Folate-receptor-targeted radionuclide imaging agents

Chun Yen Ke, Carla J. Mathias, Mark A. Green

Research output: Contribution to journalArticle

110 Scopus citations


The cell-membrane folate receptor is a potential molecular target for tumor-selective drug delivery, including delivery of radiolabeled folate-chelate conjugates for diagnostic imaging. This review surveys the growing literature on tumor imaging with radionuclide agents targeted to the folate receptor. Successful folate-receptor targeting has been reported, both in vitro and in vivo, using a variety of radionuclides that are suitable for clinical diagnostic imaging (67Ga, 111In, 99mTc, 66Ga, and 64Cu). While none of these agents has, to date, been demonstrated to have clinical efficacy as a diagnostic tool, existing data indicates that it is feasible to noninvasively assess (at least qualitatively) tissue folate receptor levels by external radionuclide imaging.

Original languageEnglish (US)
Pages (from-to)1143-1160
Number of pages18
JournalAdvanced Drug Delivery Reviews
Issue number8
StatePublished - Apr 29 2004
Externally publishedYes


  • Diagnostic imaging
  • Folate receptor
  • Nuclear medicine
  • Radiopharmaceutical

ASJC Scopus subject areas

  • Pharmaceutical Science

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