Drug Forecast - DRUG FORECAST Exenatide (Byetta), an...

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D RUG F ORECAST 258 ® May 2006 Vol. 31 No. 5 INTRODUCTION Diabetes is a growing problem in the U.S. In 2002, it was estimated that 18.2 million people had diabetes, and this number continues to grow. Approxi- mately 90% of cases are type-2 diabetes. 1 The rise is attributed to increasing rates of obesity; therefore, the initial steps to controlling blood glucose levels include diet and exercise. However, too often, lifestyle modifications are not enough, and pharmacological treatment becomes a necessity. Currently, all treatment medications for type-2 diabetes available in the U.S. belong to six drug classes: biguanides, sulfonylureas, thiazolidinediones, meglit- inides, alpha-glucosidase inhibitors, and insulins. These classes of medications work in different ways to lower blood glu- cose levels. They can be used as mono- therapy or as combination therapy for diabetes management. Among adults with diabetes, about 12% take both insulin and oral medications, 19% take insulin only, 53% take oral medications, and only 15% do not take either. 1 Despite the availability of various treatment options, uncontrolled blood glucose remains a problem in patients with type-2 diabetes. Research has dem- onstrated that glycosylated hemoglobin (HbA 1C ) levels below 7% decrease the risk of developing complications related to diabetes. These complications can be reduced by as much as 40% for each 1% lowering of HbA 1C . 2,3 However, the aver- age HbA 1C concentration benefit of dia- betes patients in the U.S. is reported to be well above 8%. 4 Medications often have adverse effects, such as hypoglycemia and weight gain, which can offset the many benefits of therapy for hyperglycemia. New treatment modalities and innova- tive mechanisms can greatly aid in com- bating a disease that, to this date, does not have a cure. Exenatide injection (Byetta, Amylin/ Eli Lilly) was approved by the U.S. Food and Drug Administration (FDA) in April 2005 as adjunctive therapy to improve glycemic control in patients with type-2 diabetes who have not achieved ade- quate control with metformin (e.g., Glu- cophage, Bristol-Myers Squibb) or a sulfonylurea. 5 PHARMACOLOGY Exenatide is an incretin mimetic, a new therapeutic class in the treatment of diabetes. Incretins are peptide hormones secreted by specific cells in the small intestine in response to food intake. In the pancreas, incretin hormones act to increase glucose-dependent insulin secretion from beta cells and maintain postprandial glucose levels. Exenatide is a 39–amino acid peptide amide that exhibits glucoregulatory activities similar to those observed with the mammalian incretin hormone gluca- gon-like peptide (GLP)-1. 5–7
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This note was uploaded on 09/26/2010 for the course CHEMICAL E 119 taught by Professor Dale during the Spring '09 term at UCSB.

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Drug Forecast - DRUG FORECAST Exenatide (Byetta), an...

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