metabolic parameters and potential side effects is common.
- Beyond 24 weeks: Long-term research protocols continue to evaluate efficacy and safety, particularly for sustained weight management and maintenance.
Side Effects & Safety
| Effect | Frequency | Severity |
|---|---|---|
| Increased heart rate | Common | Moderate |
| Dry mouth | Common | Mild |
| Insomnia | Common | Mild |
| Nausea | Common | Mild |
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