Peptides›Metabolic›Tesofensine

Tesofensine

/ Triple monoamine reuptake inhibitor (noradrenaline, dopamine, serotonin)

TIER 2 · TranslationalN = 0 · TESTING PENDINGLAST REVIEW 2026·04·20

ALIAS · NS2330

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Research use onlyAny dose figures below describe what specific cited studies used, reported factually. Nothing on this page is guidance for human use.READ FIRST →

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§ A · Identity

Primary sequence— sequence not captured —

MW · —CLASS · Triple monoamine reuptake inhibitor (noradrenaline, dopamine, serotonin)CATEGORY · Metabolic

Phase 2 obesity data (Astrup 2008) showed notable weight loss but cardiovascular adverse events slowed US development. Not FDA-approved.

§ B · Mechanism of action

Tesofensine is an oral non-peptide small molecule that inhibits reuptake of noradrenaline, dopamine, and serotonin. Originally developed for neurodegenerative disease, redirected toward obesity after incidental weight loss observations in early trials.

§ C · Human clinical evidence

Phase 2 RCT (Astrup 2008) in obesity reported -6.7% to -12.8% weight loss at tesofensine 0.25-1.0 mg daily vs -2.2% placebo over 24 weeks. Cardiovascular adverse events (heart rate, blood pressure) slowed US development. Approved in Mexico as Tesomet in 2023.

§ D · Primary literature

PubMed18950853Astrup A et al. — Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial · Lancet · human-phase-2Phase 2 RCT in obese patients: weight loss of -6.7% to -12.8% at tesofensine 0.25-1.0 mg daily vs -2.2% placebo over 24 weeks.Limitations: Cardiovascular adverse events (increased heart rate, blood pressure) caused program slowdown; not subsequently approved in the US.2008

§ F · Safety signal

Dose-dependent heart rate and blood pressure increases are the principal concern. Insomnia, dry mouth, and reduced appetite are common. Cardiovascular safety signal has slowed US development.

§ H · Regulatory status

Regulatory status

FDA status:: Not FDA-approved

§ I · Notable gaps and controversies

Tesofensine is a small molecule, not a peptide — inclusion in peptide-market catalogs is a distribution phenomenon. Not FDA-approved in the US. The cardiovascular signal distinguishes it from GLP-1 approaches now dominating obesity therapeutics.