Biodistribution and Radiation Dosimetry of the Integrin Marker ¹⁸F-RGD-K5 Determined from Whole-Body PET/CT in Monkeys and Humans

Cyclic RGD peptide-modified liposomal drug delivery system for targeted oral apatinib administration: enhanced cellular uptake and improved therapeutic effects

“…[35][36][37][38] In addition, tissue sections, biodistribution, and pharmacokinetics of cRGD-peptide-conjugated quantum dots (QDs), 39 gold nanoclusters, 40 doxorubicin-loaded nanoparticles, 41 polymeric micelles, 42 and dendrimers 43 were imaged or analyzed in mice bearing tumor xenografts, confirming specific tumor targeting. All the results presented here as well as reports in the literature suggest that cRGD-Lipo-PEG liposomes would result in improved tumor inhibition in mouse models.…”

Interrogating Tumor Metabolism and Tumor Microenvironments Using Molecular Positron Emission Tomography Imaging. Theranostic Approaches to Improve Therapeutics

“…[ 18 F]RGD-K5 was found to be stable in human blood and cleared rapidly from the blood pool. High uptake of [ 18 F]RGD-K5 was observed in the kidneys, bladder, liver, intestine, and gallbladder in healthy volunteers, indicating that the peptide modification did not achieve its goal (Doss et al, 2012 (Kenny et al, 2008). Cell studies showed that [ 18 F]fluciclatide was not selective to a v b 3 and had 100-fold higher affinity to integrin a v b 5 .…”

“…This derivative contains a highly polar 1,2,3-antitriazole moiety that increases the tracer's excretion via the kidneys into the bladder, thus circumventing unwanted liver uptake (Doss et al, 2012). [ 18 F]RGD-K5 was found to be stable in human blood and cleared rapidly from the blood pool.…”

A novel PET tracer for targeted imaging of atherosclerosis

“…20 Moreover, it exhibits a favourable biodistribution and safety profile in healthy volunteers with rapid clearance from blood (*12 minutes) and primary excretion through the kidneys. The highest [18F]-RGD-K5 activity was found in the renal system, liver and guts while a near-to-background activity was observed in the heart following injection.…”