( wing eight weeksof therapy. Additional...)Arisaph Pharmaceuticals Announces Results of its Potent Smart DPP-4,Inhibitor, ARI-2243, at the ADA,Health

wing eight weeks of therapy. Additionally, animals treated with 3.0 mg/kg of ARI-2243 showed less diabetes progression than animals treated with placebo or 3.0 mg/kg of vildagliptin. Such superior efficacy data in an highly refractory diabetes animal model suggest that ARI- 2243 will produce a differentiated efficacy profile in human type II diabetes.

In addition to the compelling efficacy, ARI-2243 is functionally selective through a smart, soft drug inactivation process. Specifically, ARI-2243 binds rapidly and tightly to DPP-4 and once bound, the complex dissociates very slowly, thereby preventing the degradation of GLP-1 at the site of action. Unbound ARI-2243 then undergoes a unique soft drug inactivation as it passes through the gut and into the systemic circulation, which limits the exposure of the active species to unwanted targets, such as DPP 8 and 9. The conversion product, ARI 2498 is a millimolar inhibitor of the DPP family, in particular, DPP 8 and 9. Such soft drug inactivation confers functional selectivity and contributes to a favorable therapeutic window in animals.

"In ARI-2243, we have designed a smart, long acting DPP-4 inhibitor that is extremely potent and functionally selective," commented Christopher P. Kiritsy, President and Chief Executive Officer of Arisaph Pharmaceuticals. "The preclinical efficacy data presented at the ADA highlight the compelling efficacy of ARI-2243 at low doses. With such promising data, we expect to achieve superior HbA1c lowering in humans using significantly lower doses of ARI-2243, thereby supporting our goal of developing best-in-class medicines for validated targets."

About Arisaph

Arisaph, located in Boston, Massachusetts, is an emerging drug design and discovery biopharmaceutical company with active programs to develop differentiated therapies for diabetes, cancer and cardiovascular disease. Arisaph utilizes proprietary drug discovery platforms to develop ultra-smart drugs that are
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