Previous studies have demonstrated the
tumor-targeting potential of radioiodinated
5-iodo-2'-deoxyuridine (
IUdR) in experimental animal models following direct intratumoral or intracavitary administration. The aim of this study was to measure the
tumor uptake and metabolic fate of 5-[125I]iodo-2'-
deoxyuridine ([125I]UdR) in humans after a single intratumoral injection. Ten patients with
colorectal cancer were injected intratumorally with [125I]UdR) (0.24-3.9 MBq) during endoscopy 24 hr before ablative surgery. Blood and urine samples were collected up to 72 hr after [125I]UdR injection. Following resection, the radioactivity in the
tumor and the surrounding tissues was measured in a gamma counter, and microautoradiography was performed on semi-thin tissue sections to assess localization of the
radiopharmaceutical at the cellular level. An average of 0.234% of the injected dose was present per gram of
tumor (range 0.009-0.918, median value 0.147), and
tumor-to-nontumor radioactivity incorporation ratios were high for colonic mucosa when the nontumor tissue was taken at 1 cm (mean 629, range 27-2391) and 15 cm (mean 2387, range 122-12674) from the injection site. Microautoradiography confirmed these high
tumor-to-nontumor ratios and demonstrated localization of [125I]UdR in the
tumor cell nuclei. These results suggest that radioiodinated
IUdR might have potential as a
tumor-targeting agent in humans, provided homogeneous intratumoral distribution of the
radiopharmaceutical by a suitable route of loco-regional administration can be achieved.