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Abstract：
The prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPR) are overexpressed in prostate cancer (PCa). In preclinical studies, the iPSMA-Lys3-Bombesin (iPSMA-BN) heterodimeric ligand has shown a suitable affinity for PSMA and GRPR. This research aimed to assess the biokinetics and radiation dosimetry of [68Ga]Ga-iPSMA-BN in four healthy volunteers based on biodistribution data obtained from whole-body PET/CT studies, as well as to visualize the [68Ga]Ga-iPSMA-BN tumor uptake in a patient with PCa.
PET/CT images acquired at 5 min, 0.5, 1, and 2 h after radiotracer administration (124.5 ± 2.1 MBq) were corrected for attenuation, scattering, dead-time, and decay. The activity in the segmented volumes of interest (VOIs) in each source organ at different times was adjusted to mono- and bi-exponential biokinetic models (A(t)VOI), from which the total disintegrations (N) were calculated to assess the internal radiation doses by using the OLINDA V1.1 code.
Images from the patient showed an evident uptake by the metastasis (SUVmax of 4.7) and by the organs expressing GRPR (pancreas) and PSMA (salivary glands). The average effective dose was 2.70 ± 0.05 mSv, which was like those known for most of the 68Ga studies, making [68Ga]Ga-iPSMA-BN a promising dual-target PET imaging radiotracer for PCa.
[68Ga]Ga-iPSMA-BN, capable of detecting both PSMA and GRPR with suitable biokinetics and dosimetric patterns, could be a potential complementary diagnostic tool for the improvement of prostate cancer PET imaging.
PET/CT images acquired at 5 min, 0.5, 1, and 2 h after radiotracer administration (124.5 ± 2.1 MBq) were corrected for attenuation, scattering, dead-time, and decay. The activity in the segmented volumes of interest (VOIs) in each source organ at different times was adjusted to mono- and bi-exponential biokinetic models (A(t)VOI), from which the total disintegrations (N) were calculated to assess the internal radiation doses by using the OLINDA V1.1 code.
Images from the patient showed an evident uptake by the metastasis (SUVmax of 4.7) and by the organs expressing GRPR (pancreas) and PSMA (salivary glands). The average effective dose was 2.70 ± 0.05 mSv, which was like those known for most of the 68Ga studies, making [68Ga]Ga-iPSMA-BN a promising dual-target PET imaging radiotracer for PCa.
[68Ga]Ga-iPSMA-BN, capable of detecting both PSMA and GRPR with suitable biokinetics and dosimetric patterns, could be a potential complementary diagnostic tool for the improvement of prostate cancer PET imaging.
摘要：
前列腺特异性膜抗原（PSMA）和胃泌素释放肽受体（GRPR）在前列腺癌（PCa）中过表达。在临床前研究中,iPSMA-Lys3-Bombesin(iPSMA-BN)异二聚配体已显示出对PSMA和GRPR的合适亲和力。这项研究旨在根据从全身PET/CT研究中获得的生物分布数据，评估四名健康志愿者中[68Ga]Ga-iPSMA-BN的生物动力学和辐射剂量学，以及可视化PCa患者的[68Ga]Ga-iPSMA-BN肿瘤摄取。
在5分钟时采集的PET/CT图像，放射性示踪剂给药后0.5、1和2小时（124.5±2.1MBq）进行衰减校正，散射,死时间,和衰变。将每个源器官在不同时间的分段感兴趣体积（VOI）中的活动调整为单指数和双指数生物动力学模型（A（t）VOI），通过使用OLINDAV1.1代码计算总崩解量（N）以评估内部辐射剂量。
来自患者的图像显示通过转移(SUVmax为4.7)和通过表达GRPR(胰腺)和PSMA(唾液腺)的器官的明显摄取。平均有效剂量为2.70±0.05mSv，就像大多数68Ga研究中已知的那样，使[68Ga]Ga-iPSMA-BN成为PCa的有前途的双目标PET成像放射性示踪剂。
[68Ga]Ga-iPSMA-BN,能够以合适的生物动力学和剂量模式检测PSMA和GRPR，可能是改善前列腺癌PET成像的潜在补充诊断工具。
在5分钟时采集的PET/CT图像，放射性示踪剂给药后0.5、1和2小时（124.5±2.1MBq）进行衰减校正，散射,死时间,和衰变。将每个源器官在不同时间的分段感兴趣体积（VOI）中的活动调整为单指数和双指数生物动力学模型（A（t）VOI），通过使用OLINDAV1.1代码计算总崩解量（N）以评估内部辐射剂量。
来自患者的图像显示通过转移(SUVmax为4.7)和通过表达GRPR(胰腺)和PSMA(唾液腺)的器官的明显摄取。平均有效剂量为2.70±0.05mSv，就像大多数68Ga研究中已知的那样，使[68Ga]Ga-iPSMA-BN成为PCa的有前途的双目标PET成像放射性示踪剂。
[68Ga]Ga-iPSMA-BN,能够以合适的生物动力学和剂量模式检测PSMA和GRPR，可能是改善前列腺癌PET成像的潜在补充诊断工具。
