A phase one, single-dose, open-label, clinical safety and PET/MR imaging study of Ga-DOTATOC in healthy volunteers.

This prospective pilot study provides a dynamic whole body PET/MR image database, clinical safety, biodistribution profile and dosimetry of Ga-DOTATOC in healthy subjects, to establish a baseline and standard reference for its use in diagnosis and treatment response evaluation among patients with somatostatin receptor expressing neoplastic diseases. Dynamic whole body PET/MR imaging was performed in 12 healthy subjects (male/female: 8/4) after injection of 242.39 ± 53.

Phase-1 clinical trial results of high-specific-activity carrier-free 123I-iobenguane.

Unlabelled: A first-in-human phase 1 clinical study was performed on 12 healthy adults with a high-specific-activity carrier-free formulation of (123)I-iobenguane. Clinical data are presented on the behavior of this receptor-targeting imaging agent.

Methods: Whole-body and thoracic planar and SPECT imaging were performed over 48 h for calculation of tissue radiation dosimetry and for evaluation of clinical safety and efficacy.

Comparison of high-specific-activity ultratrace 123/131I-MIBG and carrier-added 123/131I-MIBG on efficacy, pharmacokinetics, and tissue distribution.

Metaiodobenzylguanidine (MIBG) is an enzymatically stable synthetic analog of norepinephrine that when radiolabled with diagnostic ((123)I) or therapeutic ((131)I) isotopes has been shown to concentrate highly in sympathetically innervated tissues such as the heart and neuroendocrine tumors that possesses high levels of norepinephrine transporter (NET). As the transport of MIBG by NET is a saturable event, the specific activity of the preparation may have dramatic effects on both the efficacy and safety of the radiodiagnostic/radiotherapeutic. Using a solid labeling approach (Ultratrace), noncarrier-added radiolabeled MIBG can be efficiently produced.

Preclinical evaluation of an 131I-labeled benzamide for targeted radiotherapy of metastatic melanoma.

Radiolabeled benzamides are attractive candidates for targeted radiotherapy of metastatic melanoma as they bind melanin and exhibit high tumor uptake and retention. One such benzamide, N-(2-diethylamino-ethyl)-4-(4-fluoro-benzamido)-5-iodo-2-methoxy-benzamide (MIP-1145), was evaluated for its ability to distinguish melanin-expressing from amelanotic human melanoma cells, and to specifically localize to melanin-containing tumor xenografts. The binding of [(131)I]MIP-1145 to melanoma cells in vitro was melanin dependent, increased over time, and insensitive to mild acid treatment, indicating that it was retained within cells.

Synthesis and biodistribution of a Lipophilic 64Cu-labeled monocationic Copper(II) complex.

The lipophilic, monocationic copper(II) complex of the diiminedioxime ligand 2,10-di-n-butyl-3,9-dimethyl-1,4,8,11-tetraazaundeca-1,3,8,10-tetraen-1,11-dione dioxime was synthesized and labeled with 64Cu. The biological properties of the 64Cu-labeled complex were measured in vivo and in vitro. In vivo, the complex shows uptake by the heart similar to that of 99mTc-tetrofosmin.