Peptimmune, Inc. a privately held biotechnology company, announced that physicians have treated the first participant in a clinical trial to evaluate the safety, tolerability and pharmacokinetics of GT389-255, a lipase inhibitor conjugated to a fat binding polymer for the treatment of obesity.
The Phase I single ascending dose (SAD) double blind placebo controlled randomized study will involve 48 healthy male volunteers who will receive the drug in six escalating dose cohorts. Later in 2004, the SAD study will be followed by a multiple ascending dose Phase I study (MAD). If Phase I development is successful, Peptimmune anticipates launching a Phase II trial in patients with obesity in 2005.
GT389-255 is a novel conjugate of a pancreatic lipase inhibitor and a fat binding hydrogel polymer. It acts within the gastro-intestinal tract to prevent fat digestion and is expected to have fewer side-effects than currently marketed therapies. The reduction in caloric intake and lowering of fat absorption may lead to weight loss, with potential concomitant improvement in both diabetic and cardiovascular risk profiles. GT389-255 has been evaluated in a number of preclinical studies, including investigational new drug-enabling toxicology studies. Peptimmune licensed GT389-255 from Genzyme Corporation earlier this year.
"The commencement of this clinical trial is an important milestone for the development of GT389-255 and for the company," stated Thomas Mathers, President of Peptimmune. "The goal for GT389-255 is the development of a lipase inhibitor/fat binder that provides inhibition of fat absorption and associated weight loss, but mitigates the gastrointestinal side effects associated with undigested trigylerides in the colon."
Obesity is nearing epidemic proportions in the developed world. The prevalence of obesity is increasing worldwide, with 2003 World Health Organization estimates that over 300 million people are affected. Since 1980, the number of adults in the US has doubled and the number of obese teens has tripled. Obesity is associated with an increased risk of serious metabolic diseases, including cardiovascular disease, Type 2 diabetes, hypertension, stroke, dyslipidemia, and osteoarthritis. Approximately 300,000 deaths per year are attributed to being overweight or obese. Obesity exerts a significant burden on the health care system.
Diet and exercise alone have failed to treat this growing epidemic. Currently approved pharmacological therapies for weight loss have had limited success due to insufficient efficacy and burdensome, unpleasant side effects and safety concerns. New therapies with improved tolerability and fewer side effects are needed not only to treat obesity, but also to prevent the significant co-morbidities associated with it, such as diabetes, hypertension and cardiovascular disease.