Liver Cancer
Copyright ©The Author(s) 2002. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Feb 15, 2002; 8(1): 69-73
Published online Feb 15, 2002. doi: 10.3748/wjg.v8.i1.69
Pharmacokinetics of radioimmunotherapeutic agent of direct labeling mAb 188Re-HAb18
Chao Lou, Zhi-Nan Chen, Hui-Jie Bian, Jie Li, Shou-Bo Zhou
Chao Lou, Zhi-Nan Chen, Hui-Jie Bian, Jie Li, Department of Cell Engineering Research Centre, Department of Oral Cell Biology, Qingdu Hospital, Fourth Military Medical University, Xi’an 710033, Shaanxi Province, China
Shou-Bo Zhou, School of Biological Science, University of Manchester, Oxford Road, United Kingdom
Author contributions: All authors contributed equally to the work.
Supported by National Natural Science Foundation of China, No. 39700175(Dr.Hui-Jie Bian)
Correspondence to: Chao Lou, Cell Engineering Research Centre, Fourth Military Medical University, Xi’an 710033,Shaanxi Province, China.
Telephone: +86-29-3374057
Received: July 19, 2001
Revised: September 9, 2001
Accepted: October 24, 2001
Published online: February 15, 2002

AIM: To label anti-hepatoma monoclonal antibody (mAb) fragment HAb18 F(ab’)2 was labeled with 188Re for the pharmacokinetic model of 188Re-HAb18 F(ab’)2 and to evaluate its pharmacokinetic parameters in hepatoma-bearing nude mice.

METHODS: HAb18 F(ab’)2 was directly labeled with 188Re using 2-mercaptoethanol (2-ME) as reducing agents. Labeling efficiency and immunoreactivity of 188Re-HAb18 F(ab’)2 were evaluated by Whatman 3MM paper chromatography and live cell assay, respectively. Biodistribution analysis was also conducted in nude mice bearing human hepatoma in which animals were sacrificed at different time points (1, 4, 18, 24 and 24 h) after 188Re-HAb18 F (ab’)2 was injected through tail-vein into hepatoma-bearing nude mice. The blood and radioactivity of organs and mass were measured. The concentrations of 188Re-HAb18 F(ab’)2 were evaluated with apharmacokinetic 3P97 software.

RESULTS: The optimum labeling efficiency and immunoreactive fraction were 91.7% and 0.78% respectively. The parameters of 188Re-HAb18 F(ab’)2 were: T1/2, 2.29 h; Vd,1.49 × 10-9 L·Bq-1; AUC, 20. 49 × 109 Bq·h·L-1;CL, 0.45 × 10-3 L·h-1. 188Re-HAb18 F(ab’)2 could locate specially in hepatoma with high selective reactivity of HAb18 F(ab’)2. 188Re-HAb18 F(ab’)2 was mainly eliminated by kidney. The maximal tumor to blood ratio was at 48 h, and maximal tumor to liver ratio was at 18 h.

CONCLUTION: The pharmacokinetics of 188Re-HAb18 F (ab’)2 fital-compartment model.188Re-HAb18 F(ab’)2 can be uptaken selectively at the hepatoma site.

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