Biodistribution and radiation dosimetry in humans of a new PET ligand, (18)F-PBR06, to image translocator protein (18 kDa)

J Nucl Med. 2010 Jan;51(1):145-9. doi: 10.2967/jnumed.109.068064. Epub 2009 Dec 15.

Abstract

As a PET biomarker for inflammation, translocator protein (18 kDa) (TSPO) can be measured with an (18)F-labeled aryloxyanilide, (18)F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline ((18)F-PBR06), in the human brain. The objective of this study was to estimate the radiation absorbed doses of (18)F-PBR06 based on biodistribution data in humans.

Methods: After the injection of (18)F-PBR06, images were acquired from head to thigh in 7 healthy humans. Urine was collected at various time points. Radiation absorbed doses were estimated by the MIRD scheme.

Results: Moderate to high levels of radioactivity were observed in organs with high densities of TSPO and in organs of metabolism and excretion. Bone had low levels of radioactivity. The effective dose was 18.5 muSv/MBq.

Conclusion: The effective dose of (18)F-PBR06, compared with other (18)F radioligands, was moderate. This radioligand had negligible defluorination, as indirectly assessed by bone radioactivity. Doses to the gallbladder wall and spleen may limit the amount of permissible injected radioactivity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural

MeSH terms

  • Acetanilides / administration & dosage*
  • Acetanilides / pharmacokinetics*
  • Acetanilides / pharmacology
  • Adult
  • Biotransformation
  • Blood Pressure / drug effects
  • Bone and Bones / metabolism
  • Electrocardiography / drug effects
  • Female
  • Heart Rate / drug effects
  • Humans
  • Male
  • Positron-Emission Tomography
  • Radiometry
  • Radiopharmaceuticals / administration & dosage*
  • Radiopharmaceuticals / pharmacokinetics*
  • Radiopharmaceuticals / pharmacology
  • Receptors, GABA / metabolism*
  • Respiratory Mechanics / drug effects
  • Tissue Distribution

Substances

  • Acetanilides
  • N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline
  • Radiopharmaceuticals
  • Receptors, GABA
  • TSPO protein, human