PEGylation (the covalent binding of one or more polyethylene glycol molecules to another molecule) is a technology frequently used to improve the half-life and other pharmaceutical or pharmacological properties of proteins, peptides, and aptamers. To date, 11 PEGylated biopharmaceuticals have been approved and there is indication that many more are in nonclinical or clinical development. Adverse effects seen with those in toxicology studies are mostly related to the active part of the drug molecule and not to polyethylene glycol (PEG). In 5 of the 11 approved and 10 of the 17 PEGylated biopharmaceuticals in a 2013 industry survey presented here, cellular vacuolation is histologically observed in toxicology studies in certain organs and tissues. No other effects attributed to PEG alone have been reported. Importantly, vacuolation, which occurs mainly in phagocytes, has not been linked with changes in organ function in these toxicology studies. This article was authored through collaborative efforts of industry toxicologists/nonclinical scientists to address the nonclinical safety of large PEG molecules (>10 kilo Dalton) in PEGylated biopharmaceuticals. The impact of the PEG molecule on overall nonclinical safety assessments of PEGylated biopharmaceuticals is discussed, and toxicological information from a 2013 industry survey on PEGylated biopharmaceuticals under development is summarized. Results will contribute to the database of toxicological information publicly available for PEG and PEGylated biopharmaceuticals.

译文

PEG化(一种或多种聚乙二醇分子与另一种分子的共价结合)是一种经常用于改善蛋白质,肽和适体的半衰期以及其他药物或药理特性的技术。迄今为止,已经批准了11种PEG化生物药物,并且有迹象表明,还有更多的药物正在非临床或临床研究中。在毒理学研究中看到的不良反应主要与药物分子的活性部分有关,与聚乙二醇(PEG)无关。在此处呈现的2013年行业调查中,在11种已批准的11种PEG化生物药物中有5种在17种药物中,有10种在组织学上在某些器官和组织的毒理学研究中观察到了细胞空泡化。尚无单独归因于PEG的其他影响的报道。重要的是,在这些毒理学研究中,主要发生在吞噬细胞中的空泡化与器官功能的变化没有联系。本文是通过行业毒理学家/非临床科学家的共同努力撰写的,旨在解决PEG化生物药物中大PEG分子(> 10千道尔顿)的非临床安全性的问题。讨论了PEG分子对PEG化生物药品的整体非临床安全性评估的影响,并总结了2013年有关正在开发的PEG化生物药品行业调查的毒理学信息。结果将有助于公开可用于PEG和PEG化生物制药的毒理学信息数据库。

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