General Information

Bydureon is specifically indicated as an adjunct to diet and exercise to improve glycemic control in adults and pediatric patients aged 10 years and older with type II diabetes mellitus.

Bydureon is supplied as a powder suspension to be reconstituted into a solution. The recommended dose is 2 mg administered once every seven days (weekly). The dose can be administered at any time of day, with or without meals. Bydureon is administered as a subcutaneous (SC) injection in the abdomen, thigh or upper arm region.

Mechanism of Action

Bydureon is an extended-release formulation of exenatide, a GLP-1 receptor agonist that enhances glucose-dependent insulin secretion by the pancreatic beta-cell, suppresses inappropriately elevated glucagon secretion, and slows gastric emptying. The amino acid sequence of exenatide partially overlaps that of human GLP-1. Exenatide is a GLP-1 receptor agonist that has been shown to bind and activate the human GLP-1 receptor in vitro. This leads to an increase in both glucose-dependent synthesis of insulin and in vivo secretion of insulin from pancreatic beta cells, by mechanisms involving cyclic AMP and/or other intracellular signaling pathways. Exenatide promotes insulin release from pancreatic beta cells in the presence of elevated glucose concentrations.

Clinical Trial Results

The FDA approval of Bydureon was based on a 24-week comparator-controlled study. This randomized, open-label trial was conducted to compare the safety and efficacy of Bydureon to Byetta in 252 subjects with type II diabetes and inadequate glycemic control with diet and exercise alone or with oral antidiabetic therapy, including metformin, a sulfonylurea, a thiazolidinedione, or combination of two of those therapies. The subjects were randomly assigned to receive Bydureon 2 mg once every seven days (weekly) or Byetta (10 mcg twice-daily), in addition to existing oral antidiabetic agents. Subjects assigned to Byetta initiated treatment with 5 mcg twice-daily then increased the dose to 10 mcg twice-daily after 4 weeks. The mean baseline HbA1c was 8.4%. The primary endpoint was change in HbA1c from baseline to Week 24 (or the last value at time of early discontinuation). The mean change from baseline was for Bydureon -1.6 and for -0.9 Byetta. The percentage achieving HbA1c <7% at Week 24 was 58% in the Bydureon arm and 30% in the Byetta arm. Reductions from mean baseline (97/94 kg) in body weight were observed in both Bydureon (-2.3 kg) and Byetta (-1.4 kg) treatment groups.