PEGylated Biopharmaceuticals: Current Experience and Considerations for Nonclinical Development

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