Journal article

First-in-Human Safety, Imaging, and Dosimetry of a Carbonic Anhydrase IX - Targeting Peptide, [ 68 Ga]Ga-DPI-4452, in Patients with Clear Cell Renal Cell Carcinoma

Michael S Hofman, Ben Tran, Darren R Feldman, Anna Pokorska-Bocci, Solen Pichereau, Jonathan Wessen, Mohammad B Haskali, Richard B Sparks, Olena Vlasyuk, Ivana Galetic

Journal of Nuclear Medicine | Society of Nuclear Medicine and Molecular Imaging | Published : 2024

Open access

Abstract

[68Ga]Ga-DPI-4452, a first-in-class carbonic anhydrase IX–binding radiolabeled peptide, is the imaging agent of a theranostic pair with [177Lu]Lu-DPI-4452, developed for selecting and treating patients with carbonic anhydrase IX–expressing tumors. Here, [68Ga]Ga-DPI-4452 imaging characteristics, dosimetry, pharmacokinetics, and safety were assessed in 3 patients with clear cell renal cell carcinoma. Methods: After [68Ga]Ga-DPI-4452 administration, patients underwent serial full-body PET/CT imaging. Blood and urine were sampled. Safety was monitored for 7 d after injection. Results: Tumor uptake was observed at all time points (15 min to 4 h). Across 36 lesions, the SUVmax at 1 h after admini..

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Grants

Funding Acknowledgements

We thank the patients and their families/carers for participating inthis study, and we acknowledge Peter Mac coinvestigators Brittany Emmerson, Associate Prof. Grace Kong, and Dr. Sidney Levy and the nuclear medicine, medical oncology, and clinical trials teams. Editorial assistance was provided by Can-cer Communications & Consultancy Ltd., funded by Debiopharm.