Park Eun Ji, Lim Sung Mook, Lee Kang Choon, Na Dong Hee
a College of Pharmacy and Research Institute of Pharmaceutical Sciences , Kyungpook National University , Daegu , Republic of Korea.
b Drug Targeting Laboratory, College of Pharmacy , SungKyunKwan University , Suwon , Republic of Korea.
Expert Opin Ther Pat. 2016 Jul;26(7):833-42. doi: 10.1080/13543776.2016.1192130. Epub 2016 Jun 9.
Since exendin-4 (exenatide) was approved for diabetes therapy in 2005, several exendin analogs have been developed for the treatment of type 2 diabetes mellitus. As exenatide is a relatively short-acting injectable agent, major approaches have focused on developing long-acting exendin analogs to improve patient compliance and convenience.
In this review, the authors report on patents related to exendins and exendin analogs from 2012 to 2015. The patents have been divided into three categories based on the technologies used to develop the new chemical entities: 1) chemical bioconjugate analogs; 2) recombinant fusion protein analogs; and 3) multifunctional peptide analogs.
Recently, research on exendins and their analogs has grown significantly, leading to the development of long-acting analogs and multifunctional peptides. While long-acting injectable agents are still the major products in the pharmaceutical industry, a significant growth is expected in the development of orally available exendins.
自2005年艾塞那肽（exendin-4）被批准用于糖尿病治疗以来，已开发出多种艾塞那肽类似物用于治疗2型糖尿病。由于艾塞那肽是一种作用相对较短的注射剂，主要的研发方向集中在开发长效艾塞那肽类似物以提高患者的依从性和便利性。
在本综述中，作者报告了2012年至2015年期间与艾塞那肽及其类似物相关的专利。这些专利根据用于开发新化学实体的技术分为三类：1）化学生物共轭类似物；2）重组融合蛋白类似物；3）多功能肽类似物。
近年来，对艾塞那肽及其类似物的研究显著增加，推动了长效类似物和多功能肽的开发。虽然长效注射剂仍是制药行业的主要产品，但口服艾塞那肽的开发有望实现显著增长。
