Koizumi M, Endo K, Watanabe Y, Saga T, Sakahara H, Konishi J, Arano Y, Miyachi Y, Kashihara-Sawami M, Imamura S
Department of Nuclear Medicine, Kyoto University.
Jpn J Cancer Res. 1988 Aug;79(8):973-81. doi: 10.1111/j.1349-7006.1988.tb00063.x.
Immunoscintigraphic and pharmacokinetic characteristics of 111In-labeled ZME-018 monoclonal antibody were examined in 8 patients with malignant melanoma. Each patient received a single intravenous infusion of 20 mg of ZME-018, coupled to 3 mCi of 111In without any acute toxicity. Scintigrams were taken 1, 3, and 6 days after the administration, and blood and urine samples were also taken frequently. Rapid clearance of some radioactivity was seen in early urine samples in the form of 111In DTPA, but after 1 day, urinary excretion of radioactivity was slow and steady, with an average of 2.5% of the injected dose excreted per day. The scans demonstrated that there was blood retention of radioactivity in the heart and great vessels 1 day after infusion and considerable clearance from the blood pool occurred by 3 days. However, 111In was deposited in the liver, spleen and bone for up to 6 days. The optimal time for imaging appeared to be at 3 days. Nineteen out of 26 known lesions or 6 out of 8 patients were positive. There were 21 lesions detected that were not suspected during the work-up the patient. Five patients developed human anti-mouse antibody in the serum by 3 weeks. These results suggest that immunoscintigraphy with 111In-labeled ZME-018 antibody is safe and useful for the detection of metastatic lesions in a selected group of patients with malignant melanoma.
对8例恶性黑色素瘤患者研究了¹¹¹铟标记的ZME - 018单克隆抗体的免疫闪烁显像和药代动力学特征。每位患者单次静脉输注20mg与3mCi¹¹¹铟偶联的ZME - 018，未出现任何急性毒性。给药后1天、3天和6天进行闪烁显像，同时频繁采集血样和尿样。早期尿样中可见部分放射性以¹¹¹铟 - 二乙三胺五乙酸（¹¹¹In DTPA）形式快速清除，但1天后，放射性的尿排泄缓慢且稳定，平均每天排泄量为注射剂量的2.5%。扫描显示，输注后1天心脏和大血管中有放射性血潴留，3天时血池中有大量放射性清除。然而，¹¹¹铟在肝脏、脾脏和骨骼中沉积长达6天。最佳显像时间似乎为3天。26个已知病灶中有19个或8例患者中有6例呈阳性。发现了21个在患者检查期间未被怀疑的病灶。3周时5例患者血清中出现人抗鼠抗体。这些结果表明，¹¹¹铟标记的ZME - 018抗体免疫闪烁显像对特定组的恶性黑色素瘤患者转移病灶的检测是安全且有用的。
