Development of [Zn-62/Cu-62]-DOTA-rituximab as a possible novel in vivo PET generator for anti-CD20 antigen imaging

作者：Gholipour Nazila; Jalilian Amir R^*; Fazaeli Yousef; Sabzevari Omid; Moradkhani Sedigheh; Bolourinovin Fateme; Khalaj Ali

来源：Radiochimica Acta, 2014, 102(11): 1035-1045.

DOI：10.1515/ract-2013-2196

• Zn-62
• Production
• rituximab
• Biodistribution/co-incidence imaging

In this study, zinc-62 was prepared at radiopharmaceutical grade (for Zn-62/Cu-62 generator production) using Cu-nat(p, xn) reaction with the production yield of 5.9 mCi/mu Ah at 30 MeV proton energy (radiochemical separation yield %26gt;95%, radionuclidic purity %26gt;99% and radiochemical purity %26gt;99%). In the next step, rituximab was successively labeled with [Zn-62]-ZnCl2 after conjugation with p-SCN-Bz-DOTA followed by molecular filtration and determination of the average number of DOTA conjugated permAb (6:1) by spectrophotometric method. Radiochemical purity (%26gt;97%, measured by ITLC and HPLC), integrity of protein after radiolabeling (gel electrophoresis) and stability of [Zn-62]-DOTA-rituximab (in final formulation, and human serum) were determined 1-8 has well as biodistribution studies in wild-type rats followed by coincidence imaging for 6 h. However, the accumulation of the radiolabeled antibody was not consistent with the former reported rituximab conjugates. [Zn-62]-labeled monoclonal antibodies and fragments can be prepared as potential in vivo PET generators for molecular imaging however, the search for application of stable zinc complexes must be continued.

• 出版日期2014-11