利卡汀的人体显像和组织分布

IC

李云春 谭天秩 莫廷树 卢武胜 邓候富 杨晓川 www.tws.org.cn/qikan/Cpaper/zhaiyao.asp?bsid=5264 www.tws.org.cn/qikan/manage/wenzhang/2006-043.pdf 四川大学华西医院核医学科 成都 四川大学华西医院核医学科 成都 四川大学华西医院核医学科 成都 四川大学华西医院普外科 成都 四川大学华西医院核医学科 成都 四川大学华西医院核医学科 成都   收稿日期 2006-7-12 修回日期 网络版发布日期: 2007-8-14 摘要   摘要：研究我国具有自主知识产权的国家一类新药—碘[131I]-肝癌单抗片段HAb18 F(ab’)2注射液的人体显像和组织分布特征。拟定纳入标准、排除标准和剔除标准，严格按标准选择患原发性肝细胞肝癌的受试者24例，平均分为3组，分别为低剂量组（注入量18.5 MBq/ kg人体）、中剂量组（注入量27.75 MBq/ kg人体）和高剂量组（注入量37 MBq/ kg人体），每组8例。再采用溴代琥珀酰亚胺法标记制备碘[131I]-肝癌单抗片段 HAb18 F(ab’)2注射液后，各组每位受试者经插至肝固有动脉或肿瘤的供血肝动脉的导管注入相应的碘[131I]-肝癌单抗片段HAb18 F(ab’)2注射液，并在给药后不同时刻进行全身显像，用感性趣区技术测定受试者组织的放射性计数率，计算受试者组织的放射性药物摄取率及肝肿瘤组织/非瘤组织（T/NT）比值，以观察药物在各组织及肿瘤内分布的动态变化。研究显示：碘[131I]-肝癌单抗片段HAb18 F(ab’)2在肝癌组织中有明显的摄取，早期主要浓聚于肝癌组织及肝组织中，体内其他组织的浓聚甚少；随着时间的延长，肝癌组织的放射性浓聚相对于肝组织持续增强，而肝组织的放射性逐渐减少；在显像期间（8 d），除肝外的其他正常组织的T/NT值为1.04～3.79，而肝脏的T/NT值随时间推延而增加，至d8时为1.09。因此，碘[131I]-肝癌单抗片段 HAb18 F(ab’)2注射液能特异性结合肝癌组织。 关键词   单克隆抗体片段   原发性肝癌   碘[131I]   显像   组织分布   人体   分类号 Imaging and Biodistribution of Licartin In Human Body   Abstract  Imaging and Biodistribution of Injection of Iodine-131 Labeled Hepatoma Monoclonal Antibody HAb18 F(ab’)2 for Radioimmunotherapy in Human Body LI Yun-chun1, TAN Tian-zhi1, MO Ting-shu1, LU Wu-sheng2, DENG Hou-fu1, YANG Xiao-chuan1, LI Xiao2 (1.Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu 610041,China; 2. Department of Surgery , West China Hospital, Sichuan University, Chengdu 610041,China) Abstract: Imaging and biodistribution of injection of iodine-131 labeled hepatoma monoclonal antibody HAb18 F(ab’)2 for radioimmunotherapy were assessed in vivo . Inclusion criteria, exclusion criteria and withdrawal criteria were drafted. 24 of cases with primary hepatocelluar carcinoma (PHC), strictly selected according to these criteria, were equally divided into three groups (8 of cases per group ). Every group was low dose group (administration dosage is 18.5 MBq/ kg human body ), middle dose group (administration dosage is 27.75 MBq/ kg human body ), high dose group (administration dosage is 37 MBq/ kg human body ), respectively. After relevant injection of Iodine-131 labeled hepatoma monoclonal antibody HAb18 F(ab’)2 for radioimmunotherapy, prepared using N-bromosuccinimide (NBS) labeling method, was administrated into the hepatic artery of every case. Every case was carried out whole body imaging at different time after administrating drug. The uptake of every tissue and the ratios of tumor tissue and non-tumor tissue (T/NT) were calculated using region of interest technique in order to observe the dynamic change of drug distribution in every tissue or tumor. The study of biodistribution showed that Iodine-131 labeled hepatoma monoclonal antibody HAb18 F(ab’)2 mainly accumulated in liver cancer and liver tissue and a small amount of that accumulated in other tissue at early stage, the radioactive concentration continuously increased in liver cancer and the uptake of radioactivity gradually decreased in liver with the extension of time. During the imaging time period ( 8 d ), T/NT ratios of other normal tissue besides liver were 1.04 -3.79, but T/NT ratios of liver gradually increased as the time increased and were 1.09 at d 8. PHC could specifically combine with Iodine-131 labeled hepatoma monoclonal antibody HAb18 F(ab’)2.   Key words   Monoclonal Antibody Fraction   Primary Hepatocelluar Carcinoma   Iodine-131   Imaging   Biodistribution   Human Body   DOI

通讯作者 李云春 [email protected]