Does Tesofensine actually work?

Tesofensine is a novel triple monoamine reuptake inhibitor (SNDRI) that affects appetite and metabolism by regulating neurotransmitter levels. Tesofencin was originally developed by Danish pharmaceutical company NeuroSearch and has now been licensed to other companies for further scientific research and commercialization.

Its chemical name is (1R)-1-{3-[(3S)-3-(dimethylamino)-2-methylpropyl]phenyl}-2,3,4,9-tetrahydro-1H-pyridino[3,4-b]indole, with a white appearance to a white crystalline powder. It is soluble in organic solvents (such as DMSO, ethanol), and has poor water solubility. Because it is susceptible to humidity and oxidation, it needs to be kept away from light, sealed and stored at 2-8°C to prevent degradation. In this regard, Xi'an Tongze Bio can provide sealed packaging for vial and aluminum foil bags.

1. Treatment of obesity

Tesofensine works through triple monoamine reuptake inhibition (SNDRI) and is mainly for triple neurotransmitter regulation, including dopamine (DA), norepinephrine (NE), and serotonin (5-HT).

1) Suppress appetite

Through 5-HT (serotonin) elevation, POMC neurons in the hypothalamus are activated, thereby enhancing the effect of satiety

Then again increase by DA (dopamine), which reduces the "craving" for high sugar and high fat foods

2) Promote fat burning

Through the increase of NE (norepinephrine), β3-adrenaline receptors are activated, thereby promoting fat decomposition, reducing fasting blood sugar and triglycerides, and improving basal metabolic rate.

Suitable for patients with simple obesity with BMI ≥30 kg/m² or patients with BMI ≥27 kg/m² and with at least one metabolic complication (hypertension, type 2 diabetes, dyslipidemia). It is recommended to take oral capsules of related products. The dosage is the starting dosage: 0.25 mg/day, and gradually adjust it to 0.5 mg-1 mg/day according to the doctor's advice. It usually takes 3-6 months to achieve significant weight loss effect.

2. Exploration of neurological diseases

For Alzheimer's/Parkinson's disease research, it improves cognitive function and execution ability by increasing dopamine and norepinephrine levels. Due to the side effects that occur during weight loss, we have conducted a deep research direction on this.

The commonly accepted forms of Tesofensine include powder and capsules. At the same time, Xi'an Tongze Biological can provide OEM/ODM customized services, from raw materials to packaging, private labels, and then to capsules.We have a regular production line and can provide one-stop service.

1. Common side effects, related to activation of the sympathetic nervous system, symptoms such as dry mouth, insomnia, too fast heart rate, and increased blood pressure. It also has an impact on the digestive system, and it may cause constipation and nausea.

2. Severe adverse reactions

On the impact of the cardiovascular system, hypertension crisis and arrhythmia will occur.

For neurological effects, especially when combined with SSRI/SNRI antidepressants, high fever, myoclonus, and confusion will occur.

3. Special groups

Including patients with cardiovascular disease, mental illness, pregnant women and breastfeeding, pregnant women and breastfeeding. Especially for patients with cardiovascular diseases, taking Tesofensine-related products will cause a history of myocardial infarction/stroke and have high risk of not controlling hypertension.

Tesofensine is better than the existing drugs Semaglutide, etc., and needs to be strictly followed by the dosage. It must be taken for a long time and the weight loss effect must be significant within 6 months. Therefore, for obese patients, Tesofensine is clearly effective in short-term (within 6 months) weight loss and metabolic regulation.

1.Tesofensine, a novel triple monoamine reuptake inhibitor, induces appetite suppression by indirect stimulation of α1-adrenoceptor and dopamine D1 receptor pathways in the diet-induced obese rat

2.Tesofensine induces appetite suppression and weight loss through inhibition of serotonin, noradrenaline and dopamine reuptake

3.Controversies in the cardiometabolic risk associated with anti-obesity pharmacotherapy

Journal： Current Atherosclerosis Reports

4.Pharmacotherapy for Obesity: New Drugs and Emerging Targets
Journal： Circulation Research