Pilot Pharmacokinetic and Dosimetric Studies of¹⁸F-FPPRGD2: A PET Radiopharmaceutical Agent for Imaging α_vβ₃Integrin Levels

Abstract

Purpose:To assess the safety, biodistribution, and dosimetric properties of the positron emission tomography (PET) radiopharmaceutical agent fl uorine 18 ( 18 F) FPPRGD2 (2-fl uoropropionyl labeled PEGylated dimeric RGD peptide [PEG3-E{c(RGDyk)}2]), which is based on the dimeric arginine-glycine-aspartic acid (RGD) peptide sequence and targets a v b 3 integrin, in the fi rst volunteers imaged with this tracer. Materials and Methods:The protocol was approved by the institutional review board, and written informed consent was obtained from all participants. Five healthy volunteers underwent whole-body combined PET-computed tomography 0.5, 1.0, 2.0, and 3.0 hours after tracer injection (mean dose, 9.5 mCi 6 3. Results:The administration of With an injected dose of 10 mCi (370 MBq) and a 1-hour voiding interval, a patient would be exposed to an effective radiation dose of 1.5 rem (15 mSv). Above the diaphragm, there was minimal uptake in the brain ventricles, salivary glands, and thyroid gland. Time-activity curves showed rapid clearance from the vasculature, with a mean 26% 6 17 of the tracer remaining in the circulation at 30 minutes and most of the activity occurring in the plasma relative to cells (mean whole blood-plasma ratio, 0.799 6 0.096).

A Molecular Imaging Primer: Modalities, Imaging Agents, and Applications

“…Peptide imaging agents can be used to visualize a range of targets, including integrins (20,57,294), matrix metalloproteinases (36,187), caspases (91,95), somatostatin receptors (82,136,331), neuropeptide Y receptor (253,485), and gastrin releasing peptide receptor (372,427,428). See TABLE 2 for some specific examples of peptide molecular imaging agents that can be used for optical, PET, and SPECT imaging.…”

Clinical Translation of a Dual Integrin αvβ3– and Gastrin-Releasing Peptide Receptor–Targeting PET Radiotracer, 68Ga-BBN-RGD

“…With a typical 130 MBq (3.5 mCi) injected activity of 68 Ga-BBN, the whole-body effective dose is 2.90 mSv, which is much lower than the dose limit set by the Food and Drug Administration (27). All these data confirmed the safety of 68 Ga-BBN for further clinical applications.…”

Magnetic Resonance Imaging and Positron Emission Tomography Approaches to Imaging Vascular and Cardiac Inflammation

“…29 Proteases Because of the various implications of proteases produced by macrophages in atherosclerosis and aneurysms, activity-based probe tracers have been developed and tested preclinically, targeting MMPs (eg, P947) or cathepsins (eg, ABP BMV101). 30 Fibrosis T1 mapping has the potential to provide quantitative assessment of more diffuse myocardial fibrosis.…”