聚乙二醇定点修饰蛋白质药物的技术和临床研究进展  

The Technique and Clinical Development of Site-specific PEGylated Protein Drugs

作　　者：杨凯睿[1] 高向东[1] 徐晨[2] 童梅[2] 陆小冬[2] 

机构地区：[1]中国药科大学生命科学与技术学院,江苏南京210000 [2]北京三元基因工程有限公司,北京102600

出　　处：《现代生物医学进展》2015年第32期6381-6385,6301,共6页Progress in Modern Biomedicine

基　　金：北京市科技计划项目(D08080200290808)

摘　　要：聚乙二醇(PEG)定点修饰蛋白药物是针对蛋白特定基团特定位点的修饰,相比于非定点随机修饰的特点是PEG修饰位点的单一与确定,避免了修饰异构体的干扰,能较好的保留药物体内外活性;修饰产物组成均一、性质稳定,便于质量控制,降低由修饰异构体引起的潜在的安全性风险,并很大程度上提高得率,降低成本。已有PEG定点修饰蛋白药物上市,还有部分处于临床试验阶段。本文综述了PEG定点修饰蛋白药物的技术研究与临床进展,包括PEG定点修饰剂、定点修饰方法、PEG定点修饰的上市和临床药物及面临的问题,并展望了PEG修饰技术未来的发展前景。Site-specific polyethylene glycol （PEG） modification is the PEGylation of specific site of the protein. Compared with non-specific PEGylation, the advantages of site-specific PEGylation are the uniqueness of PEGylated site, no interference of modified isomers, preserved activity in vitro and in vivo; the modified product is homogeneous, stable, and convenient for quality control, and can reduce side effects of modified isomers, increase production yield and decrease costs. Site-specific PEGylation protein drugs are already on the market, others are still in clinical trials. This paper reviews the research progress of technique and clinical development of site-specific PEGylated protein drugs, including typical site-specific PEG modifiers, general methods of site-specific PEGylation, site-specific PEGylated drugs on the market and in clinical development, and problems faced with by researchers, and looks into the future development of site-specific PEG modification technique.

关 键 词：聚乙二醇定点修饰 定点修饰技术 PEG修饰药物 临床进展 

分 类 号：R914[医药卫生—药物化学]