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KMID : 1148920200540020114
Nuclear Medicine and Molecular Imaging
2020 Volume.54 No. 2 p.114 ~ p.119
First In-Human Medical Imaging with a PASylated 89Zr-Labeled Anti-HER2 Fab-Fragment in a Patient with Metastatic Breast Cancer
Richter Antonia

Knorr Karina
Schlapschy Martin
Robu Stephanie
Morath Volker
Mendler Claudia
Yen Hsi-Yu
Steiger Katja
Kiechle Marion
Weber Wolfgang
Skerra Arne
Schwaiger Markus
Abstract
Purpose: PASylation¢ç offers the ability to systematically tune and optimize the pharmacokinetics of protein tracers for molecular imaging. Here we report the first clinical translation of a PASylated Fab fragment (89Zr?Df-HER2-Fab-PAS200) for the molecular imaging of tumor-related HER2 expression.

Methods: A patient with HER2-positive metastatic breast cancer received 37 MBq of 89Zr?Df-HER2-Fab-PAS200 at a total mass dose of 70 ¥ìg. PET/CT was carried out 6, 24, and 45 h after injection, followed by image analysis of biodistribution, normal organ uptake, and lesion targeting.

Results: Images show a biodistribution typical for protein tracers, characterized by a prominent blood pool 6 h p.i., which decreased over time. Lesions were detectable as early as 24 h p.i. 89Zr?Df-HER2-Fab-PAS200 was tolerated well.

Conclusion: This study demonstrates that a PASylated Fab tracer shows appropriate blood clearance to allow sensitive visualization of small tumor lesions in a clinical setting.
KEYWORD
Breast cancer (BCa), Fab fragment, Human epidermal growth factor receptor 2 (HER2), Imaging, PASylation, 89Zr
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