Tesofensine monotherapy for treatment of obesity

Tesofensine, a triple monoamine reuptake inhibitor, is positioned for obesity. Tesofensine has been evaluated in Phase 1 and Phase 2 human clinical studies with the aim of investigating treatment potential with regards to obesity, Alzheimer’s disease and Parkinson’s disease. Tesofensine demonstrated strong weight reducing effects in Phase 2 clinical studies in obese patients. In general, tesofensine has been administered to more than 1,200 patients and is well tolerated.

The clinical Phase 2b trial (TIPO-1), reported in The Lancet, showed levels of weight loss over a six-month period that were of high clinical relevance and highly competitive to other approaches. Patients lost an average of 12.8 kg on a 1 mg dose, 11.3 kg on a 0.5 mg dose and 6.7 kg on a 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. Of the patients receiving 0.5 mg daily, considered the relevant therapeutic dose, 87% of the patients (58% versus placebo) achieved more than 5% weight loss and 53% of the patients (46% versus placebo) achieved a weight loss of more than 10% after 6 months follow up. There has also been reported interim results 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 three months’ wash-out. All were then treated with 0.5 mg tesofensine once daily but up-titration to 1 mg once daily was allowed in the first 24 weeks of the extension study. The 24-week interim results for those who were previously treated with 0.5 mg tesofensine 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 the patients who were previously treated with placebo lost additionally approximately 9 kg in the first 24 weeks of the TIPO-4 study.

Saniona is collaborating with Medix on developing tesofensine for obesity in Mexico and Argentina. According to Medix, the current market for prescription medicine for obesity in Mexico is about US$ 250 million. Medix has filed a clinical trial application in Mexico for the initiation of a Phase 3 study for tesofensine in obese Mexican patients.