Two Birds with One Stone: First in Class Novel Glucokinase Activator

First in class drug stimulates glucose-induced pancreatic insulin secretion and augments hepatic glucose metabolism. The hormones glucagon and insulin delicately regulate the concentration of blood glucose. When patients become resistant to the effects of insulin or produce too little of it to properly regulate glucose concentrations, then diabetes can result. Unfortunately, not all patients with insulin-resistant, type 2 diabetes respond to drugs that improve insulin sensitivity. However, there is reason to be hopeful. A new molecule that targets glucokinase (GK), the enzyme responsible for phosphorylating glucose in pancreatic ß cells and hepatic cells, acts to significantly reduce blood glucose concentrations may be coming soon.

Array BioPharma’ announced that it’s diabetes drug ARRY-403 a glucokinase activator  was found to be effective in preclinical studies for the treatment of type 2 diabetes.

The data showed that in multiple well-established in vivo models of Type 2 diabetes, ARRY-403 was highly efficacious in controlling both fasting and non-fasting glucose, with rapid onset of effect and maximal efficacy within five to eight days.
In combination with existing standard-of-care drugs (metformin, DPP4 inhibitor) ARRY-403 provided additional glucose-control, which reached maximal efficacy after five to seven days of once-daily dosing, the company said.

Based on these and other results, Array plans to advance ARRY-403 into human clinical studies in the first half of 2009.
Kevin Koch, president and chief scientific officer of Array BioPharma, said: "There is a significant need for new, more effective oral diabetes treatments – and glucokinase activation represents a promising new mechanism. Glucokinase activators hold the potential to bring a significant benefit to Type 2 diabetes patients and we believe ARRY-403 is a highly potent and safe glucokinase activator."

================================

Advertisement
Dr. Bernstein’s Secrets To Normal Blood Sugars.  A five CD set containing personal education straight from Dr. Bernstein himself. Audio and Video, plus hours of seminars, transcripts, and more.  Learn more here. https://www.diabetes911.net/secrets.php