Comparison study of [18F] FAl-NOTA-PRGD2, [18F] FPPRDG2 and [68Ga] Ga-NOTA-PRGD2 for PET imaging of U87MG tumors in mice

Wednesday, October 26, 2011 — Poster Session III
10:00 a.m. – Noon	Natcher Conference Center	NIBIB	IMAG-20

Authors

• W Li
• L Lang
• N Guo
• Y Ma
• DO Kiesewetter
• G Niu
• X Chen

Abstract

Among the various radiolabeled RGD peptides, [18F]FPPRGD2, an F-18 labeled dimeric cyclic RGDyK peptide, has favorable properties for PET imaging of angiogenesis by targeting the v3 integrin receptor. This radiotracer has been approved by the FDA for use in a clinical trial. However, the time-consuming multiple-step synthetic procedure required for preparation may hinder widespread usage of this tracer. The recent discovery and development of F-18 fluorine-aluminum complex to radiolabel peptides provides a unique strategy for simplifying the labeling procedure. On the other hand, the easy to prepare [68Ga]-labeled NOTA-RGD derivatives have also been reported to have promising properties for tumor imaging. The purpose of this study was to prepare [18F]FPPRDG2, [18F]FAl-NOTA-PRGD2, and [68Ga]Ga-NOTA-PRGD2 and to compare their pharmacokinetics and tumor imaging properties using small animal PET. All three compounds showed high tracer uptake in U87MG tumors and high target-to-background ratio. The uptake in the liver, kidneys and muscle was similar for all three tracers with predominant renal clearance. In conclusion, [18F]FAl-NOTA-PRGD2 and [68Ga]Ga-NOTA-PRGD2 have similar or superior imaging properties and pharmacokinetics to those of [18F]FPPRGD2. Considering their ease of preparation and good imaging quality, [18F]FAl-NOTA-PRGD2 and [68Ga]NOTA-PRGD2 are promising alternatives to [18F]FPPRGD2 for PET imaging of tumor v3 integrin expression.

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