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

Author:

Patra Sourav12,Jadhav Sachin1,Shetty Priyalata12,Singh Khajan1,Rajeswari Ardhi1,Vimalnath K. V.1,Chakraborty Avik23,Chakravarty Rubel12,Chakraborty Sudipta12ORCID

Affiliation:

1. Radiopharmaceuticals Division , Bhabha Atomic Research Centre , Trombay , Mumbai 400085 , India

2. Homi Bhabha National Institute , Anushaktinagar , Mumbai 400094 , India

3. Radiation Medicine Centre , Bhabha Atomic Research Centre , Trombay , Mumbai 400085 , India

Abstract

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.

Funder

Bhabha Atomic Research Centre

Publisher

Walter de Gruyter GmbH

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