Folate-receptor-targeted radionuclide imaging agents

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.