Anti-obesity drugs: a review about their effects and their safety.
The review highlighted that tesofensine is among the emerging anti-obesity therapies currently under investigation, alongside other pharmacotherapies for weight loss.
NS2330
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.
| Formula | C17H23Cl2NO |
| Molecular Weight | 328.3 g/mol |
| CAS Number | 195875-84-4 |
| PubChem CID | 11370864 |
Not applicable
Approximately 8-10 hours
Tesofensine exhibits a long half-life suitable for once-daily dosing.
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.
779
Total Citations
4
Human/RCT
3.3
Avg. Influence
2025
Latest
The review highlighted that tesofensine is among the emerging anti-obesity therapies currently under investigation, alongside other pharmacotherapies for weight loss.
Researchers noted that tesofensine is one of several new anti-obesity drugs in development, aimed at addressing the urgent need for effective obesity treatments.
Researchers observed that tesofensine is among the drugs under development that may beneficially alter appetite expression in obese individuals.
The review indicated that tesofensine, a potent triple reuptake inhibitor, is currently in Phase III trials for obesity treatment.
The review concluded that tesofensine, targeting multiple mechanisms of energy balance control, may contribute to more effective obesity treatments in the future.
The study demonstrated that chronic treatment with tesofensine increased BDNF and Arc mRNA levels and enhanced cell proliferation in the hippocampus of rats.
Li Yue, et al. · Nature communications · 2025
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
Perez Claudia I, et al. · PloS one · 2024
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
George Melvin, et al. · Journal of cardiovascular pharmacology and therapeutics · 2014
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
Schoedel K A, et al. · Clinical pharmacology and therapeutics · 2010
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
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.
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.
🇩🇪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.
Publications per Year
6 total| Vendor | Amount | Price | Price/mg | Link |
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BESTUmbrella LabsUS | 15mg | $79.99 | $5.33/mg | |
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Bulk Peptide WholesaleUS | 0.5mg | $100.00 | $200.00/mg | |
Orbitrex PeptideUS | 0.5mg | $129.99 | $259.98/mg | |
Iron PeptidesUS | 0.5mg | $129.99 | $259.98/mg |
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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