RT Journal Article SR Electronic T1 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 JF Journal of Nuclear Medicine JO J Nucl Med FD Society of Nuclear Medicine SP 740 OP 743 DO 10.2967/jnumed.123.267175 VO 65 IS 5 A1 Hofman, Michael S. A1 Tran, Ben A1 Feldman, Darren R. A1 Pokorska-Bocci, Anna A1 Pichereau, Solen A1 Wessen, Jonathan A1 Haskali, Mohammad B. A1 Sparks, Richard B. A1 Vlasyuk, Olena A1 Galetic, Ivana YR 2024 UL http://jnm.snmjournals.org/content/65/5/740.abstract AB [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 administration ranged from 6.8 to 211.6 (mean, 64.6 [SD, 54.8]). The kidneys, liver, and bone marrow demonstrated low activity. [68Ga]Ga-DPI-4452 was rapidly eliminated from blood and urine. No clinically significant toxicity was observed. Conclusion: [68Ga]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.