Abstract：
BACKGROUND: Prostate-specific membrane antigen (PSMA)-targeted radiopharmaceuticals allow whole-body imaging to detect prostate cancer (PC). Positron emission tomography imaging using gallium-68 (68Ga)-PSMA-11 has been shown to have a favorable safety and tolerability profile and high diagnostic performance. The study evaluates the safety and pharmacokinetics of 68Ga-PSMA-11 in Japanese patients with primary, recurrent, or suspected recurrent prostate cancer.
METHODS: This single arm study enrolled Japanese patients with primary PC (n = 3), suspected recurrent PC following radical prostatectomy (n = 4), or suspected recurrent PC following radical radiotherapy (n = 3). All patients received a single intravenous dose of 68Ga-PSMA-11 2.0 MBq/kg (±10%) followed by PSMA PET imaging and safety and pharmacokinetic evaluations. Based on the blood concentrations of 68Ga-PSMA-11 and the radioactivity distribution rate in each organ/tissue, the absorbed doses in major organs/tissues and the whole-body effective dose were calculated by the Medical Internal Radiation Dose method.
RESULTS: Ten patients were enrolled. Mean age was 73.3 ± 4.8 years, and median prostate-specific antigen was 8.250 ng/mL. Five patients (50%) experienced a total of 6 adverse events, and no grade ≥ 2 adverse events or serious adverse events were reported. No clinically significant changes in vital signs, haematology parameters, or blood chemistry or ECG abnormalities were observed. The estimated whole body effective dose of 68Ga-PSMA-11 (mean ± standard deviation) was 2.524 × 10-2 ± 2.546 × 10-3 mSv/MBq. Time to maximum concentration (1.16 × 10-4 ± 1.3 × 10-5% ID/mL) in whole blood was 2.15 ± 0.33 min.
CONCLUSIONS: 68Ga-PSMA-11 has a favourable safety and tolerability profile in Japanese patients with primary, recurrent, or suspected recurrent prostate cancer, which is comparable to previous observations in other populations.
METHODS: This single arm study enrolled Japanese patients with primary PC (n = 3), suspected recurrent PC following radical prostatectomy (n = 4), or suspected recurrent PC following radical radiotherapy (n = 3). All patients received a single intravenous dose of 68Ga-PSMA-11 2.0 MBq/kg (±10%) followed by PSMA PET imaging and safety and pharmacokinetic evaluations. Based on the blood concentrations of 68Ga-PSMA-11 and the radioactivity distribution rate in each organ/tissue, the absorbed doses in major organs/tissues and the whole-body effective dose were calculated by the Medical Internal Radiation Dose method.
RESULTS: Ten patients were enrolled. Mean age was 73.3 ± 4.8 years, and median prostate-specific antigen was 8.250 ng/mL. Five patients (50%) experienced a total of 6 adverse events, and no grade ≥ 2 adverse events or serious adverse events were reported. No clinically significant changes in vital signs, haematology parameters, or blood chemistry or ECG abnormalities were observed. The estimated whole body effective dose of 68Ga-PSMA-11 (mean ± standard deviation) was 2.524 × 10-2 ± 2.546 × 10-3 mSv/MBq. Time to maximum concentration (1.16 × 10-4 ± 1.3 × 10-5% ID/mL) in whole blood was 2.15 ± 0.33 min.
CONCLUSIONS: 68Ga-PSMA-11 has a favourable safety and tolerability profile in Japanese patients with primary, recurrent, or suspected recurrent prostate cancer, which is comparable to previous observations in other populations.
摘要：
背景：前列腺特异性膜抗原（PSMA）靶向的放射性药物允许全身成像以检测前列腺癌（PC）。使用镓-68（68Ga）-PSMA-11的正电子发射断层扫描成像已被证明具有良好的安全性和耐受性特征以及高诊断性能。该研究评估了68Ga-PSMA-11在日本原发性，经常性,或怀疑复发性前列腺癌。
方法：这项单臂研究招募了日本原发性PC患者（n=3），前列腺癌根治术后疑似复发性PC（n=4），或怀疑根治性放疗后PC复发（n=3）。所有患者均接受单次静脉内剂量的68Ga-PSMA-112.0MBq/kg（±10％），然后进行PSMAPET成像以及安全性和药代动力学评估。根据68Ga-PSMA-11的血液浓度和每个器官/组织中的放射性分布速率，主要器官/组织的吸收剂量和全身有效剂量通过医学内部辐射剂量法计算。
结果：纳入10例患者。平均年龄为73.3±4.8岁，前列腺特异性抗原中位数为8.250ng/mL.5名患者（50%）共经历了6次不良事件，未报告≥2级不良事件或严重不良事件.生命体征无临床意义变化,血液学参数，或观察到血液化学或心电图异常。68Ga-PSMA-11的估计全身有效剂量（平均值±标准偏差）为2.524×10-2±2.546×10-3mSv/MBq。达到全血中最大浓度（1.16×10-4±1.3×10-5％ID/mL）的时间为2.15±0.33分钟。
结论：68Ga-PSMA-11在日本患者中具有良好的安全性和耐受性，经常性,或者怀疑复发性前列腺癌，这与以前在其他人群中的观察结果相当。
方法：这项单臂研究招募了日本原发性PC患者（n=3），前列腺癌根治术后疑似复发性PC（n=4），或怀疑根治性放疗后PC复发（n=3）。所有患者均接受单次静脉内剂量的68Ga-PSMA-112.0MBq/kg（±10％），然后进行PSMAPET成像以及安全性和药代动力学评估。根据68Ga-PSMA-11的血液浓度和每个器官/组织中的放射性分布速率，主要器官/组织的吸收剂量和全身有效剂量通过医学内部辐射剂量法计算。
结果：纳入10例患者。平均年龄为73.3±4.8岁，前列腺特异性抗原中位数为8.250ng/mL.5名患者（50%）共经历了6次不良事件，未报告≥2级不良事件或严重不良事件.生命体征无临床意义变化,血液学参数，或观察到血液化学或心电图异常。68Ga-PSMA-11的估计全身有效剂量（平均值±标准偏差）为2.524×10-2±2.546×10-3mSv/MBq。达到全血中最大浓度（1.16×10-4±1.3×10-5％ID/mL）的时间为2.15±0.33分钟。
结论：68Ga-PSMA-11在日本患者中具有良好的安全性和耐受性，经常性,或者怀疑复发性前列腺癌，这与以前在其他人群中的观察结果相当。
