[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 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. [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.

[ ⁶⁸ Ga]Ga-DPI-4452 是一种一流的碳酸酐酶 IX 结合放射性标记肽，是与 [ ¹⁷⁷ Lu]Lu-DPI-4452 的治疗诊断对的显像剂，开发用于选择和治疗患有以下疾病的患者：表达碳酸酐酶 IX 的肿瘤。在此，对 3 名透明细胞肾细胞癌患者的 [ ⁶⁸ Ga]Ga-DPI-4452 成像特征、剂量测定、药代动力学和安全性进行了评估。方法： [ ⁶⁸ Ga]Ga-DPI-4452 给药后，患者接受连续全身 PET/CT 成像。采集了血液和尿液样本。注射后监测7天的安全性。结果：在所有时间点（15 分钟至 4 小时）观察到肿瘤摄取。在 36 个病灶中，给药后 1 小时的 SUV_最大值范围为 6.8 至 211.6（平均值为 64.6 [SD，54.8]）。肾脏、肝脏和骨髓的活性较低。 [ ⁶⁸ Ga]Ga-DPI-4452 迅速从血液和尿液中消除。没有观察到临床上显着的毒性。结论： [ ⁶⁸ Ga]Ga-DPI-4452 在透明细胞肾细胞癌患者中显示出异常的肿瘤摄取，具有非常高的肿瘤与背景比率并且没有显着的不良事件，表明潜在的诊断和患者选择应用。