© 2012, Hacettepe University, Faculty of Pharmacy. All rights reserved.Diabetes mellitus is a disease in which a person has a high blood glucose level as a result of the body’s either not producing enough insulin (type 1), or because body cells do not properly respond or are resistant to the insulin that is produced (type 2). Insulin is synthesized in pancreas; it is responsible for the absorption and conversion of glucose to energy. Glucagon-like peptide analogues are drugs that bind to glucagon- like peptide-1 (GLP-1) receptor and enhance insulin secretion from pancreatic β-cells. As the half-life of GLP-1 is very short, instead of GLP-1 analogues, GLP-1 agonists with long half-lives are developed to provide longer duration of insulin secretion. Exenatide is an approved GLP-1 agonist and “incretinmimetic” used in type 2 diabetes and is suggested in diabetes that cannot be treated with oral antidiabetics. Though its mode of action is not clear, it is a drug that controls fasting and postprandial glycemia by increasing glucose-dependent insulin secretion from pancreatic β-cells and enables satiety in shorter period. However, the drug prolongs the gastric emptying time and this brings the side effects nausea and vomiting in turn. On the other hand, it should not be forgotten that the drug causes different types of pancreatitis which is a serious lifethreatening disease. The drug must be used with caution by prescription. Comprehensive surveillance studies and reliable feedbacks are needed to evaluate the clarification of contradictory issues in the usage of this particular drug. This review will focus on the toxicological profile of exenatide: Pharmaco/toxico-kinetics and dynamics, safety/efficacy, adverse reactions, drug interactions and its relationship with pancreatitis.