First in Man Study of [F]fluoro-PEG-folate PET: a Novel Macrophage Imaging Technique to Visualize Rheumatoid Arthritis

Overview

Journal Sci Rep

Specialty Science

Date 2020 Jan 25

PMID 31974480

Citations 29

Authors

Nicki J F Verweij

Maqsood Yaqub

Stefan T G Bruijnen

S Pieplenbosch

Marieke M Ter Wee

Gerrit Jansen

Qingshou Chen

Philip S Low

Albert D Windhorst

Adriaan A Lammertsma

Otto S Hoekstra

Alexandre E Voskuyl

Conny J van der Laken

Affiliations

Soon will be listed here.

Abstract

Non-invasive imaging of arthritis activity in rheumatoid arthritis (RA) patients using macrophage PET holds promise for early diagnosis and therapeutic response monitoring. Previously obtained results with macrophage tracer (R)-[C]PK11195 were encouraging, but the imaging signal could be further improved by reduction of background uptake. Recently, the novel macrophage tracer [F]fluoro-PEG-folate was developed. This tracer showed excellent targeting of the folate receptor β on activated macrophages in synovial tissue in a preclinical arthritic rat model. We performed three substudies to investigate the biodistribution, potential for imaging arthritis and kinetic properties of [18F]fluoro-PEG-folate in RA patients. Firstly, biodistribution demonstrated fast clearance of [F]fluoro-PEG-folate from heart and blood vessels and no dose limiting uptake in organs. Secondly, [F]fluoro-PEG-folate showed uptake in arthritic joints with significantly lower background and hence significantly higher target-to-background ratios as compared to reference macrophage tracer (R)-[C]PK11195. Lastly, dynamic scanning demonstrated fast tracer uptake in affected joints, reaching a plateau after 1 minute, co-existing with a rapid blood clearance. In conclusion, this first in man study demonstrates the potential of [F]fluoro-PEG-folate to image arthritis activity in RA with favourable imaging characteristics of rapid clearance and low background uptake, that allow for detection of inflammatory activity in the whole body.

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