Song Jinxing, Su Dihan, Wu Hongbing, Guo Jeremy
WuXi Biologics, 190 Hedan Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
Pharmaceutics. 2025 Jun 19;17(6):798. doi: 10.3390/pharmaceutics17060798.
The mRNA vaccine has protected humans from the Coronavirus disease 2019 (COVID-19) and has taken the lead in reversing the epidemic efficiently. However, the Centre of Disease Control (CDC) reported and raised the alarm of allergic or acute inflammatory adverse reactions after vaccination with mRNA-LNP vaccines. Meanwhile, the US Food and Drug Administration (FDA) has added four black-box warnings in the instructions for mRNA-LNP vaccines. Numerous studies have proven that the observance of side effects after vaccination is indeed positively correlated to the level of anti-PEG antibodies (IgM or IgG), which are enhanced by PEGylated preparations like LNP vaccine and environmental exposure. After literature research and review in the past two decades, it was found that the many clinical trial failures (BIND-014, RB006 fell in phase II) of PEG modified delivery system or PEGylated drug were related to the high expression of anti-PEG IgM and IgG. In the background of shooting multiple mRNA-LNP vaccines in billions of people around the world in the past three years, the level of anti-PEG antibodies in the population may have significantly increased, which brings potential risks for PEG-modified drug development and clinical safety. This review summarizes the experience of using mRNA-LNP vaccines from the mechanism of the anti-PEG antibodies generation, detection methods, clinical failure cases of PEG-containing products, harm analysis of abuse of PEGylation, and alternatives. In light of the increasing prevalence of anti-PEG antibodies in the population and the need to avoid secondary injuries, this review article holds greater significance by offering insights for drug developers. It suggests avoiding the use of PEG excipients when designing PEGylated drugs or PEG-modified nano-formulations and provides references for strategies such as utilizing PEG-free or alternative excipients.
mRNA疫苗保护人类免受2019冠状病毒病(COVID-19)侵害,并率先有效扭转了疫情。然而,疾病控制中心(CDC)报告并敲响了接种mRNA-LNP疫苗后出现过敏或急性炎症不良反应的警钟。与此同时,美国食品药品监督管理局(FDA)在mRNA-LNP疫苗说明书中增加了四项黑框警告。大量研究证明,接种疫苗后副作用的出现确实与抗聚乙二醇抗体(IgM或IgG)水平呈正相关,而LNP疫苗等聚乙二醇化制剂和环境暴露会增强这些抗体。经过对过去二十年的文献研究和综述发现,聚乙二醇修饰的递送系统或聚乙二醇化药物的许多临床试验失败案例(BIND-014、RB006在II期失败)都与抗聚乙二醇IgM和IgG的高表达有关。在过去三年全球数十亿人接种多种mRNA-LNP疫苗的背景下,人群中的抗聚乙二醇抗体水平可能已显著上升,这给聚乙二醇修饰药物的开发和临床安全性带来了潜在风险。本综述从抗聚乙二醇抗体产生的机制、检测方法、含聚乙二醇产品的临床失败案例、聚乙二醇化滥用的危害分析以及替代方案等方面总结了使用mRNA-LNP疫苗的经验。鉴于人群中抗聚乙二醇抗体的患病率不断上升以及避免二次伤害的必要性,这篇综述文章为药物开发者提供了见解,具有更大的意义。它建议在设计聚乙二醇化药物或聚乙二醇修饰的纳米制剂时避免使用聚乙二醇辅料,并为使用无聚乙二醇或替代辅料等策略提供参考。