Tesofensine is a serotonin–noradrenaline–dopamine reuptake inhibitor or triple reuptake inhibitor. It reduces the reabsorption of the neurotransmitters serotonin, norepinephrine, and dopamine. This boosts extracellular neurotransmitter concentrations. This phenomenon is responsible for tesofensine’s therapeutic advantages because each neurotransmitter has a unique role in the brain.
What Does Tesofensine Do?
Tesofensine increases dopamine, norepinephrine, and serotonin. Motor function, emotion, motivation, reward, cognitive function, and reproduction are regulated by dopamine. Norepinephrine promotes muscle and cardiac contractions to improve physical function. The hormone serotonin regulates mood, memory, sleep, and appetite.
Tesofensine Research On Obesity
Tesofensine Benefits aids in weight loss. Boosting dopamine in the brain may help treat obese and overweight people, say, researchers. A deficit in this neurotransmitter is connected to obesity and overeating. The fat-burning action of tesofensine is supported by human investigations.
The 2018 phase 3 Viking research found that obese patients who took both dosages of oral tesofensine (0.25 and 0.50 mg once a day) lost statistically and clinically significant weight at week 24 with a minimal incidence of side effects.
Phase 2b trial (TIPO-1) showed that obese patients treated with tesofensine lost an average of 12.8 kg on the 1 mg dose, 11.3 kg on the 0.5 mg dose, and 6.7 kg on the 0.25 mg dose, compared to a 2.2 kg loss in the placebo group. This suggests that tesofensine has the potential to produce a weight loss twice that of currently approved drugs.
- Tesofensine reduced obese patients’ urge to eat and boosted their satiety in the TIPO-2 experiment.
- Tesofensine treatment at 0.25 mg, 0.5 mg, or 1.0 mg led to statistically significant and clinically relevant weight loss with good effects on energy balance, hunger, physical activity, and quality of life.
- Tesofensine at 0.5 mg for 26 weeks produced weight loss double that of sibutramine or rimonabant.
- In overweight patients, 24 weeks of tesofensine causes appetite suppression and weight loss.
- In phase II clinical trials with tesofensine in obese people, significant weight, body fat, and waist circumference reductions were seen without serious side effects.
- In obese patients, long-term tesofensine administration is well-tolerated and results in significant weight loss.
- Patients with Parkinson’s or Alzheimer’s disease who took tesofensine once daily for 14 weeks without a weight-loss program lost about 4% of their body weight.
- Multiple doses of 0.125–1 mg tesofensine decrease hunger in healthy guys via increasing dopamine levels.
- In diet-induced obese rats, tesofensine suppressed hunger and boosted forebrain dopamine.
- In a rat model of diet-induced obesity (DIO), tesofensine (2 mg/kg, s.c.) for 16 days lowered body weights.
- Tesofensine at 2 mg/kg for 28 days reduced food intake and body weight in diet-induced obese rats.
- In 203 obese people, tesofensine 0.5 mg doubled the weight reduction of approved anti-obesity medicines.
- Obese patients who took tesofensine lost 10 percent of their body weight in 24 weeks.
- Tesofensine has a better weight-loss effect than licensed anti-obesity medicines, a study found.
- Tesofensine and an energy-restricted diet lowered weight in obese people.
Research shows that tesofensine helps sustain cognitive health by indirectly boosting cholinergic neurotransmission. It improves learning, memory, and thinking skills. The following studies show this:
- The first clinical outcomes of two short 4-week phase IIa trials in mild Alzheimer’s disease (AD) patients demonstrated tesofensine treatment improved cognitive performance.
- Obesity is a substantial risk factor for cognitive impairment in older adults. With its anti-obesity action, tesofensine may protect against cognitive impairment.
- In a mouse model of Alzheimer’s disease, tesofensine lowered brain concentrations of amyloid beta, aberrant protein clumps that cause the illness.
- Patients with advanced Parkinson’s disease and motor fluctuations benefited from low-dose tesofensine.
The antidepressant action of tesofensine has been found to boost mood.
- Increasing brain-derived neurotrophic factor (BDNF), which has an antidepressant impact.
- Anti-anxiety impact in obese patients with depression and anxiety symptoms.
- Raise serotonin, noradrenaline, and dopamine levels.
Raised Blood Sugar
Tesofensine lowers blood sugar levels.
- In obese patients, tesofensine at 0.25 mg, 0.5 mg, and 1.0 mg reduced blood sugar and improved quality of life.
- In rodents, tesofensine reduced blood sugar and caused weight loss.
Tesofensine improves productivity by boosting energy. Evidence supports tesofensine’s energy-boosting effects:
- Tesofensine boosts energy by boosting dopamine and norepinephrine, which regulate motivation, energy, interest, and drive.
- In one study, tesofensine increased energy expenditure in overweight and obese males compared to placebo.
Sexual Dysfunction Treated
Due to its antidepressant impact, tesofensine has also been researched for sexual dysfunction.
- Tesofensine increases dopamine, a neurotransmitter that contributes to sexual desire, erection, and ejaculation.
- Tesofensine is beneficial in treating depression-related sexual dysfunction, suggesting it can boost sexual power.
Helps Eating Disorders
Tesofensine, a triple reuptake inhibitor, may treat eating problems, according to studies.
- Tesofensine reduces appetite and increases satiety in obese people after 14 days.
- Tesofensine administration has been demonstrated to improve binge eating disorder symptoms, presumably due to its antidepressant impact.
- Tesofensine suppressed hunger in diet-induced obese rats through activating 1 adrenoceptor and dopamine d1 receptor pathways.
Treats Autism (ADHD)
ADHD causes short attention span, hyperactivity, and impulsivity in kids and adults. Evidence suggests tesofensine may help this mental condition:
- ADHD is linked to low levels of dopamine and serotonin, and tesofensine can help by raising these neurotransmitters.
- Tesofensine can reduce the risk of obesity-related ADHD.
Studies suggest tesofensine’s capacity to boost neurotransmitter levels improves sleep quality.
- Serotonin insufficiency is connected to insomnia and other sleeping problems.
- Increasing serotonin levels using selective serotonin reuptake inhibitors improves objective and subjective sleep quality in people with sleeping disorders, like tesofensine.
Evidence suggests tesofensine helps heal alcoholism by boosting neurotransmitter levels.
- Low dopamine levels are related to alcohol addiction; tesofensine’s ability to boost dopamine levels may help minimize excessive alcohol intake and accompanying consequences.
- Triple reuptake inhibitors reduced alcohol consumption without reducing food or water intake in ethanol-preferring rats.