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 1,300 patients and is well tolerated.

The clinical Phase 2b trial (TIPO-1), reported in The Lancet, shows levels of weight loss over a six-month period that is 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. In August 2017, Medix initiated a Phase 3 study for tesofensine in obese Mexican patients and recruitment was completed in January 2018. The trial is expected to be completed in 2018 and topline data is expected by early 2019.