TY - JOUR
T1 - Whole-body biodistribution and radiation dosimetry of 18F-FP-(+) -DTBZ (18F-AV-133)
T2 - A novel vesicular monoamine transporter 2 imaging agent
AU - Lin, Kun Ju
AU - Weng, Yi Hsin
AU - Wey, Shiaw Pyng
AU - Hsiao, Ing Tsung
AU - Lu, Chin Song
AU - Skovronsky, Daniel
AU - Chang, Hsiu Ping
AU - Kung, Mei Ping
AU - Yen, Tzu Chen
PY - 2010/9
Y1 - 2010/9
N2 - Vesicular monoamine transporter 2 (VMAT2) is highly expressed in the endocrine cells and brain. We investigated the biodistribution and radiation dosimetry of (2R,3R,11bR)-9-(3-18F-fluoropropoxy)-3-isobutyl-10- methoxy-2,3,4,6,7, 11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-ol ( 18F-FP-(+)-dihydrotetrabenazine [DTBZ] or 18F-AV-133), a potential VMAT2 imaging agent showing encouraging results in humans, to facilitate its future clinical use. Methods: Nine healthy human subjects (mean age ± SD, 58.6 ± 4.2 y) were enrolled for the whole-body PET scan. Serial images were acquired for 3 h immediately after a bolus injection of 390.7 ± 22.9 MBq of 18F-AV-133 per individual. The source organs were delineated on PET/CT images. The OLINDA/EXM application was used to determine the equivalent dose for individual organs. Results: The radiotracer did not show any noticeable adverse effects for the 9 subjects examined. The radioactivity uptake in the brain was the highest at 7.5% ± 0.6% injected dose at 10 min after injection. High absorbed doses were found in the pancreas, liver, and upper large intestine wall. The highest-dosed organ, which received 153.3 ± 23.8 μGy/MBq, was the pancreas. The effective dose equivalent and effective dose for 18F-AV-133 were 36.5 ± 2.8 and 27.8 ± 2.5 μSv/MBq, respectively. These values are comparable to those reported for any other 18F-labeled radiopharmaceutical. Conclusion: 18F-AV-133 is safe, with appropriate biodistribution and radiation dosimetry for imaging VMAT2 sites in humans. COPYRIGHT
AB - Vesicular monoamine transporter 2 (VMAT2) is highly expressed in the endocrine cells and brain. We investigated the biodistribution and radiation dosimetry of (2R,3R,11bR)-9-(3-18F-fluoropropoxy)-3-isobutyl-10- methoxy-2,3,4,6,7, 11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-ol ( 18F-FP-(+)-dihydrotetrabenazine [DTBZ] or 18F-AV-133), a potential VMAT2 imaging agent showing encouraging results in humans, to facilitate its future clinical use. Methods: Nine healthy human subjects (mean age ± SD, 58.6 ± 4.2 y) were enrolled for the whole-body PET scan. Serial images were acquired for 3 h immediately after a bolus injection of 390.7 ± 22.9 MBq of 18F-AV-133 per individual. The source organs were delineated on PET/CT images. The OLINDA/EXM application was used to determine the equivalent dose for individual organs. Results: The radiotracer did not show any noticeable adverse effects for the 9 subjects examined. The radioactivity uptake in the brain was the highest at 7.5% ± 0.6% injected dose at 10 min after injection. High absorbed doses were found in the pancreas, liver, and upper large intestine wall. The highest-dosed organ, which received 153.3 ± 23.8 μGy/MBq, was the pancreas. The effective dose equivalent and effective dose for 18F-AV-133 were 36.5 ± 2.8 and 27.8 ± 2.5 μSv/MBq, respectively. These values are comparable to those reported for any other 18F-labeled radiopharmaceutical. Conclusion: 18F-AV-133 is safe, with appropriate biodistribution and radiation dosimetry for imaging VMAT2 sites in humans. COPYRIGHT
KW - Dosimetry
KW - PET
KW - Parkinson disease
KW - Vesicular monoamine transporter 2
KW - Whole-body biodistribution
UR - https://www.scopus.com/pages/publications/77957028183
U2 - 10.2967/jnumed.110.078196
DO - 10.2967/jnumed.110.078196
M3 - 文章
C2 - 20720042
AN - SCOPUS:77957028183
SN - 0161-5505
VL - 51
SP - 1480
EP - 1485
JO - Journal of Nuclear Medicine
JF - Journal of Nuclear Medicine
IS - 9
ER -