THE SCALE OF THE PROBLEM
More than two billion people worldwide are overweight and 600 million morbidly obese, representing an immense opportunity for the pharmaceutical industry. The US is presently the biggest market for weight loss drugs with around 68% of its population being either overweight or obese. The US is followed by the UK and other European countries. In future, emerging economies such as China, Russia, India and Brazil are also expected to become a huge market for weight loss products. With China’s obesity and overweight levels predicted to be in region of 665-670 million people in 2015, this country will emerge as the most potential weight loss market. Many public health experts classify the rise in obesity as an epidemic. Largely as the result of increased risk for diabetes and cardiovascular disease, obesity carries an increased risk of premature death.
Because of the enormous market potential much pharmaceutical industry interest exists. However, there have been many failures, either in getting registration approval or reimbursement. Furthermore, some products have been withdrawn because benefits do not outweigh the risks. For example, Acomplia, a cannabinoid CB2 receptor antagonist, has been suspended from the US and European two and a half years after its launch due the overt risk of serious psychiatric disorders. Furthermore, the majority of weight loss products currently marketed have proven to be relatively ineffective, with only a small proportion of consumers having been able to achieve and maintain weight loss. Only two drugs are approved in the United States for long-term treatment of obesity: these being the serotonin-noradrenaline uptake inhibitor sibutramine (Abbott’s Meridia/Reductil) and the pancreatic lipase inhibitor orlistat (Roche’s Xenical and GlaxoSmithKline’s low-dose, over-the-counter form, alli). Both are minimally effective and have significant side effects, which tend to discourage their use.
There are many pharmacological strategies currenly in development. These include melanocortin receptor agonists, neuropeptide Y (NPY) receptor antagonists, melanin-concentrating hormone receptor antagonists, Protein Tyrosine Phosphatase 1B inhibitors, adenosine monophosphate-activated protein kinase (AMPK) activators, ghrelin recptor antagonists, drugs that increase energy utilization in peripheral tissues, pharmacological exercise mimetics and increasing brown adipose tissue.
Vastrata’s approach is an NCE based programme in collaboration with structural biology and medicinal chemistry collaborators.