Pretargeted Imaging and Therapy

J Nucl Med. 2017 Oct;58(10):1553-1559. doi: 10.2967/jnumed.117.189944. Epub 2017 Jul 7.


In vivo pretargeting stands as a promising approach to harnessing the exquisite tumor-targeting properties of antibodies for nuclear imaging and therapy while simultaneously skirting their pharmacokinetic limitations. The core premise of pretargeting lies in administering the targeting vector and radioisotope separately and having the 2 components combine within the body. In this manner, pretargeting strategies decrease the circulation time of the radioactivity, reduce the uptake of the radionuclide in healthy nontarget tissues, and facilitate the use of short-lived radionuclides that would otherwise be incompatible with antibody-based vectors. In this short review, we seek to provide a brief yet informative survey of the 4 preeminent mechanistic approaches to pretargeting, strategies predicated on streptavidin and biotin, bispecific antibodies, complementary oligonucleotides, and bioorthogonal click chemistry.

Keywords: biotin; bispecific antibody; click chemistry; multistep targeting; pretargeting; streptavidin.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Diagnostic Imaging / methods*
  • Humans
  • Immunoconjugates / chemistry
  • Immunoconjugates / genetics
  • Immunoconjugates / metabolism
  • Immunoconjugates / therapeutic use
  • Molecular Targeted Therapy / methods*


  • Immunoconjugates