SavePeptides
SavePeptidesCompound
Re-checked hourly
All peptides
Weight LossFDA-approvedVendors pending
FDA-approvedVendors pendingFacts verified · 2026-05-25

Tesofensine (oral tablets)

Also known as Tesofensine (Tablets), ns2330, sndri, serotonin–norepinephrine–dopamine reuptake inhibitor · Wikipedia

Tesofensine (NS2330) is a phenyltropane-class triple monoamine reuptake inhibitor (SNDRI) blocking dopamine, norepinephrine, and serotonin transporters. It is NOT a peptide. Originally developed for Parkinson's disease and Alzheimer's disease (where it failed efficacy endpoints), it produced unexpectedly large weight loss in trial participants and was subsequently developed for obesity by Saniona. The Phase II Astrup et al. 2008 trial showed up to ~10.6% weight loss at 24 weeks on 1 mg/day - among the largest single-agent effects in appetite-suppression history (https://pubmed.ncbi.nlm.nih.gov/18950853/). Tesofensine (as Tesomet, a fixed combination with metoprolol) is approved in Mexico via Medix for obesity but is NOT FDA-approved.

—

best

price

—

per

mg

—

vendors

tracked

FDA-approved

stage

Vendor data

Coming soon.

Per-vendor pricing and verification tiers populate as the SavePeptides crawler comes online. Until then, browse all approved vendors directly.

Browse all vendors

Mechanism of action

Tesofensine is a small-molecule phenyltropane triple monoamine reuptake inhibitor that blocks the dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters in the CNS, elevating synaptic levels of all three monoamines. Appetite suppression appears to be mediated primarily via hypothalamic and mesolimbic circuits - rodent in-vivo electrophysiology shows tesofensine silences GABAergic neurons in the lateral hypothalamus and indirectly activates alpha-1 adrenoceptor and dopamine D1 receptor pathways (https://pmc.

Tesofensine is a small-molecule phenyltropane triple monoamine reuptake inhibitor that blocks the dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters in the CNS, elevating synaptic levels of all three monoamines. Appetite suppression appears to be mediated primarily via hypothalamic and mesolimbic circuits - rodent in-vivo electrophysiology shows tesofensine silences GABAergic neurons in the lateral hypothalamus and indirectly activates alpha-1 adrenoceptor and dopamine D1 receptor pathways (https://pmc.ncbi.nlm.nih.gov/articles/PMC11042726/, https://pmc.ncbi.nlm.nih.gov/articles/PMC3055463/). Modest increases in resting energy expenditure and satiety contribute additionally. Tesofensine is structurally and mechanistically distinct from incretin-based weight-loss agents and is fully orally bioavailable as a small molecule, unlike peptides such as semaglutide.

Pharmacokinetic properties

Half-life

~9 days (very long; allows once-daily dosing with prolonged accumulation)

Routes

oral

Bioavailability

Small molecule with high oral bioavailability. Long half-life means steady-state takes 4-8 weeks; effects and side effects accumulate over time.

Amino-acid sequence

(Not a peptide; phenyltropane SNDRI)

Use & research dosing

Appetite ControlMetabolic SupportEnergy ExpenditureWeight LossEnergy

The pivotal Astrup et al. 2008 Phase II trial (TIPO-1) randomized obese adults to 0.25, 0.5, or 1.0 mg orally once daily versus placebo for 24 weeks, with respective mean weight losses of 4.5%, 9.2%, and 10.6% on a 500-kcal-deficit diet (https://pubmed.ncbi.nlm.nih.gov/18950853/). Mexican approval of Tesomet (tesofensine + metoprolol) is at 0.5 mg/day tesofensine. Saniona Phase III in hypothalamic obesity uses 0.5 mg/day (https://pmc.ncbi.nlm.nih.gov/articles/PMC9625380/). Community/research-source dosing typically starts at 0.25 mg daily and may titrate to 0.5-1.0 mg, recognizing that the ~9-day half-life means steady-state and side effects accumulate over 4-8 weeks.

Research-use framing only. SavePeptides sells nothing for human consumption. Doses above reflect reported research / self-experimentation ranges, not clinical recommendations.

Editorial perspective

Tesofensine is not a peptide despite being sold on peptide-research marketplaces. The Phase II efficacy signal (~12.8% placebo-subtracted weight loss at 1.0 mg over 24 weeks) is among the largest single-agent results in the obesity literature, but development has been slowed by cardiovascular signals (heart-rate elevation) and psychiatric AEs (mood changes, insomnia) at the higher doses. The very long ~9-day half-life is a unique pharmacology landmine: dose changes take many weeks to fully manifest, and side effects persist long after stopping. Saniona's Tesomet (fixed-dose tesofensine + metoprolol) is the path to manage the cardiovascular signal in current trials.

— SavePeptides editorial desk · last updated 2026-05-25

Cautions & contraindications

Before researching this compound, note:

  • Not a peptide - small-molecule SNDRI with stimulant-class pharmacology
  • Not FDA-approved; approved only in Mexico (Tesomet) and select jurisdictions
  • Dose-dependent increases in heart rate (~7-8 bpm at 0.5 mg) and blood pressure (1-5 mmHg); avoid in uncontrolled hypertension, arrhythmia, recent MI, or significant cardiovascular disease
  • Psychiatric adverse events: insomnia, depressed mood, anxiety, irritability, and dose-dependent increases in anger/hostility and confusion at 1 mg (https://pmc.ncbi.nlm.nih.gov/articles/PMC4125319/)
  • Contraindicated with concurrent MAO inhibitors and within 14 days of MAOI discontinuation
  • Caution or avoid with SSRIs, SNRIs, triptans, tramadol, and other serotonergic agents (serotonin syndrome risk)
  • Caution with other stimulants, sympathomimetics, and DAT-active drugs - additive cardiovascular and psychiatric effects, potential abuse liability via DAT inhibition
  • Contraindicated in pregnancy and breastfeeding
  • Very long ~9-day half-life means dose changes take 4-8 weeks to reach new steady state; adverse effects persist weeks after discontinuation
  • GI: dry mouth, nausea, constipation, hard stools, diarrhea (most common AEs in Phase II)

Research foundation

The papers behind the page.

  1. [01]https://pubmed.ncbi.nlm.nih.gov/18950853/
  2. [02]https://pubmed.ncbi.nlm.nih.gov/19777399/
  3. [03]https://pmc.ncbi.nlm.nih.gov/articles/PMC9175551/
  4. [04]https://pmc.ncbi.nlm.nih.gov/articles/PMC9625380/
  5. [05]https://pmc.ncbi.nlm.nih.gov/articles/PMC11042726/

Facts verified

2026-05-25

Confidence

medium

What this means

  • not a peptide - small-molecule SNDRI
  • approved only in Mexico (Tesomet); not FDA-approved
  • 9-day half-life - dose changes accumulate over weeks

How we check →

Vendor data coming soon

All vendors

001 — Independent

We don't list what we wouldn't research.

SavePeptides lists vendors after an initial review and distinguishes verified vendors where additional checks have been completed. We may earn commissions from referral links, and sponsored placements will be clearly disclosed.

002 — Vendor-funded

Free to browse. Supported by referrals.

SavePeptides is free for buyers. We may earn a commission when you order through our links, but we do not lock deals behind a paywall, require an email to view codes, or inflate comparison prices.

003 — Research use

Research-use disclaimer.

SavePeptides surfaces vendor, pricing, and coupon information for research compounds. These products are not intended, approved, or recommended for human consumption. Our content is informational only and does not constitute medical advice.

Tesofensine (oral tablets) · SavePeptides