Tesofensine (NS2330) is a serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity. R
1. Helps with Weight Loss
Phase 2b trial (TIPO-1) results showed levels of weight loss over a 6-month period that were significantly greater than those achieved with any currently available drugs. R
Tesofensine also indirectly potentiates cholinergic neurotransmission. R
This has been proven to have beneficial effects on cognition, particularly in learning and memory. R
3. Anti-Depressant Effects
Sustained treatment with tesofensine has been shown to increase BDNF levels in the brain, and may possibly have an antidepressant effect. R
Tesofensine has a long half life of about 9 days (220h). R
NS2360 has a longer half-life than tesofensine, 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%).