Anti-obesity drugs: a review about their effects and their safety.
The review highlighted that tesofensine is among emerging anti-obesity therapies currently being studied for efficacy and safety in weight management.
NS2330
Tesofensine is a novel triple monoamine reuptake inhibitor that enhances the neurotransmission of noradrenaline, serotonin, and dopamine. Researchers primarily study Tesofensine for its potential effects on appetite regulation and its antidepressant properties. Key findings from studies indicate that chronic administration of Tesofensine increases the expression of brain-derived neurotrophic factor (BDNF) and activity-regulated cytoskeleton protein (Arc) in the hippocampus, which are associated with neurogenesis and mood regulation. Additionally, preclinical evidence suggests that Tesofensine may influence appetite expression in obese individuals, positioning it as a candidate for obesity pharmacotherapy. Currently, Tesofensine is undergoing Phase III clinical trials to further evaluate its efficacy and safety in the context of obesity treatment.
| 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 neurotransmission of noradrenaline, serotonin, and dopamine by blocking their respective transporters. This modulation is believed to influence various signaling pathways, including the BDNF signaling pathway, which is implicated in neurogenesis and synaptic plasticity, as evidenced by increased expression of brain-derived neurotrophic factor (BDNF) and activity-regulated cytoskeleton protein (Arc) in the hippocampus. While the precise mechanisms underlying its effects on appetite regulation and neurogenesis are not fully understood, the drug's action on these neurotransmitter systems suggests a multifaceted role in mediating both mood and metabolic processes.
783
Total Citations
4
Human/RCT
3.3
Avg. Influence
2025
Latest
The review highlighted that tesofensine is among emerging anti-obesity therapies currently being studied for efficacy and safety in weight management.
Researchers noted that tesofensine is one of several new anti-obesity drugs in development aimed at addressing the global obesity crisis through innovative pharmacological approaches.
Researchers observed that various pharmacological agents, including tesofensine, are under development to modulate appetite expression in obese individuals, although their effects on eating behavior remain poorly characterized.
The review indicated that tesofensine, a potent triple reuptake inhibitor, is in Phase III trials for obesity, reflecting advancements in pharmacotherapy for long-term weight management.
The review concluded that tesofensine targets multiple mechanisms of energy balance control, potentially leading to more effective obesity treatments in the future.
The study demonstrated that chronic treatment with tesofensine in rats increases the expression of BDNF and Arc mRNA, as well as enhances hippocampal neurogenesis.
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 randomized controlled human trials specifically evaluating the long-term efficacy and safety of tesofensine for obesity treatment have been published. Additionally, the precise mechanisms by which tesofensine modulates appetite and energy regulation in humans remain unclear, and its effects on eating behavior and psychological factors influencing appetite have not been thoroughly characterized.
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 |
|---|---|---|---|---|
BESTUmbrella LabsUS | 15mg | $79.99 | $5.33/mg | |
Umbrella LabsUS | 1mg | $99.99 | $99.99/mg | |
Bulk Peptide WholesaleUS | 0.5mg | $100.00 | $200.00/mg | |
Mile High CompoundsUS | 0.5mg | $119.99 | $239.98/mg | |
Iron PeptidesUS | 0.5mg | $129.00 | $258.00/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