Genaera Initiates Trial Of Type 2 Diabetes, Obesity Compound Trodusquemine
Study 103 is similar in design to the previously completed Study 101 which was conducted in healthy obese and overweight volunteers. The current study will continue to expand the safety database for MSI-1436 and establish the pharmacokinetics of the drug in a population of type 2 diabetics who are poorly controlled on metformin. The study will also evaluate a range of secondary endpoints including short-term insulin/glucose control indices, glucose tolerance and evaluation of insulin sensitivity.
"We have achieved another important milestone in the development of MSI- 1436 and can now begin collecting data from obese type 2 diabetics," said Jack Armstrong, President and Chief Executive Officer of Genaera. "The unique mechanism of action provides MSI-1436 with the potential to impact two of the key pathologies of type 2 diabetes: insulin resistance and obesity. We anticipate that this clinical study will provide a first step in demonstrating the safety of MSI-1436 in obese and overweight type 2 diabetics and will help determine an optimal therapeutic dose for this population."
This randomized, vehicle-controlled study, being conducted at dgd Research, Inc., a leading diabetes clinical research center in San Antonio, Texas, is enrolling otherwise healthy overweight and obese type 2 diabetic volunteers to evaluate the safety, tolerability, and pharmacokinetics of ascending single doses of intravenously administered MSI-1436 in this special population. The ascending single dose protocol will initially enroll approximately 28 subjects at four dose levels (3, 6, 10, and 15 mg/m2) and is expected to be completed late in the first half of 2008.
About Trodusquemine (MSI-1436)
Trodusquemine is a centrally and peripherally-acting appetite suppressant and the first highly selective inhibitor of protein tyrosine phosphatase 1B (PTP-1B). PTP-1B is central to controlling the function of both the leptin and insulin pathways. By inhibiting PTP-1B, MSI-1436 is expected to decrease appetite and normalize blood sugar. Trodusquemine has produced consistent, sustainable weight loss in a variety of animal models and appears to overcome metabolic readjustment, which often limits sustained weight loss during caloric restriction. In addition, trodusquemine has shown the ability to reverse co-morbidities associated with obesity such as abnormal glucose metabolism and cholesterol elevation.