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
- Author(s)
- Hofman, MS; Tran, B; Feldman, DR; Pokorska-Bocci, A; Pichereau, S; Wessen, J; Haskali, MB; Sparks, RB; Vlasyuk, O; Galetic, I;
- Journal Title
- Journal of Nuclear Medicine
- Publication Type
- Online publication before print
- Abstract
- [(68)Ga]Ga-DPI-4452, a first-in-class carbonic anhydrase IX-binding radiolabeled peptide, is the imaging agent of a theranostic pair with [(177)Lu]Lu-DPI-4452, developed for selecting and treating patients with carbonic anhydrase IX-expressing tumors. Here, [(68)Ga]Ga-DPI-4452 imaging characteristics, dosimetry, pharmacokinetics, and safety were assessed in 3 patients with clear cell renal cell carcinoma. Methods: After [(68)Ga]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 SUV(max) at 1 h after administration ranged from 6.8 to 211.6 (mean, 64.6 [SD, 54.8]). The kidneys, liver, and bone marrow demonstrated low activity. [(68)Ga]Ga-DPI-4452 was rapidly eliminated from blood and urine. No clinically significant toxicity was observed. Conclusion: [(68)Ga]Ga-DPI-4452 showed exceptional tumor uptake in patients with clear cell renal cell carcinoma, with very high tumor-to-background ratios and no significant adverse events, suggesting potential diagnostic and patient selection applications.
- Keywords
- Pet/ct; [68Ga]Ga-DPI-4452; clear cell renal cell carcinoma; theranostic
- Department(s)
- Cancer Imaging; Medical Oncology
- Publisher's Version
- https://doi.org/10.2967/jnumed.123.267175
- Open Access at Publisher's Site
https://doi.org/10.2967/jnumed.123.267175- Terms of Use/Rights Notice
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Creation Date: 2024-04-02 04:06:04
Last Modified: 2024-04-02 04:14:45