OT: Anti-Obesity Drug that I've been working on enters clinic

[Randy Holmes-Farley]

The anti-obesity drug that I've been working on for a number of years has just entered human clinical trials. Here are the press releases:

http://www.peptimmune.com/pep080904.htm

"Peptimmune Announces Start of Phase I Trial for Obesity

August 9, 2004

CAMBRIDGE, Mass. - 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. "

and

http://www.peptimmune.com/pep051004.htm

"Peptimmune is Granted Exclusive License from Genzyme to Develop and Commercialize Treatment for Metabolic Diseases including Obesity

May 10, 2004

CAMBRIDGE, Mass. - Genzyme Corporation and Peptimmune, Inc. today announced that Genzyme has granted an exclusive worldwide license to Peptimmune to develop and market a Genzyme investigational drug candidate for the treatment of obesity and other metabolic disease indications. Peptimmune plans to file an IND with the U.S. Food and Drug Administration to begin clinical trials of the drug later this year.

Under the agreement, Genzyme grants Peptimmune exclusive rights to develop, manufacture and commercialize GT389-255, in exchange for royalties, in addition to shared milestones and payments if the program is partnered further. Financial details were not disclosed.

"The acquisition of a product in the metabolic disease field that could enter the clinic in 2004 broadens and diversifies Peptimmune's pipeline," stated Tom Mathers, president of Peptimmune. "It accelerates our evolution from a research and discovery stage company, to a fully integrated biopharmaceutical company. The prospect of a new treatment for obesity offers hope for the millions of people suffering from this worldwide epidemic."

The investigational drug candidate, GT389-255, has a dual mechanism of action, serving as a pancreatic lipase inhibitor and a fat-binder. It acts within the gastro-intestinal tract to prevent fat digestion and is expected to have fewer side-effects than currently marketed therapies. GT389-255 has been evaluated in a number of preclinical studies, including investigational new drug-enabling toxicology studies.

"We have discovered a very innovative treatment for obesity that has the potential to address a very serious and growing worldwide public health problem," stated Ted Sybertz, Ph.D., senior vice president and general manager of Genzyme Drug Discovery and Development. "However, because of its broad physician call-point, obesity is not a strategic fit for Genzyme. Given Peptimmune's experienced management team, clinical development expertise in both autoimmune and metabolic disease, and their commitment to moving this program forward, we think they are an excellent partner."

The Genzyme drug discovery effort that developed the anti-obesity program has drawn upon the company's extensive expertise in developing compounds to treat metabolic disease and its world-renowned reputation in polymer chemistry. Two polymer products have been brought to market, Renagel® (sevelamer hydrochloride), a calcium-free, metal-free phosphate binder for patients with end-stage renal disease, and WelChol® (colesevelum hydrocholoride), a cholesterol-lowering agent. A third polymer, tolevamer, has recently completed Phase 2 clinical trials for the treatment of C. difficile associated diarrhea. These polymer therapies are not absorbed and all act within the GI tract.

Obesity - An Expanding Epidemic

Obesity is a global healthcare issue that is associated with an increased risk of serious metabolic diseases, including cardiovascular disease, Type 2 diabetes, hypertension, stroke, dyslipidemia, and osteoarthritis. Published prevalence rates indicate that more than 180 million people in the United States and Europe are obese, and the number of obese individuals continues to increase dramatically worldwide. A 1999 article published in the Journal of the American Medical Association estimates that there are some 300,000 deaths per year in the United States that are attributed to overweight and obesity. According to data released by the U.S. Department of Health and Human Services, the direct medical costs to the U.S. population that were attributed to obesity totaled $117 billion in 2000.

About Genzyme

Genzyme Corporation is a global biotechnology company dedicated to making a major positive impact on the lives of people with serious diseases. The company's broad product portfolio is focused on rare genetic disorders, renal disease, osteoarthritis and immune-mediated diseases, and includes an industry-leading array of diagnostic products and services. Genzyme's commitment to innovation continues today with research into novel approaches to cancer, heart disease, and other areas of unmet medical need. More than 6,300 Genzyme employees in offices around the globe serve patients in over 80 countries.

About Peptimmune

Peptimmune, Inc. is a privately held biotechnology company focused on development of therapeutics for the treatment of autoimmune and metabolic diseases. The company is led by an experienced management team with a track record of building commercial biotechnology companies. Peptimmune has one product in clinical trials for the treatment of pemphigus vulgaris, and a pipeline of late stage preclinical products for the treatment of autoimmune and metabolic diseases including, multiple sclerosis, rheumatoid arthritis and obesity. For information, access our website at http://www.peptimmune.com. "