In a placebo-controlled, double-blind, four-week Phase IIa study, INT131 administration demonstrated a significant improvement in fasting plasma glucose compared to baseline and placebo at doses of 1mg and 10mg daily, in subjects with Type 2 diabetes mellitus (T2DM) on no drug therapy.
The changes in fasting plasma glucose were accompanied by significant improvements in insulin resistance and an increase in adiponectin, a key biomarker of PPAR-gamma mediated efficacy. INT131 was safe and well tolerated, without evidence of the recognized side effects of the full agonist TZDs at a dose that provides glycemic improvement as good as or better than the highest approved doses of Actos and Avandia.
InteKrin has also initiated a 360-patient, 24-week placebo-controlled Phase IIb study with a 45mg Actos comparator arm in February 2008 and expects results to be completed in the second half of 2009.
Alex DePaoli, chief medical officer of InteKrin, said: “This Phase IIa data demonstrate that it may be possible to achieve significant glucose lowering without recognized TZD adverse effects, such as edema and weight gain, which is a genuine breakthrough for this target.”