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First published online September 15, 2008, 10.2967/jnumed.108.052126
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Journal of Nuclear Medicine Vol. 49 No. 10 1664-1667
© 2008 by Society of Nuclear Medicine

doi: 10.2967/jnumed.108.052126

Basic Science Investigation

The Biodistribution and Radiation Dosimetry of the Arg-Gly-Asp Peptide 18F-AH111585 in Healthy Volunteers

Brian J. McParland1,2, Matthew P. Miller1, Terence J. Spinks3, Laura M. Kenny4, Safiye Osman3, Mandeep K. Khela1, Eric Aboagye4, Raoul C. Coombes4, Ai-Min Hui1 and Pamela S. Cohen1

1 Research and Development, Medical Diagnostics, GE Healthcare Ltd., Amersham, Buckinghamshire, England; 2 Global Imaging Network, GE Healthcare Medical Diagnostics, Grove Centre, Amersham, Buckinghamshire, England; 3 Hammersmith Imanet Ltd., Hammersmith Hospital, London, England; and 4 Department of Oncology, Imperial College Faculty of Medicine, Hammersmith Hospital, London, England

Correspondence: For correspondence or reprints contact: Brian J. McParland, Global Imaging Network, GE Healthcare Medical Diagnostics, Grove Centre GC/58, White Lion Rd., Amersham, Buckinghamshire, England HP7 9LL. E-mail: brian.mcparland{at}ge.com

We report the safety, biodistribution, and internal radiation dosimetry of a new PET tracer, 18F-AH111585, a peptide with a high affinity for the {alpha}vβ3 integrin receptor involved in angiogenesis. Methods: PET scans of 8 healthy volunteers were acquired at time points up to 4 h after a bolus injection of 18F-AH111585. 18F activity in whole blood and plasma and excreted urine were measured up to 4 h after injection. In vivo 18F activities in up to 12 source regions were determined from quantitative analysis of the images. The cumulated activities subsequently calculated were then used to determine the internal radiation dosimetry, including the effective dose. Results: Injection of 18F-AH111585 was well tolerated in all subjects, with no serious or drug-related adverse events reported. The main route of 18F excretion was renal (37%), and the 3 highest initial uptakes were by liver (15%); combined walls of the small, upper large, and lower large intestines (11%); and kidneys (9%). The 3 highest absorbed doses were received by the urinary bladder wall (124 µGy/MBq), kidneys (102 µGy/MBq), and cardiac wall (59 µGy/MBq). The effective dose was 26 µGy/MBq. Conclusion: 18F-AH111585 is a safe PET tracer with a dosimetry profile comparable to other common 18F PET tracers.

Key Words: 18F-AH111585 • {alpha}vβ3 expression • PET • dosimetry • whole-body biodistribution

COPYRIGHT © 2008 by the Society of Nuclear Medicine, Inc.


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