Long-acting preparations of exenatide

Abstract

Yunpeng Cai,1,2,* Liangming Wei,3,* Liuqing Ma,2 Xiwen Huang,2 Anqi Tao,2 Zhenguo Liu,1 Weien Yuan1,2 1Department of Neurology, Xinhua Hospital affiliated to Shanghai Jiaotong University School of Medicine, 2School of Pharmacy, Shanghai JiaoTong University, 3Key Laboratory for Thin Film and Microfabrication Technology, Ministry of Education, Research Institute of Micro/Nanometer Science and Technology, Shanghai JiaoTong University, Shanghai, People’s Republic of China *These authors contributed equally to this work Abstract: Exenatide has been widely used for the treatment of type 2 diabetes mellitus. However, its short plasma half-life of 2.4 hours has limited its clinical application. The exenatide products on the market, twice-daily Byetta™ and once-weekly Bydureon™ (both Amylin Pharmaceuticals, San Diego, CA, USA), are still not perfect. Many researchers have attempted to prolong the acting time of exenatide by preparing sustained-release dosage forms, modifying its structure, gene therapies, and other means. This review summarizes recent advances in long-acting exenatide preparations. Keywords: exendin-4, diabetes mellitus type 2, sustained release, long acting, extended release, microsphere