The biodistribution and radiation dosimetry of the Arg-Gly-Asp peptide 18F-AH111585 in healthy volunteers.
We report the safety, biodistribution, and internal radiation dosimetry of a new PET tracer, (18)F-AH111585, a peptide with a high affinity for the alpha(v)beta(3) 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 (18)F-AH111585. (18)F activity in whole blood and plasma and excreted urine were measured up to 4 h after injection. In vivo (18)F 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 (18)F-AH111585 was well tolerated in all subjects, with no serious or drug-related adverse events reported. The main route of (18)F 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 microGy/MBq), kidneys (102 microGy/MBq), and cardiac wall (59 microGy/MBq). The effective dose was 26 microGy/MBq.


CONCLUSIONS
(18)F-AH111585 is a safe PET tracer with a dosimetry profile comparable to other common (18)F PET tracers.
McParland
Brian J
BJ
Medical Diagnostics, GE Healthcare Ltd., Amersham, Buckinghamshire, England. brian.mcparland@ge.com
Miller
Matthew P
MP
Spinks
Terence J
TJ
Kenny
Laura M
LM
Osman
Safiye
S
Khela
Mandeep K
MK
Aboagye
Eric
E
Coombes
Raoul C
RC
Hui
Ai-Min
AM
Cohen
Pamela S
PS
D000368:Aged; D001120:Arginine / Q000737:chemistry; D001224:Aspartic Acid / Q000737:chemistry; D001384:Azetidines / Q000493:pharmacokinetics*; D005260:Female; D005998:Glycine / Q000737:chemistry; D006801:Humans; D008297:Male; D008875:Middle Aged; D010455:Peptides / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods*; D011725:Pyridines / Q000493:pharmacokinetics*; D011829:Radiation Dosage; D011874:Radiometry / Q000379:methods*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D014018:Tissue Distribution
C119803:2-fluoro-3-(2-azetidinylmethoxy)pyridine; D001384:Azetidines; D010455:Peptides; D011725:Pyridines; D019275:Radiopharmaceuticals; D001224:Aspartic Acid; D001120:Arginine; D005998:Glycine