LOS ALTOS, Calif., June 10 /PRNewswire/ -- InteKrin Therapeutics Inc presented Phase 2a clinical study results at the American Diabetes Association annual meeting in New Orleans demonstrating that once a day oral treatment with INT131 provides anti-diabetic efficacy consistent with maximal dose thiazolidinedione (TZD) therapy but with less hematocrit reduction and weight gain.
The 4 week double blind placebo controlled study of INT131 in Type 2 Diabetes Mellitus (T2DM) patients previously not on pharmacological therapy showed a dose dependent decrease in fasting plasma glucose (FPG) at 4 weeks, the primary endpoint of the study. This decrease was already statistically significant at 1 week for both low and high doses (1 mg and 10 mg) of INT131.
The efficacy measured at 4 weeks of 1 mg of INT131 treatment was comparable to the efficacy modeled for this patient population treated with the maximal approved doses of Actos(R) and Avandia(R), but in contrast the low dose INT131 group did not show the significant weight gain or fluid retention (measured by hematocrit drop) modeled for maximal dose TZDs. The high dose INT131 group showed about twice the decrease in FPG attained with low dose INT131, and a correspondingly greater efficacy compared to that modeled for maximal dose TZDs. Importantly, this greater efficacy was achieved with INT131 without greater weight gain or hematocrit drop than expected for maximal dose TZDs. INT131 was well tolerated in this study with no safety issues noted.
"These data are supportive of INT131 acting as a selective modulator of PPARgamma in T2DM patients," remarked Dr Alex DePaoli, Chief Medical Officer of InteKrin Therapeutics, who presented the data. "The key observation from this study is that INT131 is a potent insulin sensitizer that lowers fasting glucose as well as the maximal dose of the TZDs while mitigating the typical side effect profile."
"Translation of the nonclinical profile of INT131 into the clinic is an exciting validation of the selective PPAR modulator design of the molecule," added Dr Linda Higgins, Chief Scientific Officer of InteKrin Therapeutics. "INT131 retains or exceeds TZD potency and efficacy for glycemic lowering in rodent models of T2DM, while also showing remarkable safety in nonclinical studies of INT131 even at multiples of clinical exposures that far exceed those at which toxicities are observed with TZDs."
These Phase 2a study data provided the rationale for a double blind placebo controlled 24 week Phase 2b study of 4 doses of INT131 and 45 mg Actos(R) as active comparator in 360 T2DM patients. InteKrin completed enrollment of the study in March, 2009.
INT131 is a next-generation, non-TZD insulin sensitizer and selective modulator of PPARgamma (SPPARM). INT131 belongs to a unique, non-TZD chemical class, and was purposely designed to retain the well validated and robust insulin sensitizing efficacy of PPARgamma while minimizing the typical side effects seen with the full agonists TZDs Actos(R) and Avandia(R). PPARgamma activation treats insulin resistance, a key etiological feature in the onset and subsequent progression of type 2 diabetes.
About InteKrin (www.InteKrin.com)
InteKrin Therapeutics is a privately-held clinical-stage drug development company focused on diabetes, obesity and metabolic disease. InteKrin's business strategy is to build a robust portfolio of high value products by in-licensing clinical-stage therapeutic candidates that address significant unmet medical needs and rapidly move them through critical development stages. InteKrin's team of world-class scientific and medical experts includes veterans from several successful BioPharma organizations, internationally recognized experts in nuclear receptors and metabolism, top scientists formerly with the Food and Drug Administration and key clinical and commercialization leaders.
|SOURCE InteKrin Therapeutics Inc|
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