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[64Cu]Cu-CryptTM – A novel cryptate for copper-64?

Foerster, Christian, Knight, James C., Wuest, Melinda, Rowan, Brendan, Lapi, Suzanne E., Amoroso, Angelo James ORCID:, Edwards, Peter G. and Wuest, Frank 2014. [64Cu]Cu-CryptTM – A novel cryptate for copper-64? Nuclear Medicine and Biology 41 (7) , p. 633. 10.1016/j.nucmedbio.2014.05.127

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Methods: Stability of [64Cu]Cu-CryptTM was assessed in vitro by challenging experiments using competitive chelators EDTA and NOTA. Radiopharmacological profile of [64Cu]Cu-CryptTM was evaluated by dynamic PET studies in EMT6-tumor bearing Balb/C mice. The current “gold standard” for kinetically inert 64Cu-cryptates [64Cu]Cu-DiAmSar was prepared and used as internal reference for in vitro and in vivo studies. Results: Radiochemical yields of > 95% were achieved by mixing CryptTM (0.25 nmol/μL) and [64Cu]Cu(OAc)2 (4.1 ± 0.5 MBq/μL) for 60 min at 37 °C. EDTA and NOTA clearly demonstrated kinetically- and thermodynamically-driven trans-chelation. Dynamic PET studies showed fast blood clearance for [64Cu]Cu-CryptTM and [64Cu]Cu-DiAmSar. [64Cu]Cu-CryptTM was predominantly eliminated hepatobiliary. Uptake of [64Cu]Cu-CryptTM in EMT6 tumors resulted in an SUV 0.40 ± 0.03 which was higher compared to muscle (SUV 0.16 ± 0.02 (n = 3) 60 min p.i.). Conclusion: Radiopharmacological evaluation of [64Cu]Cu-CryptTM revealed insufficient kinetic stability for in vivo applications. However, the facile synthetic access and its favorable 64Cu-labeling properties warrant further investigation of related derivatives possessing a tri-pyridyl/tri-amine donor group set to allow the formation of more kinetically inert 64Cu-cryptates.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Publisher: Elsevier
ISSN: 0969-8051
Last Modified: 01 Nov 2022 10:02

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