The amino acid sequence of Exenatide Acetate partially overlaps with human GLP-1. Exenatide acetate has been shown to bind to and activate the known human GLP-1 receptor in vitro. This means that by including cAMP (cyclic adenosine monophosphate) or other intracellular signaling mechanisms, glucose-dependent insuli synthesis and insuli secretion by pancreatic β cells in the body are increased.

Application of exenatide acetate causes an increase in acinar cAMP without stimulating amylase release. As an incretin mimetic, exenatide acetate acts as agonist of the glucagon-like peptide-1 (GLP-1) receptor. As GLP-1, though with prolonged activity, exenatide acetate augments the postprandial production of insuli and suppresses secretion of glucagon. For this reason, exenatide acetate has found use as a medication of diabetes II.