March 28, 2011 - ActiveSite Pharmaceuticals, Inc., announced the online publication of a study in the journal Diabetes that describes the effectiveness of its novel plasma kallikrein inhibitor ASP-440 in reducing blood-retinal barrier breakdown in a rodent model of diabetes. Diabetes-induced breakdown of the blood-retinal barrier results in leaky blood vessels in the eye, and the gradual buildup of fluid in the retina from the leakage can result in diabetic macular edema (DME), the primary cause of vision loss in diabetic individuals. DME affects more than 1 million individuals in the U.S. alone, and no FDA-approved medicines are currently available for its treatment.In the study, co-authored by scientists from the Joslin Diabetes Center, an affiliate of Harvard Medical School, and ActiveSite Pharmaceuticals, the integrity of the blood-retinal barrier in diabetic rats was measured using a well-established technique that measures the leakage of the plasma protein albumin from the vascular compartment into the retina. Compared to non-diabetic healthy rats, diabetic animals demonstrated a 2.6-fold increase in the rate of albumin leakage into the retina. Treatment of diabetic animals with systemically-administered ASP-440 for four weeks reduced the excess rate of albumin leakage by more than 80%, without affecting blood glucose.
ASP-440 was also effective in preventing blood-retinal barrier breakdown in hypertensive rats, reducing excessive albumin leakage into the retina by 90% following systemic treatment for seven days, without affecting blood pressure. Hypertension is a known risk factor for development of DME... ActiveSite Pharmaceuticals' Press Release -
