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Isis Pharmaceuticals Reports Positive Phase 1 Data On Three Drugs In Development To Treat Metabolic Disorders
Date:12/7/2012

sis observed encouraging data in measures of insulin sensitivity and in a biomarker associated with weight loss.  Previous clinical experience with the PTP-1B inhibitor ISIS 113715 demonstrated that PTP-1B inhibition improved glucose control and reduced LDL-cholesterol without causing weight gain.  "These new ISIS-PTP1BRx data are consistent with our findings from the earlier Phase 2 studies of ISIS 113715.  It is also important to note that ISIS-PTP1BRx is a significantly more potent PTP-1B inhibitor than our earlier inhibitor, ISIS 113715, and, as such, we expect more robust effects in clinical trials," said Sanjay Bhanot, M.D., Ph.D., vice president, clinical development and translational medicine at Isis.  "We believe that ISIS-PTP1BRx has the potential to be broadly useful in combination with most of the other commonly used drugs to treat patients with diabetes, including insulin, glucagon-like peptide (GLP-1) agonists, and more traditional drugs like metformin." 

ISIS-GCGRRx
ISIS-GCGRRx targets the glucagon receptor (GCGR) and is designed to reduce the effects of glucagon, a hormone that causes increased glucose production in the liver.  In patients with advanced diabetes, uncontrolled glucagon action leads to a significant increase in blood glucose levels. Therefore, attenuating glucagon action could have a significant glucose lowering effect in patients with severe diabetes.  "Although small molecule inhibitors of GCGR have demonstrated glucose-lowering effects in diabetic patients, they also have produced limiting side effects, including increases in lipids and blood pressure.  In contrast, in our Phase 1 study ISIS-GCGRRx displayed a good safety profile with no clinically significant increases in blood pressure or lipids and with no hypoglycemia. In addition, we observed an increase in active GLP-1, a hormone that preserves pancreatic func
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SOURCE Isis Pharmaceuticals, Inc.
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