Tumor Detection Using Folate Receptor-Targeted Imaging Agents

Cancer Metastasis Rev. 2008 Dec;27(4):655-64. doi: 10.1007/s10555-008-9155-6.


Folate receptors are up-regulated on a variety of human cancers, including cancers of the breast, ovaries, endometrium, lungs, kidneys, colon, brain, and myeloid cells of hematopoietic origin. This over-expression of folate receptors (FR) on cancer tissues can be exploited to target folate-linked imaging and therapeutic agents specifically to FR-expressing tumors, thereby avoiding uptake by most healthy tissues that express few if any FR. Four folate-targeted therapeutic drugs are currently undergoing clinical trials, and several folate-linked chemotherapeutic agents are in late stage preclinical development. However, because not all cancers express FR, and because only FR-expressing cancers respond to FR-targeted therapies, FR-targeted imaging agents have been required to select patients with FR-expressing tumors likely to respond to folate-targeted therapies. This review focuses on recent advances in the use of the vitamin folic acid to target PET agents, gamma-emitters, MRI contrast agents and fluorescent dyes to FR(+) cancers for the purpose of diagnosing and imaging malignant masses with improved specificity and sensitivity.

Publication types

  • Review

MeSH terms

  • Animals
  • Carrier Proteins / administration & dosage*
  • Diagnostic Imaging*
  • Drug Delivery Systems / methods
  • Folate Receptors, GPI-Anchored
  • Folic Acid / administration & dosage*
  • Humans
  • Neoplasms / diagnosis*
  • Neoplasms / drug therapy
  • Neoplasms / metabolism
  • Radiopharmaceuticals*
  • Receptors, Cell Surface / administration & dosage*


  • Carrier Proteins
  • Folate Receptors, GPI-Anchored
  • Radiopharmaceuticals
  • Receptors, Cell Surface
  • Folic Acid