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Folate-receptor-targeted radionuclide imaging agents

Chun-Yen Ke1, Carla J Mathias, Mark A Green

  • 1Division of Nuclear Pharmacy, Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907-2091, USA.

Advanced Drug Delivery Reviews
|April 20, 2004
PubMed

Insights

Targeting the cell-membrane folate receptor with radiolabeled agents shows promise for tumor imaging. While clinical efficacy is pending, external radionuclide imaging can assess folate receptor levels noninvasively.

Area of Science:

  • Oncology
  • Radiochemistry
  • Molecular Imaging

Background:

  • The cell-membrane folate receptor is a validated molecular target for cancer therapy and diagnostics.
  • Radiolabeled folate-chelate conjugates offer a strategy for tumor-selective drug delivery and imaging.

Purpose of the Study:

  • To review the current literature on tumor imaging using radionuclide agents targeting the folate receptor.
  • To assess the feasibility and potential of folate receptor-targeted radionuclide imaging for diagnostic purposes.

Main Methods:

  • Survey of published studies on folate receptor-targeted radionuclide imaging.
  • In vitro and in vivo investigations of various radionuclides (67Ga, 111In, 99mTc, 66Ga, 64Cu) conjugated to folate-based targeting agents.

Main Results:

  • Successful in vitro and in vivo targeting of folate receptors has been demonstrated with multiple radionuclides suitable for clinical imaging.
  • Various radiolabeled folate analogs have shown effective tumor targeting in preclinical studies.
  • Qualitative assessment of tissue folate receptor levels via external radionuclide imaging is feasible.

Conclusions:

  • Folate receptor-targeted radionuclide imaging is a promising approach for noninvasive tumor detection and characterization.
  • Further clinical studies are needed to establish the diagnostic efficacy of these agents.
  • Radiolabeled folate conjugates represent a viable platform for developing novel cancer diagnostic tools.

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