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Genaera Corporation Presents Data on Mechanism of Inhibition of PTP-1B for Trodusquemine (MSI-1436) at Federation of American Societies for Experimental Biology (FASEB) Meeting
Date:7/14/2008

in diet induced and genetically obese animal models. The poster described the inhibition of PTP-1B by MSI-1436 as fully reversible and characterized by a classic noncompetitive, dose-dependent mechanism which exhibited greatest potency for the full-length form of the enzyme. Cellular studies demonstrating that phosphatase inhibition by MSI-1436 in the presence of insulin pretreatment provided further support for the inhibition of PTP-1B and a greater understanding of the role of enhanced insulin signaling associated with weight loss and glucose control observed during treatment in preclinical models of obesity and diabetes with MSI-1436.

To date, MSI-1436 has been shown to have few adverse events and to be well-tolerated in the over 50 subjects who participated in the Phase 1 clinical program of MSI-1436. Genaera plans to conduct an ascending multiple-dose study later this year.

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.

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 redefine the treatment paradigm for obesity and type 2 diabetes and is presently in a phase
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SOURCE Genaera Corporation
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