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Tesofensine is widely known as a weight loss drug. Researchers believe that tesofensine may help treat obese and overweight patients because it boosts the levels of dopamine in the brain. A deficiency in this neurotransmitter has been shown to be linked with overeating and obesity. [1-5] An overwhelming body of human studies supports the fat-burning effect of tesofensine:
1. The results of the 2018 phase 3 Viking study showed that obese patients who received both doses of oral tesofensine (0.25 and 0.50 mg once daily) had statistically and clinically significant weight loss with low incidence of adverse events. [6]
2. The results of 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 with a 2.2 kg loss in the placebo group, suggesting that tesofensine has the potential to produce a weight loss twice that of currently approved drugs. [7]
3. In the TIPO-2 trial, tesofensine administration in obese patients reduced their desire to eat and increased their satiety levels after 14 days of treatment. [8]
4. Preliminary results of the TIPO-4 trial, a 48-week open-label extension to the TIPO-1 trial, showed that patients continuing with 0.5mg oral tesofensine achieved a total mean weight loss of 13–14kg at 24 weeks. [9]
5. In obese patients, tesofensine treatment at varying doses (0.25 mg, 0.5 mg or 1.0 mg) resulted in statistically significant and clinically relevant weight loss with positive effects on energy balance, appetite, physical activity, and quality of life. [10]
6. In obese patients, tesofensine administration at a dose of 0.5 mg for 26 weeks produced weight loss twice that of anti-obesity agents such as sibutramine or rimonabant. [11]
7. In overweight patients, tesofensine administration for 24 weeks is associated with enhanced appetite suppression and significant weight loss. [12]
8. In phase II clinical trials with tesofensine in obese individuals, significant reductions in body weight, body fat and waist circumference were observed without any adverse side effects. [13]
9. In obese patients, long-term tesofensine supplementation is well-tolerated and resulted in significant weight loss. [14]
10. In patients with Parkinson’s or Alzheimer’s disease, tesofensine administration once daily for 14 weeks without any weight loss program induced weight loss of approximately 4%, which is similar to that of sibutramine. [15]
11. In healthy males, multiple administration of tesofensine at doses of 0.125–1 mg induced a significant increase in dopamine levels, resulting in appetite suppression. [16]
12. In diet-induced obese rat, tesofensine administration resulted in appetite suppression and weight loss with reversal of low forebrain dopamine levels. [17]
13. In a rat model of diet-induced obesity (DIO), administration of tesofensine (2.0 mg/kg, s.c.) for 16 days significantly reduced body weights. [18]
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