Comparison of Ga-68-Labeled Fusarinine C-Based Multivalent RGD Conjugates and 68GaNODAGA-RGD—In Vivo Imaging Studies in Human Xenograft Tumors

摘要

PurposeMultimeric arginine-glycine-aspartic acid (RGD) peptides have advantages for imaging integrin αvβ3 expression. Here, we compared the in vitro and in vivo behavior of three different Ga-68-labeled multimeric Fusarinine C-RGD (FSC-RGD) conjugates, whereby RGD was coupled directly, via a succinic acid or PEG linker (FSC(RGDfE)3, FSC(succ-RGD)3, FSC(Mal-RGD)3). The positron emission tomography/X-ray computed tomography (PET/CT) imaging properties were further compared using [⁶⁸Ga]FSC(succ-RGD)3 with the monomeric [⁶⁸Ga]NODAGA-RGD in a murine tumor model.