Peptora
← All peptides

Tesofensine

★ 80

Tesofensine (NS2330)

Triple monoamine reuptake inhibitor for weight loss

Fat Loss
Half-life
~9 days (parent); ~16 days (M1/NS2360 active metabolite)
Route
Oral tablet
Cycle
Continuous 24-week treatment
Status
Phase 3 complete in Mexico; not FDA-approved; investigational in US/EU

About

Tesofensine is a small-molecule (not a peptide) triple monoamine reuptake inhibitor that blocks reabsorption of dopamine, norepinephrine, and serotonin in the brain. Originally developed for Parkinson's and Alzheimer's disease, weight loss emerged as a striking side effect, redirecting development toward obesity. Phase 2 trials showed roughly twice the weight loss of approved drugs at the time, though cardiovascular and psychiatric signals at higher doses delayed FDA approval. It remains investigational in the US as of 2026, with conditional approval pathways advancing in Mexico.

Mechanism

Inhibits presynaptic reuptake of dopamine, norepinephrine, and serotonin, prolonging hypothalamic monoamine signaling — suppressing appetite and modestly raising resting energy expenditure.

Dosage

beginner

Amount
0.25 mg
Frequency
1x per day (morning)
Route
Oral tablet
Duration
24 weeks

standard

Amount
0.5 mg
Frequency
1x per day (morning)
Route
Oral tablet
Duration
24 weeks

advanced

Amount
0.5 mg (1.0 mg discontinued in Phase 2 due to BP elevation)
Frequency
1x per day (morning)
Route
Oral tablet
Duration
24 weeks
Timing

Morning, with or without food. Evening dosing causes insomnia due to long half-life and dopaminergic activity.

Cycle structure

Continuous 24-week treatment courses as studied in trials. Steady state reached at 4-6 weeks due to long half-life; abrupt discontinuation followed by a 4-6 week washout.

Reconstitution & Storage

N/A + N/A → N/A

Oral compound — no reconstitution needed.

Room temperature (15-25°C / 59-77°F), sealed container, protected from light and moisture.

Benefits

  • • ~10% body weight loss at 0.5 mg over 24 weeks (Phase 2)
  • • Roughly twice the weight loss of older approved anti-obesity drugs
  • • Once-daily oral dosing — no injections required
  • • Early appetite suppression within 1-2 weeks
  • • Possible mood and motivation lift from dopaminergic activity

Side effects

  • • Dry mouth, nausea, constipation, abdominal pain
  • • Insomnia and sleep disturbance
  • • Heart rate increase of 5-10 bpm at 0.5 mg
  • • Blood pressure elevation at 1.0 mg (dose discontinued)
  • • Anxiety, irritability, mood changes
  • • ~20% withdrawal rate due to adverse events in trials

Contraindications

  • • Uncontrolled hypertension or significant cardiovascular disease
  • • Anxiety disorders, bipolar disorder, or psychosis history
  • • Current MAO inhibitor use (serotonin syndrome risk)
  • • Concurrent SSRI, SNRI, or other serotonergic medications
  • • Strong CYP3A4 inhibitors (certain antifungals, antibiotics)
  • • Pregnancy, pregnancy planning, or breastfeeding
  • • Children and adolescents

Gender notes

Men

Standard dosing applies. Monitor blood pressure carefully — men in trials showed slightly higher BP signal at 1.0 mg.

Women

Standard dosing applies. Strict pregnancy avoidance required due to long half-life (effects persist weeks after discontinuation).

Research

Stacks well with

5-AMINO-1MQ SEMAGLUTIDE AOD-9604

Track Tesofensine doses in the app

Built-in reconstitution calculator, dose log, and reminders. Free on Android.

Get on Google Play

Educational use only. Not medical advice. Many peptides shown are not FDA-approved and remain research compounds. Always consult a qualified healthcare provider.