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FDA Accepts Investigational New Drug Application for ARI-2243 and a First in Man Clinical Trial Set to Begin During the First Half of 2008
Date:3/11/2008

htly 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 non-enzymatic conversion as it passes through the gut and into systemic circulation, which limits the exposure of the active species to unwanted targets, such as DPP 8 and 9. Such "soft drug" properties of ARI-2243 confer functional selectivity and are believed to contribute to a favorable therapeutic index in animals.(3)

About Arisaph

Arisaph, located in Boston, Massachusetts, is an emerging drug 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 efficacious and act on select targets. Arisaph has successfully applied its specificity profiling and retro-inversal chiral chemistry technology platforms to synthesize promising candidate drugs for seven targets, including ARI-2243, a lead candidate for DPP-4 inhibition to treat Type II diabetes and ARI-1778 or reverse D-4F, an orally active mimetic peptide, being developed in collaboration with Abbott Laboratories to treat atherosclerosis. Through a licensing agreement with Tufts University the Company has exclusive worldwide rights to several important issued patents in the diabetes area and several pending patents that have utility for the treatment of cancer and cardiovascular disease.

About DPP-4:

Dipeptidylpeptidase (DPP) - 4 is a naturally occurring, proteolytic enzyme that rapidly degrades the incretin hormones, gastric inhibitory polypeptide (GIP) and glucagon-like protein (GLP-1). GLP-1 has a favorable anti-diabetic role because it stimulates glucose dependent insulin secretion from the pancreas, slows gastric emptying and decreases glucagon secretion. Inhibitors to DPP-4 improve glycemic control in patients with Type II diabetes by
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SOURCE Arisaph Pharmaceuticals, Inc.
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