Tesofensine
Tesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor or also known as a triple reuptake inhibitor, which means that it inhibits the reabsorption of the neurotransmitters (brain chemicals) serotonin, norepinephrine, and dopamine. This process increases the extracellular concentrations of these neurotransmitters. The therapeutic benefits of tesofensine are attributed to this effect because each of these neurotransmitters exerts an important function at different locations in the brain.
What is Tesofensine?
Tesofensine (TE) inhibits the presynaptic reuptake of the neurotransmitter’s noradrenaline, dopamine and serotonin. Other types of selective serotonin reuptake inhibitors are used to treat depression and eating disorders, but they have generally failed to produce sustained weight loss. Sibutramine, in addition to its effect on serotonin, also inhibits the reuptake of other monoamines and has been shown to enhance postprandial satiety, reduce total calorie intake and to diminish the decline in energy expenditure usually associated with a diet-induced negative energy balance.
Tesofensine (TE) was originally studied for its effect on Parkinson's and Alzheimer's. Unfortunately, its exploration for these indications were limited because the patients were starting to lose too much weight. Since then, tesofensine has been studied as a way to treat obesity via its ability to reduce appetite. TE indirectly stimulates the cholinergic system and showed to be more successful than average weight loss remedies .
Tesofensine increases near transmission of a reuptake inhibitor 3 monoaminergic neurotransmitters in the brain. These neurotransmitters are serotonin, norepinephrine, and dopamine which help regulate energy balance and are linked to obesity and depression. On average, according to research, its 6-month weight loss results from research trials resulted in a weight loss of around 25 pounds.
What have Research Studies Shown?
Scientific research has revealed that Tesofensine can do the following:
• Increase energy metabolism
• Suppress appetite
• Improve the quality of life
• Improve body composition
• Neuroprotective
• Improved levels of insulin sensitivity
• Anti-depressant effects
Tesofensine in Research (Expanded)
Weight Loss:
Being overweight and/or obesity are major risk factors for diseases such as type 2 diabetes, coronary heart disease, sleep apnea and certain cancers, extensive efforts have been made to improve their treatment and prevention. Unfortunately, with the exception of bariatric surgery, these treatments most often produce only a modest and transient weight.
Weight-loss drugs produce an additional mean weight loss of only 3–5 kg above that of diet and placebo over 6 months, thus more effective pharmacotherapy of obesity is needed. In several studies, researchers have assessed the efficacy and safety of tesofensine—an inhibitor of the presynaptic uptake of noradrenaline, dopamine, and serotonin—in people with obesity.
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