Tesofensine
Limited human dataSmall-molecule triple monoamine reuptake inhibitor (serotonin, norepinephrine, dopamine) — NOT a peptide · Also known as NS2330, Tesomet (with metoprolol)
Overview
Tesofensine is a small molecule, not a peptide — it has no amino-acid sequence and works centrally by inhibiting the reuptake of three neurotransmitters (dopamine, norepinephrine, and serotonin), which reduces appetite. It was originally developed for Parkinson's and Alzheimer's disease, where incidental weight loss redirected it toward obesity. A Phase 2 trial (TIPO-1) reported roughly 10% average body-weight loss over 24 weeks, but development has been limited by a cardiovascular safety signal (increases in blood pressure and heart rate). As of 2026 it is NOT FDA-approved in the US (it is approved in Mexico for obesity). Human efficacy beyond Phase 2 is not established in pivotal US trials.
Commonly Reported Uses
These are uses commonly discussed or marketed by users and vendors — not a list of proven or approved benefits, and not a recommendation.
- Weight loss / obesity (Phase 2 human data; NOT FDA-approved; approved in some countries such as Mexico)
- Appetite suppression (marketed claim; based on the same Phase 2 data)
- Hypothalamic obesity / Prader-Willi syndrome with metoprolol (investigational; FDA orphan-drug designation only, not approval)
What to Track
Data points you and your clinician might monitor. For observation only — not a diagnostic protocol.
- WHOOP — resting heart rate and HRV trend (a known cardiovascular safety signal)
- Labs/vitals — blood pressure monitoring if a clinician is overseeing use
- Smart scale — weight and body-fat % trend
- MyFitnessPal — calories and protein g/kg, given appetite suppression
- Subjective — daily mood, sleep, and appetite check-ins (monoamine activity can affect mood/sleep)
Sources & References
Quick Reference
- Class
- Small-molecule triple monoamine reuptake inhibitor (serotonin, norepinephrine, dopamine) — NOT a peptide
- Evidence Level
- Limited human data
- Reported Uses
- 3 listed
- Tracking Metrics
- 5 suggested
- Citations
- 3 sources
Safety & legal notes
NOT FDA-approved in the United States for any indication (investigational/IND only); approved in Mexico as Tesomet/Nupenta for obesity. FDA has granted orphan-drug designation for certain rare conditions, which is not the same as approval. The central safety concern is cardiovascular — elevations in heart rate and blood pressure. As a centrally acting stimulant-type agent, it raises doping-relevant concerns (stimulant and related categories may be prohibited in competition); athletes should verify the current WADA List. Consult a licensed clinician.
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