PLYMOUTH MEETING, Pa., Jan. 17 GenaeraCorporation (Nasdaq: GENR) today announced that dosing of subjects has begunin study MSI-1436C-103, the ascending single dose Phase 1 study oftrodusquemine (MSI-1436), in overweight and obese type 2 diabetics. MSI-1436is a novel therapeutic for the treatment of type 2 diabetes and obesity whichworks centrally and peripherally to regulate insulin and leptin receptorsignaling through inhibition of its novel target enzyme PTP-1B.
Study 103 is similar in design to the previously completed Study 101 whichwas conducted in healthy obese and overweight volunteers. The current studywill continue to expand the safety database for MSI-1436 and establish thepharmacokinetics of the drug in a population of type 2 diabetics who arepoorly controlled on metformin. The study will also evaluate a range ofsecondary endpoints including short-term insulin/glucose control indices,glucose tolerance and evaluation of insulin sensitivity.
"We have achieved another important milestone in the development of MSI-1436 and can now begin collecting data from obese type 2 diabetics," said JackArmstrong, President and Chief Executive Officer of Genaera. "The uniquemechanism of action provides MSI-1436 with the potential to impact two of thekey pathologies of type 2 diabetes: insulin resistance and obesity. Weanticipate that this clinical study will provide a first step in demonstratingthe safety of MSI-1436 in obese and overweight type 2 diabetics and will helpdetermine an optimal therapeutic dose for this population."
This randomized, vehicle-controlled study, being conducted at dgdResearch, Inc., a leading diabetes clinical research center in San Antonio,Texas, is enrolling otherwise healthy overweight and obese type 2 diabeticvolunteers to evaluate the safety, tolerability, and pharmacokinetics ofascending single doses of intravenously administered MSI-1436 in this specialpopulation. The ascending single dose protocol will initially enrollapproximately 28 subjects at four dose levels (3, 6, 10, and 15 mg/m2) and isexpected to be completed late in the first half of 2008.
About Trodusquemine (MSI-1436)
Trodusquemine is a centrally and peripherally-acting appetite suppressantand the first highly selective inhibitor of protein tyrosine phosphatase 1B(PTP-1B). PTP-1B is central to controlling the function of both the leptin andinsulin pathways. By inhibiting PTP-1B, MSI-1436 is expected to decreaseappetite and normalize blood sugar. Trodusquemine has produced consistent,sustainable weight loss in a variety of animal models and appears to overcomemetabolic readjustment, which often limits sustained weight loss duringcaloric restriction. In addition, trodusquemine has shown the ability toreverse co-morbidities associated with obesity such as abnormal glucosemetabolism and cholesterol elevation.
Genaera Corporation is focused on advancing the science and treatment ofmetabolic diseases. The Company has significant market opportunities with afirst-in-class molecule, trodusquemine (MSI-1436), that has the potential toredefine the treatment paradigm for obesity and type 2 diabetes and ispresently in a Phase 1 trial in obesity. In addition, Genaera has a value-driven, fully out-licensed partnership with MedImmune, Inc. for a second coreprogram that is presently undergoing Phase 2 clinical testing in asthma.Genaera is committed to directing resources to its core program and theaggressive clinical development of its key assets to build stockholder value.For further information, please see our website at http://www.genaera.com.
This announcement contains forward-looking statements within the meaningof the Private Securities Litigation Reform Act of 1995 that are subject torisks and uncertainties, known and unknown. Forward-looking statements reflectmanagement's current views and are based on cert