Tesofensine

A triple monoamine reuptake inhibitor (SERT IC₅₀ 11 nM, NET 1.7 nM, DAT 65 nM) of the phenyltropane family, originally developed by NeuroSearch for neurodegeneration. Acquired by Saniona (2014), sublicensed to Medix for Mexico/Argentina (2016). Phase 2: 0.5 mg achieved 9.2% placebo-subtracted weight loss (Astrup et al., Lancet 2008). Viking Phase 3 (372 patients, 24 weeks) completed Dec 2018. COFEPRIS favorable opinion Feb 2023 but approval withheld Nov 2024.

Moderate evidence Investigational Metabolic

Written by WhatPeptide Editorial Team · Last updated 2026-03-18

Currently in clinical trials — not yet approved for any indication.

Half-life

Parent compound: ~9 days (~220 hours); active metabolite: ~16 days. CYP3A4-mediated metabolism

Dosage range

0.25-0.5 mg once daily oral. Tesomet (PWS): tesofensine 0.5 mg + metoprolol 50 mg

Administration

Oral

Research level

Moderate

How Tesofensine works

Inhibits presynaptic reuptake of serotonin, norepinephrine, and dopamine, increasing synaptic concentrations. Suppresses appetite via serotonergic and dopaminergic satiety signaling, increases thermogenesis via noradrenergic activation, and enhances satiety signaling in the hypothalamus.

Also known as: NS-2330, Tesomet (tesofensine + metoprolol)

Research relevance

Fat Loss

Moderate relevance 75

Side effects & safety

Dry mouth Insomnia Constipation Heart rate increase (up to ~8 bpm at 0.5 mg) Elevated blood pressure

Contraindications

Uncontrolled hypertension

History of cardiac arrhythmia

Concurrent use of MAO inhibitors or other monoamine reuptake inhibitors

Pregnancy

Consult a healthcare provider before use if any of these apply to you.

FAQ

What is Tesofensine? +

What is Tesofensine researched for? +

Tesofensine has the strongest research relevance for Fat Loss. Evidence is supported by moderate clinical and preclinical evidence.

What are the side effects of Tesofensine? +

Reported side effects include Dry mouth, Insomnia, Constipation, Heart rate increase (up to ~8 bpm at 0.5 mg), Elevated blood pressure. Key contraindications: Uncontrolled hypertension; History of cardiac arrhythmia; Concurrent use of MAO inhibitors or other monoamine reuptake inhibitors; Pregnancy.

Is Tesofensine FDA approved? +

Tesofensine is currently in clinical trials and is not yet approved by the FDA.

How is Tesofensine administered? +

Tesofensine is typically administered via oral route. Researched dosage range: 0.25-0.5 mg once daily oral. Tesomet (PWS): tesofensine 0.5 mg + metoprolol 50 mg. Half-life: Parent compound: ~9 days (~220 hours); active metabolite: ~16 days. CYP3A4-mediated metabolism.

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