195875-84-4

Tesofensine ((1R, 2R, 3S, 5S)-3-(3, 4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane)) is an inhibitor of neuronal reuptake of dopamine, noradrenaline, and serotonin. Tesofensine was developed for the treatment of Alzheimer's and Parkinson's disease but lacked efficacy. Meta-analysis revealed that tesofensine (0.125–1.0 mg, once daily; oral) produced dose-dependent weight loss, and 32% of obese patients had ≥ 5% weight loss following 14 wk of treatment. Weight loss was accompanied by hypophagia, suggesting an appetite suppressant action[2].

Tesofensine is a dopamine, serotonin, and noradrenaline (triple) reuptake inhibitor originally developed by NeuroSearch for the treatment of Alzheimer's disease and Parkinson's disease. Development of the compound for these neurological indications was unsuccessful but significant weight loss was reported during the clinical trials in Parkinson's disease. Hence, tesofensine is now being developed by NeuroSearch for the treatment of obesity and type 2 diabetes[1].

Tesofensine, is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is currently in clinical development for the treatment of obesity.

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[1] Dourish, C. J. Wilding and J. Halford. “Anti-obesity Drugs: From Animal Models to Clinical Efficacy.”Animal and Translational Models for CNS Drug Discovery 2008: 271-315.
[2] Vidya Narayanaswami, Linda P. Dwoskin. “Obesity: Current and potential pharmacotherapeutics and targets.” Pharmacology Therapeutics 170 (2017): Pages 116-147.