What is Tesofensine?
Tesofensine is a triple monoamine reuptake inhibitor originally developed for Parkinson's and Alzheimer's disease that showed significant weight loss effects. It inhibits reuptake of serotonin, dopamine, and norepinephrine, reducing appetite and increasing energy expenditure.
Note: Not a peptide but a small molecule often grouped with metabolic research compounds.
Development History
- Originally developed for neurodegenerative diseases
- Phase 2 trials for Parkinson's and Alzheimer's
- Efficacy insufficient for CNS indications
- BUT significant weight loss observed
- Redirected to obesity development
Mechanism
Triple Reuptake Inhibition
Inhibits reuptake of:
- Serotonin: Satiety effects
- Norepinephrine: Energy expenditure
- Dopamine: Reward/motivation
Together produce:
- Appetite suppression
- Increased metabolism
- Reduced food reward
Clinical Results
Phase 2 obesity trials showed:
- 10-13% weight loss at 6 months
- Superior to existing medications at the time
- Dose-dependent effects
Status
- Phase 3 trials ongoing
- Not yet approved
- Heart rate/BP concerns being monitored
- Potential future obesity treatment
Summary
Key Points:
- Classification: Triple reuptake inhibitor
- Mechanism: 5-HT, NE, DA reuptake
- Effect: Weight loss
- Status: Phase 3 development