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Genaera Corporation announced today the presentation of new preclinical data on trodusquemine (MSI-1436), a novel inhibitor of PTP-1B and Genaera's lead drug candidate for the treatment of type 2 diabetes and obesity, during the 10th Biennial FASEB Summer Research Conference Protein Phosphatases in Snowmass Village, Colorado
PLYMOUTH MEETING, PA, USA | July 14, 2008 | Genaera Corporation (Nasdaq: GENR) announced today the presentation of new preclinical data on trodusquemine (MSI-1436), a novel inhibitor of PTP-1B and Genaera's lead drug candidate for the treatment of type 2 diabetes and obesity, during the 10th Biennial FASEB Summer Research Conference Protein Phosphatases in Snowmass Village, Colorado. The poster presentation entitled, "Trodusquemine (MSI-1436), An Allosteric Inhibitor of Protein Tyrosine Phosphatase 1B," concluded that MSI-1436 is a selective, reversible and noncompetitive inhibitor of PTP-1B that enhances insulin signaling through potent PTP-1B inhibition both in vivo and in vitro.
"The search to discover PTP-1B inhibitors as a therapeutic target for the treatment of obesity and type 2 diabetes has long been a goal of drug development but achieving the selectivity necessary to demonstrate safety has been a significant hurdle. The new information on the mechanism by which MSI-1436 inhibits PTP-1B supports its first-in-class status," stated Jack Armstrong, President and Chief Executive Officer of Genaera. "MSI-1436 is the only reversible, noncompetitive inhibitor of PTP-1B in clinical stage development. It is the allosteric nature of MSI-1436 and its ability to reversibly inhibit PTP-1B that is believed to be the key to the safety we have observed in Phase 1. We anticipate this will be attractive to both potential partners and clinicians as we obtain further evidence of the efficacy and safety of MSI-1436 in future studies."
Inhibition of PTP-1B, a non-receptor isoform of the protein tyrosine phosphatase family, by MSI-1436 has been shown to reduce food intake, induce weight loss, and increase insulin sensitivity 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 1 trial in obesity. In addition, Genaera has a value-driven, fully out-licensed partnership with MedImmune, Inc. for a second core program that is presently undergoing phase 2 clinical testing in asthma. Genaera is committed to directing resources to its core program and the aggressive clinical development of its key assets to build stockholder value. For further information, please see our website at http://www.genaera.com.
SOURCE: Genaera Corporation |
