What is the future of PEGylated therapies?
What is the future of PEGylated therapies?
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DOI：
10.1517/14728214.2015.1113254
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发表时间：
2015
影响因子：
3.4
通讯作者：
Lee S
中科院分区：
文献类型：
--
作者：
Swierczewska M;Lee KC;Lee S
生物药物的巨大潜力受到体内半衰期短的阻碍，导致效力明显低于体外活性。这些短效治疗剂需要频繁的给药曲线，这可能降低对临床的适用性，特别是对于慢性病症。因此，半衰期延长技术正在进入临床，以实现改进的或新的生物疗法。聚乙二醇化是第一个成功改善治疗药物药代动力学（PK）特征的技术，已在临床上应用超过25年。自20世纪90年代初以来，已有超过10种聚乙二醇化治疗药物进入临床，新的聚乙二醇化药物继续扩大临床管道和药物专利寿命。聚乙二醇化是临床上最成熟的半衰期延长技术，二十多年来在人类中证明了其安全性。尽管如此，它仍然是未来二十年将应用的最具发展性和新兴的技术之一。
The tremendous potential of biologic drugs is hampered by short half-lives in vivo, resulting in significantly lower potency than activity seen in vitro. These short-acting therapeutic agents require frequent dosing profiles that can reduce applicability to the clinic, particularly for chronic conditions. Therefore, half-life extension technologies are entering the clinic to enable improved or new biologic therapies. PEGylation is the first successful technology to improve pharmacokinetic (PK) profiles of therapeutic agents and has been applied in the clinic for over 25 years. Over 10 PEGylated therapeutics have entered the clinic since the early 1990s, and new PEGylated agents continue to expand clinical pipelines and drug patent life. PEGylation is the most established half-life extension technology in the clinic with proven safety in humans for over two decades. Still, it is one of the most evolving and emerging technologies that will be applied for the next two decades.