Human biodistribution and internal dosimetry of 4-[ 18 F]fluorobenzyl-dexetimide: a PET radiopharmaceutical for imaging muscarinic acetylcholine receptors in the brain and heart

EJNMMI Research
Cameron D PainChristopher C Rowe

Abstract

4-[18F] fluorobenzyl dexetimide (F-DEX) is the first non-subtype selective fluorine-18 labelled tracer for muscarinic receptors (mAChR) used in humans. A recent first-in-human study found high regional brain uptake with low variation in normal subjects. Disturbance of mAChR has been reported in Alzheimer's and Parkinson's disease, schizophrenia and depression and various cardiac diseases. The following work assesses the biodistribution, organ tracer kinetics and radiation dose associated with F-DEX. Dose calculations were based on activity uptake derived from multiple time point whole body PET CT imaging and the organ-specific dosimetric S-factors derived from the ICRP 133 standard man and woman mathematical phantoms. Effective doses were calculated using the latest ICRP tissue weighting factors. Serial images and time activity curves demonstrate high brain and left ventricular myocardial uptake (5% and 0.65% of injected activity, respectively) with greater retention in brain than myocardium. The mean effective dose was in concordance with other 18F labelled tracers at 19.70 ± 2.27 μSv/MBq. The largest absorbed doses were in the liver (52.91 ± 1.46 μGy/MBq) and heart wall (43.94 ± 12.88 μGy/MBq) for standard man and the liver (...Continue Reading

References

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Jan 24, 2009·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Graeme J O'KeefeChristopher C Rowe
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Mar 22, 2013·EJNMMI Research·Hans Jc BuiterJosée E Leysen

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Citations

Jul 3, 2021·Pharmaceuticals·Marius OzenilVerena Pichler
Aug 17, 2021·Psychiatry Research. Neuroimaging·Christopher C RoweVictor L Villemagne

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