Tesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity.
Tesofensine is a serotonin-norepinephrine-dopamine reuptake inhibitor, originally developed to treat Parkinson's disease and Alzheimer's disease. According to a report by researchers at the 16th European Obesity Conference in Chemicalbook, Tesofensine helps obese patients lose weight and reduce the weight of suitable parts of their bodies and suitable ingredients (fat).
- Tesofensine is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity.
- Tesofensine was originally developed by a Danish biotechnology company, NeuroSearch, who transferred the rights to Saniona in 2014.
A serotonin-noradrenaline-dopamine reuptake inhibitor, tesofensine was originally in development for the treatment of neurological disorders such as Parkinson’s disease (PD) and Alzheimer’s disease.
Although tesofensine failed to demonstrate efficacy in PD trials, trial participants who were overweight achieved significant weight loss. This led the company to switch the development of tesofensine to obesity.
Tesofensine is in Phase III trials evaluating it as an anti-obesity medication. The protocol of the first Phase III trial was approved by the US Food and Drug Administration in the first half of 2010.
How does Tesofensine work?
Tesofensine is categorized as a pre-synaptic reuptake inhibitor of dopamine, serotonin, and noradrenaline. When these three neurotransmitter chemicals (serotonin, dopamine, and noradrenaline) are prevented from being reabsorbed by the central nervous system, the body responds by feeling less hungry. Patients, therefore, are more inclined to have smaller meals and are less likely to snack. Tesofensine also appears to affect the pleasure sensation of food consumption by modulating the action of dopamine on a particular sector of the brain.
Is Tesofensine Effective?
In a double-blind trial with 203 people (with half given a placebo) those taking the placebo had lost 2.0% of body weight while those taking the medication with the active ingredient had experienced far more successful results. For those taking the lowest dose of 0.25 mg, average weight loss was 6.5%, those taking the medium dose of 0.5% lost 11.2% and those taking the highest dose of 1 mg lost 12.6%. In the two highest dose groups, the treatment led to a 4 point drop in BMI in a period of 24 weeks.
Patients being treated with Tesofensine also displayed the following positive results:
- Reduction in appetite sensations within a period of 14 days, with those being treated reporting a greater level of satiety and less desire to eat.
- Significant increase in fat oxidation and reduction in fat tissue. The 24-hour fat oxidation increased by 15% and there was a reduction in protein oxidation. Scanning was able to provide confirmation of a statistically significant reduction in fat tissue compared with the placebo control group.
- Improved levels of insulin sensitivity were noted, leading to a higher metabolism of glucose, making this medication potentially suitable for patients at risk from type II diabetes.
- After 14 days, a significant increase in energy expenditure at the rest of 6% was observed compared with the placebo control group. This increase was directly linked to Tesofensine and any external factors were excluded as possible causes.
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