According to the Centers for Disease Control, approximately 24 million (8 percent) Americans have diabetes. Current therapies for this progressive disease are insufficient or have unwanted side-effects, creating a need for the development of novel therapeutic approaches.
About Glucokinase Activation
In normal individuals, the pancreas secretes insulin in response to increased levels of glucose in the blood. Glucokinase (GK) is the enzyme that senses glucose in the pancreas. GK also increases glucose utilization and decreases glucose production in the liver. In patients with Type 2 diabetes, there is a reduction of GK activity in the pancreas and the liver. Activating GK with small molecules such as ARRY-403 lowers blood glucose levels by enhancing the ability of the pancreas to sense glucose, which leads to increased insulin production. Simultaneously, glucokinase activators increase the net uptake of blood glucose by the liver. Glucokinase activators, such as ARRY-403, represent a promising new class of drugs for the treatment of Type 2 diabetes.
ARRY-403 is a potent, selective and orally administered small molecule glucokinase activator. In multiple preclinical models of Type 2 diabetes, ARRY-403 was studied in controlling both fasting and non-fasting blood glucose by itself and in combination with other existing standard-of-care diabetes drugs. In a Phase 1 single ascending dose study in patients with Type 2 diabetes, ARRY-403 demonstrated dose-dependent glucose red
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