Preparation and biological studies of 125I-DOTA-TATE

DOTA-TATE, a somatostatin analog was radiolabeled with 125I in good yields and high radiochemical purity. The product exhibited good stability in vitro. Pharmacokinetic studies in normal Swiss mice showed rapid blood clearance with low thyroid uptake. Biodistribution studies in murine melanoma showed 3.0±1.3% ID/g uptake in tumor at 3 h post injection (p.i.), with negligible reduction at 24 h p.i. Inhibition studies carried out in vivo using cold DOTA-TATE confirmed the tumor specificity of the product.