Pharmacokinetics of ~(131)I-labeled-metuximab and transarterial chemoembolization for treatment of hepatocellular carcinoma
10.3760/cma.j.issn.1005-1201.2010.01.019
- VernacularTitle:~(131)I-美妥昔单抗联合动脉化疗栓塞治疗原发性肝癌的药代动力学研究
- Author:
Jun MA
;
Jianhua WANG
;
Rong LIU
;
Sheng QIAN
;
Yi CHEN
;
Hongcheng SHI
;
Yushen GU
- Publication Type:Journal Article
- Keywords:
Iodine radioisotopes;
Antibodies,monoclonal;
Carcinoma;
heptaocellular;
Antineoplastic protocols;
Pharmacokinetics
- From:
Chinese Journal of Radiology
2010;44(1):74-78
- CountryChina
- Language:Chinese
-
Abstract:
To study the pharmacokinetics of ~(131)I-Metuximab injection (Licartin) combined with transarterial chemoembolization (TACE) for treatment of hepatocellular carcinoma (HCC). MethodsLicartin (27.75 MBq/kg) and the mixture of anticancer drug and Lipiodol were sequentially administered with interval of 20 minutes to 15 patients with HCC via a transfemoral catheter.After the Licartin was administrated, the pharmacokinetic and biodistribution data were evaluated through venous blood samples,urine collections,and 4 γ-scintigraphies (SPECT) over 7 days. The pharmacokinetic parameters were determined from integration of the blood radioactivity-time curves using the SPSS 12.0 software. The tumor-no-tumor ratio (T/NT) was calculated by ROI. Absorbed doses in organ were estimated according to the medical internal radiation dose formalism. The biodistribution of licartin within patient's body at different time points was compared for various organs using analysis of variance for repeated measures, as well as the T/NT ratio. ResultsThe blood radioactivity-time curves followed the dynamics two-compartment model, with the major pharmacokinetic parameters including t_(1/2)α(1.96±1.65) h, and t_(1/2)α(19.07±5.91) h,and t_(1/2)β (57.09±10.92) h, and C_(max) 2.113×10~9min~(-1)·L~(-1), and AUC_(0-∞) 1.302×10~(11) h·min~(-1)·L~(-1), respectively. The accumulated urine radioactivity was 52.2% of administrated dosage during 144 h after administration. There were statistical significant difference of biodistribution of licartin and T/NT ratio between organs at different time points (F=6.583, P<0.01 and F=3.546, P<0.01). SPECT scans showed the significant accumulation of the radioconjugate in liver tumor and faint uptake in other organs for 14 days. Tumor-to-liver ratio decreased from 2.88±1.02 at 3 h to 1.64±0.40 at 168 h (n=7). Organ absorbed dose was (3.19±1.01) Gy in liver (n=12) and (0.55±0.09) Gy in red marrow (n=7). ConclusionLicartin combined with TACE for treatment of HCC is helpful to significantly accrete the radioconjugate in liver tumor, and protect normal organs from radiotoxictiy.
