Metabolic Solutions Development Co.

MSDC-0602

Summary
MSDC-0602 is the result of an extensive medicinal chemistry effort to find insulin sensitizers that have a selective interaction with the mitochondrial target of the thiazolidinediones, while sparing binding to the nuclear transcription factor PPARγ. MSDC-0602 may enable dosing to even greater effect and efficacy than MSDC-0160. The candidate was selected from over 100 novel compounds designed based upon several factors that MSDCs founders believe are crucial to successfully treating targeted populations.

Development Status
The safety, tolerability and efficacy of MSDC-0602, a novel insulin sensitizer, were evaluated in a recently completed Phase 2a, 129-subject, randomized, double-blind, and comparator- and placebo-controlled multiple-dose study in type 2 diabetic patients. No safety concerns were uncovered for any treatments and all treatments were well tolerated.

The data confirm the potential of MSDC-0602 to achieve significant glucose control in type 2 diabetic subjects and the drug showed the expected increased insulin sensitivity. Unlike pioglitazone, MSDC-0602 produced no weight gain. There may be potential for weight control on longer exposures given the “browning” of adipose stores. Importantly, in this short study, the data show that MSDC-0602 has the potential to lower HbA1c in excess of 1.5 percent without weight gain, fluid retention, and other PPAR-related liabilities.

The results of this study affirm the potential of this novel insulin sensitizer and form the basis for a larger, longer duration Phase 2b study to be conducted in 2012.