A triple monoamine reuptake inhibitor with powerful central appetite suppression and significant weight-loss efficacy.
Inhibits the reuptake of serotonin, dopamine, and noradrenaline (triple monoamine reuptake inhibitor). The combined monoamine increase in hypothalamic satiety centres and the reward system produces potent appetite suppression and increased energy expenditure. Also modulates cholinergic neurons in the gut-brain axis.
Phase 2b TIPO-1 trial: Tesofensine 0.5mg produced ~10% body weight loss over 24 weeks — significantly greater than most approved weight loss drugs at the time. The drug was discontinued after showing moderate cardiovascular side effects (heart rate increase) in the trial.
There is renewed interest in tesofensine as combination therapies gain ground, with potential for sub-therapeutic doses combined with GLP-1 agonists. Research continues in obesity and binge eating.