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Tesofensine

NS2330

Metabolic & WeightPhase II
From$5.33/mgCompare prices
MW
328.3g/mol
Formula
C17H23Cl2NO

Tesofensine is a novel triple monoamine reuptake inhibitor originally developed as an antidepressant, which has garnered attention for its potential role in obesity management. Researchers primarily study tesofensine for its effects on appetite regulation and weight loss. Key findings from recent studies suggest that tesofensine enhances neurotransmission of noradrenaline, serotonin, and dopamine, leading to significant reductions in body weight and appetite in clinical trials. Additionally, preclinical evidence indicates that chronic administration may promote neurogenesis and increase the expression of brain-derived neurotrophic factor in the hippocampus, suggesting potential cognitive benefits. Currently, tesofensine is undergoing Phase III clinical trials to further evaluate its efficacy and safety as a treatment for obesity.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC17H23Cl2NO
Molecular Weight328.3 g/mol
CAS Number195875-84-4
PubChem CID11370864

Half-Life

INIntranasal

Not applicable

POOral

Approximately 8-10 hours

Tesofensine exhibits a long half-life suitable for once-daily dosing.

Mechanism

Mechanism of Action

Tesofensine acts as a triple monoamine reuptake inhibitor, enhancing the levels of norepinephrine, serotonin, and dopamine in the synaptic cleft by blocking their respective transporters (NET, SERT, and DAT). This modulation of neurotransmitter levels influences appetite regulation and energy homeostasis through pathways associated with the central nervous system, although the precise mechanisms and receptor interactions involved in its anti-obesity effects remain incompletely understood. Additionally, chronic administration of tesofensine has been shown to increase brain-derived neurotrophic factor (BDNF) expression, potentially promoting neurogenesis in the hippocampus, which may further contribute to its therapeutic effects.

Research

14 Research Publications

779

Total Citations

4

Human/RCT

3.3

Avg. Influence

2025

Latest

Sort
Filter
#01

Anti-obesity drugs: a review about their effects and their safety.

ReviewInfluence4.0
194
The review highlighted that tesofensine is among the emerging anti-obesity therapies currently under investigation, alongside other pharmacotherapies for weight loss.
PubMed
#02

Future Pharmacotherapy for Obesity: New Anti-obesity Drugs on the Horizon.

ReviewInfluence2.0
189
Researchers noted that tesofensine is one of several new anti-obesity drugs in development, aimed at addressing the urgent need for effective obesity treatments.
PubMed
#03

Pharmacological management of appetite expression in obesity.

ReviewInfluence3.0
139
Researchers observed that tesofensine is among the drugs under development that may beneficially alter appetite expression in obese individuals.
PubMed
#04

Centrally Acting Agents for Obesity: Past, Present, and Future.

ReviewInfluence2.0
134
The review indicated that tesofensine, a potent triple reuptake inhibitor, is currently in Phase III trials for obesity treatment.
PubMed
#05

New approaches to the pharmacological treatment of obesity: can they break through the efficacy barrier?

ReviewInfluence8.0
78
The review concluded that tesofensine, targeting multiple mechanisms of energy balance control, may contribute to more effective obesity treatments in the future.
PubMed
#06

Expression of brain derived neurotrophic factor, activity-regulated cytoskeleton protein mRNA, and enhancement of adult hippocampal neurogenesis in rats after sub-chronic and chronic treatment with the triple monoamine re-uptake inhibitor tesofensine.

AnimalInfluence1.0
45
The study demonstrated that chronic treatment with tesofensine increased BDNF and Arc mRNA levels and enhanced cell proliferation in the hippocampus of rats.
PubMed
#07

Structural basis for pharmacotherapeutic action of triple reuptake inhibitors.

Li Yue, et al. · Nature communications · 2025

Human
Researchers studied a new class of antidepressants called triple reuptake inhibitors (TRIs), which target serotonin, norepinephrine, and dopamine levels. They found that different TRIs bind to a brain protein in unique ways, potentially leading to more effective treatments with fewer side effects for patients with depression.

Key findings

  1. 01Researchers observed that TRIs like tesofensine and dasotraline stabilize a brain protein in an outward-facing position, while others like centanafadine and ansofaxine stabilize it in an inward-facing position.
  2. 02The study identified specific binding sites for these TRIs, which could inform the development of new antidepressants.
  3. 03Notably, ansofaxine binds closer to the inner surface of the brain cell membrane, suggesting a unique mechanism of action.
PubMed
#08

Tesofensine, a novel antiobesity drug, silences GABAergic hypothalamic neurons.

Perez Claudia I, et al. · PloS one · 2024

Animal
Researchers studied tesofensine, a new anti-obesity drug, and found that it promotes significant weight loss in obese rats by targeting specific neurons in the brain that control feeding behavior. The study suggests that tesofensine may be effective in preventing weight regain after dieting, making it a promising option for obesity treatment.

Key findings

  1. 01Researchers found that tesofensine led to greater weight loss in obese rats compared to lean rats.
  2. 02The drug inhibited certain neurons in the hypothalamus that promote feeding, enhancing its appetite-suppressing effects.
  3. 03Tesofensine also helped maintain weight loss after treatment, reducing the likelihood of weight rebound.
PubMed
#09

New and emerging drug molecules against obesity.

George Melvin, et al. · Journal of cardiovascular pharmacology and therapeutics · 2014

Review
Researchers reviewed new and emerging drug molecules aimed at combating obesity, a growing health crisis linked to serious heart conditions. They found several promising candidates in clinical trials, including drugs that target the gut and the brain, which may offer better safety and efficacy compared to existing treatments.

Key findings

  1. 01Current anti-obesity medications have limited effectiveness and safety concerns, leading to a need for new options.
  2. 02New drugs like cetilistat, exenatide, and liraglutide are being tested for their potential to manage obesity more effectively.
  3. 03Innovative approaches targeting various biological pathways, such as the histamine H3 receptor, are under investigation for their role in obesity treatment.
PubMed
#10

Subjective and objective effects of the novel triple reuptake inhibitor tesofensine in recreational stimulant users.

Schoedel K A, et al. · Clinical pharmacology and therapeutics · 2010

Human
Researchers studied the effects of tesofensine, a new drug being developed for obesity, in recreational stimulant users. They found that tesofensine did not produce significant effects compared to a placebo and had a lower potential for abuse than traditional stimulants like D-amphetamine.

Key findings

  1. 01The effects of tesofensine were not significantly different from those of a placebo.
  2. 02D-amphetamine produced much stronger effects than tesofensine.
  3. 03Tesofensine's abuse potential is similar to that of bupropion and atomoxetine, suggesting it is unlikely to be misused recreationally.
PubMed
Safety

Safety & Handling

Research Gaps

No comprehensive human trials have been published that specifically evaluate the long-term effects of tesofensine on weight management and appetite regulation. Additionally, the precise mechanisms by which tesofensine influences neurohormonal pathways and its impact on psychological factors related to appetite remain poorly understood.

Solubility

Tesofensine is moderately soluble in water and highly soluble in DMSO.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA. Not scheduled by the DEA.

🇦🇺AU

Not approved by the TGA. Not scheduled.

🇬🇧UK

Not approved by the MHRA. Not a controlled substance.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Community Insights

Publications per Year

6 total
1
07
2
10
1
12
2
18
Pricing

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer