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

Hofman, MS; Tran, B; Feldman, DR; Pokorska-Bocci, A; Pichereau, S; Wessen, J; Haskali, MB; Sparks, RB; Vlasyuk, O; Galetic, I

Author(s): Hofman, MS; Tran, B; Feldman, DR; Pokorska-Bocci, A; Pichereau, S; Wessen, J; Haskali, MB; Sparks, RB; Vlasyuk, O; Galetic, I;
Details: Publication Year 2024-02-22,Volume 65,Issue #5,Page 740-743
Journal Title: Journal of Nuclear Medicine
Publication Type: Research article
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.
Publisher: Society of Nuclear Medicine and Molecular Imaging
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: Refer to copyright notice on published article.

Creation Date: 2024-04-02 04:06:04

Last Modified: 2025-01-28 06:44:42