PET imaging with radiolabeled antibodies and tyrosine kinase inhibitors: immuno-PET and TKI-PET

Tumour Biol. 2012 Jun;33(3):607-15. doi: 10.1007/s13277-012-0316-4. Epub 2012 Jan 21.


During the last decade, the discovery of critical tumor targets has boosted the design of targeted therapeutic agents with monoclonal antibodies (mAbs) and tyrosine kinase inhibitors (TKIs) receiving most of the attention. Immuno-positron emission tomography (immuno-PET) and TKI-PET, the in vivo tracking and quantification of mAbs and TKIs biodistribution with PET, are exciting novel options for better understanding of the in vivo behavior and efficacy of these targeted drugs in individual patients and for more efficient drug development. Very recently, current good manufacturing practice compliant procedures for labeling of mAbs with positron emitters have been described, as well as the preparation of some radiolabeled TKIs, while the first proof of principle studies has been performed in patients. In this review, technical developments in immuno-PET and TKI-PET are described, and their clinical potential is discussed. An overview is provided for the most appealing preclinical immuno-PET and TKI-PET studies, as well as the first clinical achievements with these emerging technologies.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / therapeutic use*
  • Drug Evaluation, Preclinical
  • Humans
  • Immunoconjugates / therapeutic use*
  • Molecular Targeted Therapy
  • Neoplasms / diagnostic imaging
  • Neoplasms / drug therapy*
  • Positron-Emission Tomography*
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Radioisotopes


  • Antibodies, Monoclonal
  • Immunoconjugates
  • Protein Kinase Inhibitors
  • Radioisotopes
  • Protein-Tyrosine Kinases