Array BioPharma Inc. today announced the presentation of preclinical data on a novel small molecule glucokinase activator (GKA), ARRY-403, a drug for the treatment of Type 2 diabetes. The data showed that ARRY-403 demonstrated potent, highly glucose-blood-level dependent, control of both fasting and non-fasting glucose concentrations. Based on these and other results, Array plans to advance ARRY-403 into human clinical studies in the first half of 2009. The data were presented today at an annual metabolic diseases conference in London.
“There is a significant need for new, more effective oral diabetes treatments – and glucokinase activation represents a promising new mechanism,” said Kevin Koch, Ph.D., President and Chief Scientific Officer. “GKAs 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.”
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, or PPARĪ³ agonist), ARRY-403 provided additional glucose-control, which reached maximal efficacy after five to seven days of once-daily dosing. ARRY-403 showed no adverse increases of body weight, plasma triglycerides or total cholesterol, whether used as monotherapy or in combination.
According to the Centers for Disease Control, approximately 24 million (8 percent) Americans have diabetes. Current therapies for this progressive disease are insufficient or inconvenient, creating a need for the development of novel therapeutic approaches. GKAs, such as ARRY-403, represent a promising new class of drugs for the treatment of Type 2 diabetes.
The ARRY-403 presentation will be available as a PDF on Array's website: www.arraybiopharma.com.
About ARRY-403/ Glucokinase activation
Glucokinase activators (GKAs) reduce glucose levels via a dual mechanism of action – working in both the pancreas and the liver. Glucokinase (GK) is the enzyme that senses glucose in the pancreatic beta cells, stimulating insulin release in a glucose-dependent manner. GK also regulates glucose uptake and glucose production in the liver. In diabetic patients, there is a reduction of glucokinase (GK) activity in the pancreas and the liver. The activation of glucokinase lowers glucose levels by enhancing the ability of pancreatic beta cells to sense glucose, in turn increasing the level of insulin that is produced by the pancreas. Simultaneously, GKAs also increase the uptake of glucose in the liver, while reducing the amount of glucose produced by the liver. These combined actions of GKAs result in improved beta cell function and increased insulin sensitivity in the liver.
About Array BioPharma
Array BioPharma Inc. is a biopharmaceutical company focused on the discovery, development and commercialization of targeted small molecule drugs to treat patients afflicted with cancer, inflammatory diseases, pain and metabolic diseases. Our proprietary drug development pipeline includes clinical candidates that are designed to regulate therapeutically important target proteins and are aimed at significant unmet medical needs.
Contact:
Array BioPharma Inc.
Tricia Haugeto, 303-386-1193
thaugeto@arraybiopharma.com
Source: Array BioPharma Inc.
“There is a significant need for new, more effective oral diabetes treatments – and glucokinase activation represents a promising new mechanism,” said Kevin Koch, Ph.D., President and Chief Scientific Officer. “GKAs 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.”
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, or PPARĪ³ agonist), ARRY-403 provided additional glucose-control, which reached maximal efficacy after five to seven days of once-daily dosing. ARRY-403 showed no adverse increases of body weight, plasma triglycerides or total cholesterol, whether used as monotherapy or in combination.
According to the Centers for Disease Control, approximately 24 million (8 percent) Americans have diabetes. Current therapies for this progressive disease are insufficient or inconvenient, creating a need for the development of novel therapeutic approaches. GKAs, such as ARRY-403, represent a promising new class of drugs for the treatment of Type 2 diabetes.
The ARRY-403 presentation will be available as a PDF on Array's website: www.arraybiopharma.com.
About ARRY-403/ Glucokinase activation
Glucokinase activators (GKAs) reduce glucose levels via a dual mechanism of action – working in both the pancreas and the liver. Glucokinase (GK) is the enzyme that senses glucose in the pancreatic beta cells, stimulating insulin release in a glucose-dependent manner. GK also regulates glucose uptake and glucose production in the liver. In diabetic patients, there is a reduction of glucokinase (GK) activity in the pancreas and the liver. The activation of glucokinase lowers glucose levels by enhancing the ability of pancreatic beta cells to sense glucose, in turn increasing the level of insulin that is produced by the pancreas. Simultaneously, GKAs also increase the uptake of glucose in the liver, while reducing the amount of glucose produced by the liver. These combined actions of GKAs result in improved beta cell function and increased insulin sensitivity in the liver.
About Array BioPharma
Array BioPharma Inc. is a biopharmaceutical company focused on the discovery, development and commercialization of targeted small molecule drugs to treat patients afflicted with cancer, inflammatory diseases, pain and metabolic diseases. Our proprietary drug development pipeline includes clinical candidates that are designed to regulate therapeutically important target proteins and are aimed at significant unmet medical needs.
Contact:
Array BioPharma Inc.
Tricia Haugeto, 303-386-1193
thaugeto@arraybiopharma.com
Source: Array BioPharma Inc.
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