Genaera Presents Promising Preclinical Data for Trodusquemine (MSI-1436) at Keystone Symposia
PLYMOUTH MEETING, Pa., January 22, 2009 /PRNewswire-FirstCall/Genaera Corporation today announced a poster presentation of preclinical data on trodusquemine (MSI-1436), Genaera's lead drug candidate for the treatment of type 2 diabetes and obesity, during the Keystone Symposia: Obesity - Novel Aspects of the Regulation of Body Weight in Banff, Alberta.
The poster entitled "Effect of MSI-1436 (Trodusquemine) on Body Weight and Metabolic Profile in Diet-Induced Obese Rats" concluded that a single subcutaneous dose of MSI-1436 leads to marked reductions in body weight, fasting blood glucose, serum triglycerides and cholesterol in diet-induced obese (DIO) rats. In the study, the researchers reported that MSI-1436 induced dose-dependent changes in daily food intake resulting in corresponding decreases in body weight, as well as marked improvements in glucose tolerance and lipid profile.
"The DIO rat is a standard and well-accepted preclinical model for demonstrating anti-obesity impact in this class of drugs. These initial subcutaneous studies of MSI-1436 exhibit dose-related reductions across a wide range of clinical and metabolic outcomes associated with both obesity and diabetes," commented Jack Armstrong, President and CEO of Genaera. "We are continuing to progress the subcutaneous formulation and are planning our initial human studies with MSI-1436 via this route later this year."
Trodusquemine is the first highly selective inhibitor of protein tyrosine phosphatase 1B (PTP1B), an enzyme central to controlling the function of both the leptin and insulin pathways. By inhibiting both central and peripheral PTP1B, MSI-1436 is expected to decrease appetite and normalize blood sugar. Initial clinical studies of trodusquemine in obese and overweight subjects has provided early indicators of weight loss and improved glucose control. These results confirm previous work in animal models which demonstrated significant weight loss without metabolic rebound, 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.
Posted: January 2009