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Biodistribution and dosimetry of [I-123]iodo-PK 11195: a potential agent for SPET imaging of the peripheral benzodiazepine receptor

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Abstract
The highest concentrations of the peripheral benzodiazepine receptor (PBR) are found in the kidneys and heart. In addition, the PER has been reported to reflect neuro-inflammatory damage by co-localisation with activated microglia. PK 11195 is a high-affinity ligand for the PER. The aim of this study was to investigate in humans the biodistribution and dosimetry of [I-123]iodo-PK 11195, a potential single-photon emission tomography tracer for the PER. Five healthy volunteers were injected with 112 MBq of [I-123]iodo-PK 11195. Sequential whole-body scans were performed up to 72 h post injection. Multiple blood samples were taken, and urine was collected to measure the fraction voided by the renal system. Decay-corrected regions of interest of the whole-body images were analysed, and geometric mean count rates were used to determine organ activity. Organ absorbed doses and effective dose were calculated using the MIRD method. [I-123]iodo-PK 11195 was rapidly cleared from the blood, mainly by the hepatobiliary system. Approximately 22% was voided in urine after 48 h. Average organ residence times were 0.74, 0.44 and 0.29 h for the liver, upper large intestine and lower large intestine, respectively. The testes received the highest dose. 109.4 mu Gy/MBq. All other organs investigated received doses of less than 50 mu Gy/MBq. The effective dose was 40.3 mu Sv/MBq. In conclusion, [I-123]iodo-PK 11195 is a suitable agent for the visualisation of the PER and indirectly for the imaging of neuro-inflammatory lesions. Taking into account the radiation burden of 7.46 mSv following an administration of 185 MBq, a [I-123]iodo-PK 11195 investigation has to be considered an ICRP risk category IIb investigation.
Keywords
SITES, BRAIN, PK 11195, PK11195 BINDING, I-123 IODO-PK11195, IN-VIVO, ACTIVATED MICROGLIA, RAT CEREBRAL-CORTEX, DIAZEPAM-BINDING INHIBITOR, POSITRON-EMISSION-TOMOGRAPHY

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MLA
Versijpt, JAN, Filip Dumont, Hubert Thierens, et al. “Biodistribution and Dosimetry of [I-123]iodo-PK 11195: a Potential Agent for SPET Imaging of the Peripheral Benzodiazepine Receptor.” EUROPEAN JOURNAL OF NUCLEAR MEDICINE 27.9 (2000): 1326–1333. Print.
APA
Versijpt, JAN, Dumont, F., Thierens, H., Jansen, H., De Vos, F., Slegers, G., Santens, P., et al. (2000). Biodistribution and dosimetry of [I-123]iodo-PK 11195: a potential agent for SPET imaging of the peripheral benzodiazepine receptor. EUROPEAN JOURNAL OF NUCLEAR MEDICINE, 27(9), 1326–1333.
Chicago author-date
Versijpt, JAN, Filip Dumont, Hubert Thierens, Hugo Jansen, Filip De Vos, G Slegers, Patrick Santens, Rudi Dierckx, and J Korf. 2000. “Biodistribution and Dosimetry of [I-123]iodo-PK 11195: a Potential Agent for SPET Imaging of the Peripheral Benzodiazepine Receptor.” European Journal of Nuclear Medicine 27 (9): 1326–1333.
Chicago author-date (all authors)
Versijpt, JAN, Filip Dumont, Hubert Thierens, Hugo Jansen, Filip De Vos, G Slegers, Patrick Santens, Rudi Dierckx, and J Korf. 2000. “Biodistribution and Dosimetry of [I-123]iodo-PK 11195: a Potential Agent for SPET Imaging of the Peripheral Benzodiazepine Receptor.” European Journal of Nuclear Medicine 27 (9): 1326–1333.
Vancouver
1.
Versijpt J, Dumont F, Thierens H, Jansen H, De Vos F, Slegers G, et al. Biodistribution and dosimetry of [I-123]iodo-PK 11195: a potential agent for SPET imaging of the peripheral benzodiazepine receptor. EUROPEAN JOURNAL OF NUCLEAR MEDICINE. 2000;27(9):1326–33.
IEEE
[1]
J. Versijpt et al., “Biodistribution and dosimetry of [I-123]iodo-PK 11195: a potential agent for SPET imaging of the peripheral benzodiazepine receptor,” EUROPEAN JOURNAL OF NUCLEAR MEDICINE, vol. 27, no. 9, pp. 1326–1333, 2000.
@article{134249,
  abstract     = {The highest concentrations of the peripheral benzodiazepine receptor (PBR) are found in the kidneys and heart. In addition, the PER has been reported to reflect neuro-inflammatory damage by co-localisation with activated microglia. PK 11195 is a high-affinity ligand for the PER. The aim of this study was to investigate in humans the biodistribution and dosimetry of [I-123]iodo-PK 11195, a potential single-photon emission tomography tracer for the PER. Five healthy volunteers were injected with 112 MBq of [I-123]iodo-PK 11195. Sequential whole-body scans were performed up to 72 h post injection. Multiple blood samples were taken, and urine was collected to measure the fraction voided by the renal system. Decay-corrected regions of interest of the whole-body images were analysed, and geometric mean count rates were used to determine organ activity. Organ absorbed doses and effective dose were calculated using the MIRD method. [I-123]iodo-PK 11195 was rapidly cleared from the blood, mainly by the hepatobiliary system. Approximately 22% was voided in urine after 48 h. Average organ residence times were 0.74, 0.44 and 0.29 h for the liver, upper large intestine and lower large intestine, respectively. The testes received the highest dose. 109.4 mu Gy/MBq. All other organs investigated received doses of less than 50 mu Gy/MBq. The effective dose was 40.3 mu Sv/MBq. In conclusion, [I-123]iodo-PK 11195 is a suitable agent for the visualisation of the PER and indirectly for the imaging of neuro-inflammatory lesions. Taking into account the radiation burden of 7.46 mSv following an administration of 185 MBq, a [I-123]iodo-PK 11195 investigation has to be considered an ICRP risk category IIb investigation.},
  author       = {Versijpt, JAN and Dumont, Filip and Thierens, Hubert and Jansen, Hugo and De Vos, Filip and Slegers, G and Santens, Patrick and Dierckx, Rudi and Korf, J},
  issn         = {0340-6997},
  journal      = {EUROPEAN JOURNAL OF NUCLEAR MEDICINE},
  keywords     = {SITES,BRAIN,PK 11195,PK11195 BINDING,I-123 IODO-PK11195,IN-VIVO,ACTIVATED MICROGLIA,RAT CEREBRAL-CORTEX,DIAZEPAM-BINDING INHIBITOR,POSITRON-EMISSION-TOMOGRAPHY},
  language     = {eng},
  number       = {9},
  pages        = {1326--1333},
  title        = {Biodistribution and dosimetry of [I-123]iodo-PK 11195: a potential agent for SPET imaging of the peripheral benzodiazepine receptor},
  url          = {http://dx.doi.org/10.1007/s002590000295},
  volume       = {27},
  year         = {2000},
}

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