Preparation of [64Cu]Cu–NOTA complex as a potential renal PET imaging agent using 64Cu produced via the direct activation route

IF 1.4 3区化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR Radiochimica Acta Pub Date : 2024-02-13 DOI:10.1515/ract-2023-0206

Sourav Patra, Sachin Jadhav, Priyalata Shetty, Khajan Singh, Ardhi Rajeswari, K. V. Vimalnath, Avik Chakraborty, Rubel Chakravarty, Sudipta Chakraborty

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Abstract

Glomerular filtration rate (GFR) could be determined more accurately using renal positron emission tomography (PET) than conventional gamma imaging. Copper-64 [T ½ = 12.7 h, E β+ (max) = 653 keV, β+ branching ratio = 17.8 %, 1346 keV γ-photon (0.54 %), EC (43.8 %), β− emission (38.4 %)] in the form of its hydrophilic complex with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) is proposed as a potent formulation for renal PET imaging. A lyophilized kit was developed for formulation of ∼370 MBq dose of [64Cu]Cu–NOTA complex in a facile single step process using 64Cu produced by thermal neutron activation in a research reactor. The complex could be synthesized with >99 % yield and retained its integrity even when challenged by apoferritin. The rapid accumulation of [64Cu]Cu–NOTA in the kidney and clearance through urinary path was demonstrated using PET/CT imaging and ex vivo biodistribution study carried out in healthy Wistar rats to elucidate its effectiveness as a renal PET-imaging agent.

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使用通过直接活化途径生产的 64Cu 制备[64Cu]Cu-NOTA 复合物，作为一种潜在的肾脏 PET 成像剂

与传统的伽马成像相比，肾脏正电子发射断层扫描（PET）能更准确地测定肾小球滤过率（GFR）。铜-64 [T ½ = 12.7 h, E β+ (max) = 653 keV, β+ 支化率 = 17.8 %, 1346 keV γ-光子 (0.54 %), EC (43.8 %), β- 发射 (38.4 %)]以其与 1,4,7-三氮杂环壬烷-1,4,7-三乙酸（NOTA）的亲水复合物的形式被提出作为肾脏 PET 成像的有效制剂。利用在研究反应堆中通过热中子活化产生的 64Cu，开发了一种冻干试剂盒，用于配制 370 MBq 剂量的[64Cu]Cu-NOTA 复合物。该复合物的合成率高达 99%，即使在受到异铁蛋白的挑战时也能保持其完整性。在健康 Wistar 大鼠身上进行的 PET/CT 成像和体内外生物分布研究证明了 [64Cu]Cu-NOTA 在肾脏中的快速积累和通过尿路的清除，从而阐明了它作为肾脏 PET 成像剂的有效性。

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