library.onepin.app/tesofensine Peptide Education Library
Education only, not medical advice 21+ Every dose is an example to finalize with a licensed provider
Weight Triple Monoamine Reuptake InhibitorNot FDA-approved · research compound

Tesofensine

NS-2330

0.25mg daily – 0.25-0.5 mg Oral 1x daily
Small-Molecule Weight Loss DrugMexico-Approved (Tesomet 2023)Research Chemical (no FDA approval)

Tesofensine is a small-molecule monoamine reuptake inhibitor (norepinephrine, serotonin, dopamine triple reuptake inhibitor / SNRI+DRI). Originally developed by NeuroSearch for Parkinson's disease and Alzheimer's disease, repurposed for obesity after Phase 2 trials showed substantial weight loss as an off-target effect. The TIPO-1 trial in obese patients showed dose-dependent weight loss up to ~12% at 1mg daily over 24 weeks - among the largest non-injectable weight loss agents.

Quick Start
Route
Oral capsule
Start low
0.25mg Oral
Frequency
1x daily
Timing
With food

Morning preferred (CNS-active).

Start here. Every protocol below is ordered lowest-first. Begin at the smallest effective dose, hold about a week to assess tolerance, and step up only if needed.

Tiered Protocols · lowest first
Conservative start
0.25mg daily · Oral capsule · 1x daily
conservative starter
0.25mg daily
1x daily
Intermediate
Monoamine Weight Loss
0.25-0.5 mg · Oral · Daily
human clinical trial · Astrup et al. 2008 (Lancet 2008;372:1906-13)
Extreme half-life (approx 8-9 days) means it stacks significantly in the blood over weeks. Do not increase dose rapidly.
0.25-0.5 mg
Daily
01

How it works

Tesofensine is a triple monoamine reuptake inhibitor:

Norepinephrine Reuptake Inhibition

Increases synaptic NE - drives sympathetic activation, energy expenditure, and appetite suppression.

Dopamine Reuptake Inhibition

Increases synaptic DA in reward and appetite circuits - reduces hedonic feeding drive.

Serotonin Reuptake Inhibition

Modest 5-HT effect contributes to appetite suppression and satiety.

Net Effect

Substantial appetite reduction + modest energy expenditure increase = up to 12% weight loss at 1mg daily in TIPO-1 trial.

Cardiovascular Side Effects

NE/DA reuptake inhibition raises HR and BP - dose-limiting at higher doses. Tesomet combination with metoprolol (beta-blocker) mitigates this in Mexican formulation.

CNS Side Effects

Insomnia, dry mouth, nausea, anxiety - all class-typical for triple reuptake inhibitors.

02

What to expect

Early
Days 1–7

Days 1-7: rapid appetite suppression onset.

Mid
Weeks 2–4

Weeks 4-12: peak weight loss (up to ~12% at 1mg).

Later
Weeks 4–12

Long-term: efficacy beyond 24 weeks not well characterized.

03

Evidence

HumanPresent
AnimalPresent
In-vitroPresent

Each reference below was re-fetched from its PubMed record, and the quoted sentence was confirmed to appear in that abstract and to support the claim it sits under. Follow any of them to read the source.

Exact-molecule evidence boundary: the live abstract reports the quoted finding for Tesofensine; no broader inference is made.

We assessed the efficacy and safety of tesofensine-an inhibitor of the presynaptic uptake of noradrenaline, dopamine, and serotonin-in patients with obesity.

Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet (London, England) · 2008 · PMID 18950853

Evidence scope. Exact molecule wording appears in the quoted live sentence. Only the population/model, formulation, route, and outcome expressly stated there are supported.

Claims we could not support

No abstract we checked supports these for this molecule at this route. That is not the same as saying they are false — it marks where the evidence is missing.

Dose/route: 0.25mg daily; Oral capsule; 1x daily. No selected live abstract sentence verified this complete regimen.

Mechanism as written in source JSON. No selected live abstract sentence verified the complete mechanism at the card formulation/route and relevant population/model.

Primary safety claim as written in source JSON. No selected live abstract sentence verified the complete safety claim for this exact formulation and route.

04

Side effects & safety

Commonly reported

  • Dry mouth
  • Insomnia
  • Nausea
  • Anxiety
  • Elevated heart rate
  • Mild blood pressure elevation

Less common & notes

  • Severe tachycardia, hypertension.
  • Mood/psychiatric effects (mania-like in susceptible).
  • Long-term safety beyond 24 weeks limited.
  • Cardiovascular events at higher doses are the primary concern.
05

Pharmacokinetics

Illustrative plasma concentration · 36 d
Half-life
~9 days

Long

Peak · Tmax
8-10 hours

Post-ingestion

Elimination

Steady state achieved over weeks

Bioavailability

Oral high (~90%)

Duration of action

Daily dosing maintains steady state

Clearance

Hepatic

Storage. Capsule. Cool dry location.

06

Regulatory status

Approved in Mexico (Tesomet, 2023) for obesity and Prader-Willi syndrome. NOT FDA-approved. Available outside Mexico as research chemical.

Put it to work

Calculate, log & track

Open Tesofensine straight into OnePin with your vial and dose pre-filled, then let it handle the syringe math and remind you before the vial runs out.

Open Tesofensine in the app →

Go deeper

The guide & community

The complete Tesofensine walkthrough, real protocol discussion and coaching live inside the BlessUp community on Skool.

Join the community ↗
Open in app Community

Track it in OnePin. Log vials, draws, and protocols in the app.