TY - JOUR T1 - Pharmacokinetics and Metabolism of 5-<sup>125</sup>I-Iodo-4′-Thio-2′-Deoxyuridine in Rodents JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 1671 LP - 1676 VL - 44 IS - 10 AU - Jun Toyohara AU - Akie Gogami AU - Akio Hayashi AU - Yoshiharu Yonekura AU - Yasuhisa Fujibayashi Y1 - 2003/10/01 UR - http://jnm.snmjournals.org/content/44/10/1671.abstract N2 - Pharmacokinetics and metabolite analysis of radioiodinated 5-iodo-4′-thio-2′-deoxyuridine (ITdU), a potential tumor cell proliferation-imaging agent, were investigated in rodents. Methods: Blood and urine metabolites of radiolabeled ITdU were analyzed by thin-layer chromatography in rats. Tissue fractionation studies in mice were also performed to investigate the incorporation of 125I-ITdU into DNA. Results: The blood distribution study suggested the influx of 125I-ITdU into rat peripheral blood cells. The blood metabolism of 125I-ITdU in vitro was negligible. Plasma analysis at 60 min after injection showed that 50% of the radioactivity was intact 125I-ITdU. The plasma clearance of 125I-ITdU showed a biexponential function with half-lives of 0.2 and 29.5 min, representing 94.2% and 5.8% of plasma 125I-ITdU concentration, respectively. 125I-ITdU was excreted in urine 86% intact at 3.5 h after injection. Extraction of the tissues demonstrated that &gt;70% of the activity in the duodenum, spleen, and thymus was incorporated into DNA at 8 h after injection. On the other hand, &lt;8% of the activity in the liver was in the DNA fraction at that time. Conclusion: These data demonstrate that 125I-ITdU is less susceptible against catabolism and readily incorporated into DNA in proliferating tissues. Therefore, 125I-ITdU may be useful in measuring DNA synthesis with SPECT. ER -