The Effect of Bi-Terminal PEGylation of an Integrin α_vβ₆–Targeted¹⁸F Peptide on Pharmacokinetics and Tumor Uptake

Abstract

The bi-PEGylated radiotracer 5 showed a greatly improved pharmacokinetic profile, beyond what was predicted from individual N- or C-terminal PEGylation. It appears that the 2 PEG units acted synergistically to result in an improved metabolic profile including high αvβ6+ tumor uptake and retention.