Grade: Pharmaceutical Grade
CAS NO.: 402856-42-2
Molecular Formula: C17H23Cl2NO
Molecular weight: 328.277
Flash Point: 193.675 °C
Boiling Point: 396.629 °C at 760 mmHg
Density: 1.162 g/cm3
Tesofensine is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity. As of 2015, tesofensine has been discontinued for the treatment of Alzheimer's and Parkinson's disease but is in Phase II clinical trials for obesity.
Tesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity. Tesofensine was originally developed by a Danish biotechnology company, NeuroSearch, who transferred the rights to Saniona in 2014.
Tesofensin's main function is to prevent the intake of fat in the human diet by acting as a lipase inhibitor, thereby reducing calorie intake. It is designed to be used in conjunction with a low calorie diet supervised by a health care provider.
Metabolism and half-life
Tesofensine has a long half-life of about 9 days (220 h) "and is mainly metabolized by cytochrome P4503A4 to its desalkyl metabolite M1" NS2360. NS2360 is the only metabolite detectable in human plasma.
NS2330 is mainly metabolized by cytochrome P450 3A4 (CYP3A4) into .
It has a longer half-life than tesofensine, i.e. approximately 16 days (374 h) in humans, and has an exposure of 31–34% of the parent compound at steady state. In vivo data indicate that NS2360 is responsible for approximately 6% of the activity of tesofensine. As in animals, the kidney appears to play only a minor role in the clearance of tesofensine in humans (about 15–20%).
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