Folic acid conjugates for nuclear imaging of folate receptor-positive cancer

J Nucl Med. 2011 Jan;52(1):1-4. doi: 10.2967/jnumed.110.076018. Epub 2010 Dec 13.


The folate receptor (FR) is overexpressed on a variety of tumor types, whereas its distribution in normal tissues and organs is highly limited. Exploration of the utility of the FR revealed its promising potential for targeting with folate-based radiopharmaceuticals. Herein, we report the principle of the FR-targeting strategy and summarize the development of several folic acid radioconjugates useful for SPECT and PET of cancer diseases. The potential applicability of folate radiopharmaceuticals for FR-targeted radionuclide therapy is also discussed.

MeSH terms

  • Folate Receptors, GPI-Anchored / analysis*
  • Folic Acid / metabolism*
  • Humans
  • Neoplasms / diagnostic imaging*
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals*
  • Tomography, Emission-Computed, Single-Photon / methods*


  • Folate Receptors, GPI-Anchored
  • Radiopharmaceuticals
  • Folic Acid