Genaera Presents Preliminary Phase 1b Data for Trodusquemine (MSI-1436)
PLYMOUTH MEETING, Pa., February 10, 2009 /PRNewswire-FirstCall/ -- Genaera Corporation today reported promising preliminary Phase 1b clinical data for trodusquemine (MSI-1436), the first-in-class, highly selective inhibitor of PTP1B and Genaera's lead drug candidate for the treatment of type 2 diabetes and obesity. Mr. Jack Armstrong, President and CEO of Genaera, presented data from the first of three cohorts in an ascending multiple dose study of MSI-1436 (Study 102), during the BIO CEO & Investor Conference in New York.
Data from cohort 1, in which eight doses of 3 mg/m2 of MSI-1436 were administered over 21 days to overweight and obese type 2 diabetic subjects, demonstrated meaningful improvement in four primary outcomes used to evaluate type 2 diabetes, including:
"It is very exciting to see a believable biologic response to MSI-1436 in cohort 1 of Study 102. While 3 mg/m2 of drug was thought to be a sub-therapeutic dose, the data has demonstrated otherwise. We are currently completing the in-house portion of the second cohort of this study evaluating 6 mg/m2 of MSI-1436 and the initial results support proceeding to the 10 mg/m2 cohort which will begin later this month. Final Study 102 data is expected in the second quarter," commented Mr. Armstrong. "MSI-1436 continues to exhibit promise as the only PTP1B inhibitor in development to simultaneously treat both type 2 diabetes and obesity. Our recent identification of a novel binding site we believe is the key to its selectivity and safety to date. We are anxious to begin our first study of subcutaneously administered MSI-1436 to human subjects, which is planned for later this year."
In Cohort 1 of Study 102, five subjects received MSI-1436 while two subjects received placebo, with results suggesting that MSI-1436 is well-tolerated, with no serious adverse events, no severe adverse events and no dose-limiting toxicities reported. In addition to the favorable adverse event profile seen in the cohort, the multiple-dose PK of MSI-1436 was found to be similar to the PK profiles following single intravenous dosing in two previous phase 1 studies.
Trodusquemine is the first highly selective inhibitor of protein tyrosine phosphatase 1B (PTP1B), an enzyme central to controlling the function of both the leptin and insulin pathways. By inhibiting both central and peripheral PTP1B, MSI-1436 is expected to decrease appetite and normalize blood sugar. Initial clinical studies of trodusquemine in obese and overweight subjects has provided early indicators of weight loss and improved glucose control. These results confirm previous work in animal models which demonstrated significant weight loss without metabolic rebound, 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.
Posted: February 2009