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Genaera Releases Phase 1 Data and New Preclinical Data on the CNS Function of Trodusquemine (MSI-1436) at CBI Obesity Summit
Date:7/25/2008

etabolic biomarkers as well as evaluations of mood and cognition were also found to be stable in subjects receiving all levels of the drug or placebo during the trial. These positive Study MSI-1436C-103 results are expected to enable further study to fully validate proof-of-concept of MSI-1436 in an ascending multiple-dose clinical trial planned to begin later this year.

Data were also presented from preclinical studies which demonstrated that systemically administered MSI-1436 crossed the blood-brain barrier and functionally inhibited PTP1B in the hypothalamus. In this study, rats were administered a single dose of MSI-1436 one day prior to receiving insulin; 30 minutes post-insulin, hypothalami were harvested to determine the level of phosphorylated-insulin receptor beta (IR-beta), a target of PTP1B. Previous studies had shown that MSI-1436 is a reversible, noncompetitive inhibitor of PTP1B with the ability to cross the blood brain barrier. In the hypothalamus, MSI-1436 enhanced the insulin-induced phosphorylative state of the insulin receptor, which confirms the functionality of MSI-1436 in this key regulatory center of the brain. The combination of central and peripheral inhibition makes MSI-1436 a promising therapeutic candidate for both obesity and type 2 diabetes.

"The data reported today support continuing confidence in our ability to administer trodusquemine to a wide range of obese and type 2 diabetic patients," stated Jack Armstrong, President and Chief Executive Officer of Genaera. "MSI-1436 is the only reversible, noncompetitive inhibitor of PTP1B in clinical stage development that functionally inhibits PTP1B in the periphery and in the hypothalamus. This dual mechanism of action, with the demonstrated ability to cross the blood-brain barrier, makes MSI-1436 an exciting therapeutic for further clinical study."

About Trodusquemine (MSI-1436)

Trodusquemine is a centrally and peripherally-acting appetite suppressant and the firs
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SOURCE Genaera Corporation
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