EvanMan
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You guys heard of this? Seems to kill appetite like no other.
I noticed there is a company selling it, and a guy repping it on another forum. Have not seen it brought up much here.
Half life of 9 days...damnnn
I noticed there is a company selling it, and a guy repping it on another forum. Have not seen it brought up much here.
Half life of 9 days...damnnn
Source: WikipediaTesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity.[1] Tesofensine was originally developed by a Danish biotechnology company, NeuroSearch, who transferred the rights to Saniona in 2014.[2]
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.[1]
History:
Tesofensine was originally investigated for the treatment of Alzheimer's disease and Parkinson's disease,[3] and was subsequently dropped from development for these applications after early trial results showed limited efficacy for treatment of these diseases.[4][5] However, weight loss was consistently reported as an adverse event in the original studies, especially in overweight or obese patients.[6] Therefore, it was decided to pursue development of tesofensine for the treatment of obesity.
Tesofensine primarily acts as an appetite suppressant, but possibly also acts by increasing resting energy expenditure.[7] Phase 2 trials for the treatment of obesity have been successfully completed.
Tesofensine has a long half-life of about 9 days (220 h)[3] "and is mainly metabolized by cytochrome P4503A4 (CYP3A4) to its desalkyl metabolite M1" NS2360.[8][9] 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%).
Phase 2b trial (TIPO-1) results reported in The Lancet[17] showed levels of weight loss over a 6-month period that were significantly greater than those achieved with any currently available drugs. Patients lost an average of 12.8 kg on the 1 mg dose, 11.3 kg on the 0.5 mg dose and 6.7 kg on the 0.25 mg dose, compared with a 2.2 kg loss in the placebo group.
All participants were instructed to follow a diet with a 300 kcal deficit and to increase their physical activity gradually to 30–60 minutes of exercise per day. The placebo-subtracted mean weight losses were 4.5%, 9.2% and 10.6% in the 0.25 mg, 0.5 mg and 1 mg dose groups, respectively. This is approximately twice the weight loss produced by medications currently approved by the US Food and Drug Administration (FDA) for the treatment of obesity.
NeuroSearch has also reported interim results[7] from a 48-week, open-label, extension trial (TIPO-4) in which 140 patients who completed the 24-week phase 2b trial (TIPO-1) were re-enrolled after an average of 3 months’ wash-out. All were initially treated with 0.5 mg tesofensine once daily but up-titration to 1.0 mg once daily was allowed in the first 24 weeks of the extension study. At this time point, all subjects were continued on the 0.5 mg dose for an additional 24 weeks. The 24-week interim results for those who were previously treated with tesofensine 0.5 mg in TIPO-1 showed a total mean weight loss of between 13 kg and 14 kg over 48 weeks of treatment. Furthermore, TIPO-4 confirmed the TIPO-1 results since those patients who were previously treated with placebo lost approximately 9 kg in the first 24 weeks of the TIPO-4 study.