Evaluation of a flexible NOTA-RGD kit solution using Gallium-68 from different 68Ge/ 68Ga-generators: pharmacokinetics and biodistribution in nonhuman primates and demonstration of solitary pulmonary nodule imaging in humans
Date
2016Author
Ebenhan, Thomas
Schoeman, Isabel
Grobler, Anne
Zeevaart, Jan Rijn
Rossouw, Daniel D.
Metadata
Show full item recordAbstract
Purpose: Radiopharmaceuticals containing the motive tripeptide arginyl-glycyl-asparatic acid
(RGD) are known to target ανβ3 integrins during tumor angiogenesis. A more generic kit
radiolabeling procedure accommodating Ga-68 from different generators was developed for
NOTA-RGD and evaluated for its versatile use and safety in subsequent in vivo applications.
The [68Ga]NOTA-RGD kit was further verified for its expected biodistribution and pharmacokinetics
in nonhuman primates and its clinical sensitivity to detect solitary pulmonary nodules
(SPN) in cancer patients.
Procedures: Single vial kits containing 28–56 nmol of NOTA-cyclo-Arg-Gly-Asp-d-Tyr-Lys
(NOTA-RGD) and sodium acetate trihydrate buffer were formulated. Versatility of the NOTARGD
radiolabeling performance and adaption to a TiO2- and a SnO2-based generator type,
characterization and long-term storage stability of the kits were carried out. The blood clearance
and urine recovery kinetics as well as the image-guided biodistribution of [68Ga]NOTA-RGD was
studied in a vervet monkey model. [68Ga]NOTA-RGD kits were further tested clinically to target
solitary pulmonary nodules
URI
http://hdl.handle.net/10394/19207https://link.springer.com/article/10.1007%2Fs11307-016-1014-1
https://doi.org/10.1007/s11307-016-1014-1
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- Faculty of Health Sciences [2383]