作者
Zhi‐Nan Chen,Mi Li,Jing Xu,Fei Song,Qing Zhang,Zhaohui Zheng,Jinliang Xing,Huijie Bian,Jian‐Li Jiang,Xianhui Wang,Peng Shang,Airong Qian,Sihe Zhang,Ling Li,Yu Li,Qiang Feng,Xiaoling Yu,Yong Feng,Xiang-Min Yang,Rong Tian,Zhenbiao Wu,Nan Li,Tingshu Mo,Anren Kuang,Tianwei Tan,Yun‐Chun Li,Daoming Liang,Wusheng Lu,Jia Miao,Guohui Xu,Zhihui Zhang,Nan Kang,Jieun Han,Qingguang Liu,Hongxin Zhang,Ping Zhu
摘要
HAb18G/CD147 is a hepatocellular carcinoma (HCC)-associated antigen. We developed iodine (131I) metuximab injection (Licartin), a novel 131I-labeled HAb18G/CD147-specific monoclonal antibody Fab'2 fragment, and evaluated its safety, pharmacokinetics, and clinical efficacy on HCC in Phase I/II trials.In a Phase I trial, 28 patients were randomly assigned to receive the injection in 9.25-, 18.5-, 27.75-, or 37-MBq/kg doses by hepatic artery infusion. In a multicenter Phase II trial, 106 patients received the injection (27.75 MBq/kg) on Day 1 of a 28-day cycle. Response rate and survival rate were the endpoints.No life-threatening toxic effects were found. The safe dosage was 27.75 MBq/kg. The blood clearance fitted a biphasic model, and its half-life was 90.56-63.93 h. In the Phase II trial, the injection was found to be targeted and concentrated to tumor tissues. Of the 73 patients completing two cycles, 6 (8.22%) had a partial response, 14 (19.18%) minor response, and 43 (58.90%) stable disease. The 21-month survival rate was 44.54%. The survival rate of progression-free patients was significantly higher than that of patients with progressive disease after either one or two cycles (p < 0.0001 or p = 0.0019).Iodine (131I) metuximab injection is safe and active for HCC patients.