Tesofensine vs PGPIPN
Side-by-side comparison of key properties, dosing, and research.
Fat Loss & Metabolic
TesofensineImmune Support
PGPIPN- Summary
- Tesofensine is a triple monoamine reuptake inhibitor (TMRI) that blocks reuptake of serotonin, dopamine, and norepinephrine. Originally developed for Alzheimer's and Parkinson's disease, it was repurposed as a potent weight loss agent after clinical trials demonstrated substantial fat loss via appetite suppression and increased energy expenditure.
- PGPIPN is a bioactive hexapeptide (Pro-Gly-Pro-Ile-Pro-Asn) derived from beta-casein during enzymatic digestion. It exhibits anti-inflammatory properties via opioid receptor modulation and cytokine suppression, making it relevant for gut health, systemic inflammation, and as a component of casein-derived functional foods.
- Half-Life
- 8-10 days (exceptionally long; accumulates over weeks)
- Estimated 30-120 minutes (peptide degradation)
- Admin Route
- Oral
- Oral, Subcutaneous (research)
- Research
- —
- —
- Typical Dose
- 0.25-0.5 mg per day
- 200-500 mg per day
- Frequency
- Once daily
- Once or twice daily
- Key Benefits
- Potent appetite suppression via triple monoamine reuptake inhibition
- Significant weight loss (8-12% body weight in phase II trials at 0.5 mg)
- Increases basal metabolic rate and energy expenditure
- Reduces fat mass preferentially over lean mass
- Potential cognitive benefit via dopaminergic and noradrenergic enhancement
- Longer half-life than sibutramine allows once-daily dosing
- Anti-inflammatory effects via cytokine suppression
- Gut mucosal protection and intestinal barrier support
- Opioid receptor modulation for gut motility regulation
- Potential analgesic activity via central and peripheral opioid pathways
- Explored for inflammatory bowel conditions and gut dysbiosis
- Natural origin (food-derived) with favorable safety profile
- Side Effects
- Elevated heart rate and blood pressure (sympathomimetic)
- Dry mouth
- Insomnia and sleep disturbances
- Nausea
- +4 more
- Generally very well-tolerated given food-derived origin
- Theoretical opioid-mediated constipation at high doses
- Rare milk protein allergy in casein-sensitive individuals
- Stacks With
- —
- —