OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical efficacy and safety studies, adverse effects, drug interactions, and dosage and administration of exenatide, a novel incretin mimetic agent recently approved for the treatment of type 2 diabetes mellitus.

DATA SOURCES: Information was obtained from MEDLINE searches of the English-language literature (1990-November 2004). Search terms included exenatide, synthetic exendin-4, exendin-4, AC2993, and GLP-1 agonist.

STUDY SELECTION AND DATA EXTRACTION: All available data were reviewed, including animal and human data disseminated as abstracts, clinical trials, review articles, and press releases.

DATA SYNTHESIS: Exenatide is a novel therapeutic agent recently approved for the treatment of type 2 diabetes. The unique pharmacologic profile of exenatide offers a promising adjunctive treatment option for this patient population.

CONCLUSIONS: While the long-term safety and efficacy of this agent are not well documented, the available data indicate the efficacy and safety of exenatide in combination with various oral antidiabetic agents in reducing postprandial glucose concentrations, glycosylated hemoglobin values, and potentially body weight without increasing the risk of hypoglycemia.

J Pharm Technol 2005;21:191-6.