Tesofensine

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.

• Researchers 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.
• The study identified specific binding sites for these TRIs, which could inform the development of new antidepressants.
• Notably, ansofaxine binds closer to the inner surface of the brain cell membrane, suggesting a unique mechanism of action.

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.

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

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.

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

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.

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

Current opinion in investigational drugs (London, England : 2000) · 2009

Researchers studied tesofensine, a drug that affects brain chemicals, as a potential treatment for obesity. They found that it led to significant weight loss and reductions in body fat among obese individuals, with few side effects reported. The FDA has shown support for further testing of tesofensine in larger trials.

• Researchers observed that tesofensine caused dose-related reductions in body weight and body fat in obese individuals.
• The drug was associated with minor side effects, including slight increases in heart rate and blood pressure at higher doses.
• Initial results suggest that tesofensine may be a well-tolerated option for long-term obesity management.

Expert opinion on investigational drugs · 2009

Researchers found that tesofensine, a new weight loss medication, led to significant weight loss in obese individuals over 26 weeks. However, it also raised concerns due to increased blood pressure, heart rate, and potential psychiatric side effects. Further studies are needed to evaluate its long-term safety and effectiveness compared to existing weight loss medications.

• Tesofensine resulted in nearly double the weight loss compared to other anti-obesity drugs like sibutramine.
• The medication was associated with increased blood pressure and heart rate.
• Participants reported side effects such as nausea, insomnia, and mood changes.

Obesity (Silver Spring, Md.) · 2008

Researchers studied the effects of tesofensine on weight loss in patients with Parkinson's and Alzheimer's disease. They found that participants taking tesofensine lost about 4% of their body weight over 14 weeks compared to those on a placebo, with significant weight loss observed in obese patients.

• Participants taking tesofensine experienced a placebo-subtracted weight loss of approximately 4% over 14 weeks.
• In the obese subgroup, a significant percentage of patients achieved over 5% weight loss.
• Tesofensine did not affect blood pressure but was associated with a slight increase in heart rate.

British journal of clinical pharmacology · 2007

Researchers studied the drug NS2330 and its major metabolite in patients with Alzheimer's disease to understand how different factors affect their levels in the body. They found that weight, sex, kidney function, body mass index, and age can influence how the drug is processed, with significant differences observed between males and females.

• Researchers observed that the drug NS2330 and its metabolite M1 have long half-lives of 234 hours and 374 hours, respectively.
• The study identified that factors such as sex and kidney function significantly affect the drug's concentration in the bloodstream.
• Females with lower kidney function showed a 62% higher exposure to NS2330 compared to males without kidney issues.