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APD668 is a novel, highly potent and orally active glucose-dependent insulinotropic receptor (GDIR) agonist intended to more efficiently stimulate insulin release by beta cells in response to elevated blood glucose levels, and to also avoid hypoglycemia.
APD668 is a novel, highly potent and orally active glucose-dependent insulinotropic receptor (GDIR) agonist intended to more efficiently stimulate insulin release by beta cells in response to elevated blood glucose levels, and to also avoid hypoglycemia.
The GDIR mechanism is glucose dependent: in preclinical studies, GDIR agonists only lowered blood glucose when it rose above normal levels, such as after a meal. Therefore, unlike the glucose-insensitive sulfonylureas, Arena's GDIR agonists are not expected to lower normal fasting blood glucose levels or cause hypoglycemia. In addition, GDIR stimulation has been found to increase the levels and activity of intracellular factors thought to be involved in the preservation of beta cells.
Investigated for use/treatment in diabetes mellitus type 2.
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