Next New Possible Class of Meds for Diabetes- Glucokinase Activator(GKA)

GKA compounds rapidly lower blood glucose levels by increasing glucose uptake in the liver and increasing insulin secretion from the pancreas.

OSI Pharmaceuticals, Inc. announced that it has initiated a Phase I clinical study of PSN010. PSN010 is a Glucokinase Activator (GKA), which is designed to rapidly lower blood glucose levels by increasing glucose uptake in the liver and increasing insulin secretion from the pancreas.

"The science behind our research efforts is focused on the development of next-generation small molecule compounds designed to develop safer, more effective and innovative products for the treatment of metabolic diseases, particularly type 2 diabetes and obesity," stated Anker Lundemose, M.D., Ph.D., Executive Vice President of OSI Pharmaceuticals and President of (OSI) Prosidion. "We believe PSN010’s dual mechanism of action, which has been demonstrated in pre-clinical studies to reduce blood glucose levels, may ultimately offer a competitive therapeutic option for diabetes patients."

This single-center, double-blind Phase I study is scheduled to enroll up to 80 healthy volunteers. The single dose escalation study is designed to provide preliminary information on the safety, tolerability, pharmacokinetics and pharmacodynamics of PSN010.

GKAs may represent a new approach to diabetes therapy as these compounds attenuate hyperglycemia by increasing both hepatic glucose metabolism and glucose-stimulated pancreatic insulin release. Pre-clinical data showed that PSN010 activates Glucokinase (GK) strongly in vitro and in vivo. The anti-hyperglycemic capabilities of PSN010 have been confirmed in several diabetic rodent models and maximal glucose concentrations were significantly attenuated by the drug candidate. GKA PSN010 may offer a novel strategy for controlling hyperglycemia in diabetic patients through its dual mechanism of action.