Human Dose Assessment of 68Ga-NODAGA-RGD-BBN Heterodimer Peptide based on Animal Data.

Abstract

Calculation of the absorbed dose in human organs is one of the first steps for developing new radiopharmaceuticals. The aim of this study is to estimate the human absorbed dose of a newly developed 68Ga-NODAGA-RGD-BBN radiolabeled compound. 68Ga-NODAGA-RGD-BBN was prepared by varying different parameters at optimized conditions. The stability of the radiolabeled peptide in phosphate-buffered saline (PBS) and in human serum was evaluated for 120 min. Afterward, the biodistribution of the complex was assessed in normal and tumor-bearing mice, at least for 120 min postinjection. Finally, the human absorbed dose of 68Ga-NODAGA-RGD-BBN was estimated based on mice data using Radiation Dose Assessment Resource and Spark method. 68Ga-NODAGA-RGD-BBN was produced with radiochemical purity of more than 98% (high-performance liquid chromatography/ radio thin layer chromatography (RTLC)) with high stability in PBS buffer and in human serum at least for 2 h. The complex demonstrated high uptake in gastrin-releasing peptide receptor-expressing tumors compared to other nontarget organs. Furthermore, the dose assessment for the complex showed that the kidneys receive the highest absorbed dose in comparison with other organs. The result of this study showed that 68Ga-NODAGA-RGD-BBN is an effective and radiolabeled ligand for tumor detection, however more studies are still needed.