Tesofensine

A triple monoamine reuptake inhibitor originally developed for neurodegenerative diseases that was repurposed for obesity after significant weight loss was observed in clinical trials. Tesofensine suppresses appetite and increases thermogenesis through enhanced norepinephrine, dopamine, and serotonin signaling.

• Inhibits reuptake of norepinephrine, dopamine, and serotonin
• Enhances sympathetic nervous system activity to boost thermogenesis
• Modulates hypothalamic appetite regulation via monoamine signaling

• Uncontrolled hypertension or cardiovascular disease
• History of stroke or heart attack
• Concurrent use of MAO inhibitors or other stimulants
• Anxiety disorders or insomnia
• Pregnancy or breastfeeding

Store at room temperature (15–25°C (59–77°F)) in a cool, dry place away from light.

Phase 2 trials demonstrated that tesofensine 0.5 mg produced approximately 12.8% body weight loss over 24 weeks, roughly double that of existing anti-obesity medications at the time. Phase 3 trials (TESORA) are ongoing in several countries. The compound also showed improvements in metabolic parameters including HbA1c and lipid profiles. Cardiovascular safety monitoring remains a key focus.