J Mater Chem B. 2021 Apr 7;9(13):2993-2997. doi: 10.1039/d0tb02911d. Epub 2021 Mar 16.
A short PEG linker alters the in vivo pharmacokinetics of trastuzumab to yield high-contrast immuno-PET images
Abstract
The prolonged blood circulation of the radiolabeled antibody conjugates is problematic when using immuno-PET imaging due to the increased radiation exposure and longer hospitalization required until sufficient contrast develops. In contrast to the prevailing belief that PEGylation prolongs blood retention time, we observed that a PEGylated antibody with a short PEG8 linker cleared much faster from the blood while maintaining tumor uptake compared to its non-PEGylated counterpart. Breast tumors were clearly visualized with a very high tumor-to-background ratio as early as 24 h after injection in immuno-positron emission tomography (PET) imaging.
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