Genaera Corporation Presents Interim Phase 1 Data for Obesity Compound Trodusquemine (MSI-1436) at IBC ...(steady flowof clinical information in th...),Health
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steady flow of clinical information in the second half of 2007 as our clinical studies progress to broader populations."
About Trodusquemine (MSI-1436)
Trodusquemine (MSI-1436) is the first drug candidate that acts both centrally and peripherally to selectively inhibit the established and validated enzyme target, protein tyrosine phosphatase 1B (PTP-1B). The dual locations of MSI-1436 action make the drug a promising candidate for both obesity and type 2 diabetes. By inhibiting PTP-1B, trodusquemine is expected to decrease appetite and normalize blood sugar as PTB-1B is central to both the insulin and leptin pathways. Based on this unique mechanism of action, trodusquemine has the potential to bridge the treatment for two of the most serious metabolic diseases, obesity and type 2 diabetes. In addition, trodusquemine has overcome selectivity concerns that other compounds that target PTP-1B have failed to overcome. Preclinical studies demonstrate that trodusquemine is a potent, highly-selective and reversible inhibitor of PTP-1B. In vitro kinetics demonstrate that trodusquemine is an allosteric, noncompetitive inhibitor of PTP-1B, binding to a site different from the catalytic site of PTP-1B. Data also demonstrate that trodusquemine can produce 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. Trodusquemine suppresses appetite, causes differential weight loss, reduces adipocyte size, reduces body fat (with no reduction of lean mass), and improves glucose tolerance via inhibition of a unique combination of signaling pathways in a mouse model of diet induced obesity (DIO).
About Genaera
Genaera Corporation is focused on advancing the science and treatment
of metabolic diseases. The Company has significant market opportunities
with a first-in-class molecule, trodusquemine (MSI-1436), that has the
potential to redefin
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SOURCE Genaera Corporation Copyright©2007 PR Newswire. |
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