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Current research and future hope
Published in G. Michael Steelman, Eric C. Westman, Obesity, 2016
Greenway Frank L., R. Smith Steven
Tesofensine is a norepinephrine, dopamine, and serotonin reuptake inhibitor that was being developed for the treatment of Parkinson’s and Alzheimer’s diseases, and weight loss was noted in the clinical trials (78). A 24-week trial randomized 203 obese subjects to 0.25, 0.5, 1, or placebo once a day; weight loss was 6.8%, 11.4%, 12.7%, and 2.3%, respectively (79,80). This efficacy is greater than for presently approved single obesity pharmaceuticals, but the elevations in blood pressure and heart rate are a cause for concern and led to discontinuation of development.
Obesity
Published in Philip E. Harris, Pierre-Marc G. Bouloux, Endocrinology in Clinical Practice, 2014
Ahmed Yousseif, Efthimia Karra, Sofia Rahman, Rachel L. Batterham
Tesofensine is a presynaptic inhibitor of norepinephrine, dopamine, and serotonin originally developed for the treatment of Parkinson’s disease. Although its efficacy was limited for this application, study subjects were noted to experience significant weight loss. The efficacy and safety of tesofensine require further investigation.
Anorectic state of obesity medications in the United States. Are leaner times ahead?
Published in Expert Opinion on Pharmacotherapy, 2020
Another combinational therapy under investigation is tesofensine/metoprolol for the management of hypothalamic injury-induced obesity (NCT03845075) and Prader-Willi syndrome (NCT03149445). Tesofensine is a novel monoamine reuptake inhibitor (dopamine> norepinephrine> serotonin) that was developed by NeuroSearch A/S in collaboration with Boehringer Ingelheim [20]. A 24-week phase II trial (NCT00394667) in obese patents (BMI ≥ 30 kg/m2; n = 203; 68-74% female) compared three doses of tesofensine (oral daily) with placebo [21]. The placebo-subtracted mean weight loss was 4.5% for 0.25 mg, 9.2% for 0.5 mg, and 10.6% for 1.0 mg (p < 0.0001 for all doses from placebo) [21]. All doses of tesofensine significantly increased heart rate (placebo-subtracted): +4.3 bpm for 0.25 mg (p < 0.0018 from placebo), +7.4 bpm for 0.5 mg (p < 0.0001 from placebo), and 8.1 bpm for 1.0 mg (p < 0.0001 from placebo) [21]. Despite the promising weight loss reported in the phase II trial, an audit by the Danish Health and Medicine Authority revealed that subjective TEAEs and reasons for discontinuation were underreported [22]. There were also some questions regarding the integrity of the blinding procedure and the process of informed consent [23]. Nonetheless, preclinical studies have suggested that metoprolol blocks the adverse cardiovascular effects of tesofensine while preserving the feeding-suppressive effects of the drug in rats [24].
Obesity medications in development
Published in Expert Opinion on Investigational Drugs, 2020
Candida J. Rebello, Frank L. Greenway
Tesofensine (Saniona) is an inhibitor of the presynaptic uptake of noradrenaline, dopamine, and serotonin that was originally developed for the treatment of Parkinson’s and Alzheimer’s diseases, but it did not meet the efficacy criteria [88–91]. However, the unintended weight loss caused by Tesofensine treatment led to its development as an anti-obesity medication. Tesofensine causes a small increase in metabolic rate but it appears to induce weight loss primarily through a reduction in food intake [92,93].