A novel small-molecule triple monoamine reuptake inhibitor that simultaneously blocks reuptake of serotonin, dopamine, and norepinephrine — originally developed as an anti-Parkinson agent before its pronounced appetite-suppressing effects were observed. The TIPO-1 phase II trial demonstrated up to 12.8% mean weight reduction at 24 weeks with the 1.0 mg dose. Its exceptionally long half-life (~220 hours) produces steady-state plasma concentrations within 2–3 weeks of daily dosing.
Research Profile
StructureSmall molecule (~383 Da) — not a peptide
TargetsSERT, DAT, NET (serotonin, dopamine, norepinephrine transporters)
Research FocusCentral appetite regulation, thermogenesis, monoamine pharmacology, obesity models
ReconstitutionNo reconstitution — oral capsules
StabilityRoom temperature, dry storage
Key distinction: Only triple monoamine reuptake inhibitor specifically studied for metabolic research — the dopamine component distinguishes it from SSRIs and SNRIs by addressing reward-driven eating behavior.
Scientific Evidence
Published Research
[1]
Astrup A et al. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients (TIPO-1). Lancet 2008;372:1906-1913 — PubMed 18950853
[2]
Appel L et al. In vivo PET imaging of tesofensine: monoamine transporter occupancy. J Nucl Med 2014;55:1436-1441 — PubMed 25071093
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