[Pharmacokinetics of injection of iodine-131 labelling MEI-TUO-XI monoclonal antibody in human body].

To study pharmacokinetics of injection of iodine-131 labelling MEI-TUO-XI monoclonal antibody (hepatoma monoclonal antibody HAb18 F(ab')2) in vivo. 24 cases of primary hepatocelluar carcinoma (PHC) were equally divided into the low dose group, middle dose group and high dose group. After the relevant injection was administrated into the hepatic artery of each case, intravenous blood and urine samples were separately collected at different time for determination of the radioactive count ratio (min(-1)). The proportion of 131I-HAb18 F(ab')2 in serum of each blood sample was determined, and the radioactive count ratio (min(-1)) of druggery for each blood sample was revised according to the proportion. The pharmacokinetic parameters were calculated using DAS ver 1.0 (Drug And Statistics for Windows) program. The component of urine radiomaterial was determined and the percentages of urine radioactivity in administration dosage were calculated. The catabolism of the injection with time accorded with dynamics two-compartment model. The catabolism product was mainly free-131I and was excreted via kidney; the urine radioactivity was 47.70%-51.16% of administration dosage during 120 h after administration of drug. Therefore, the pharmacokinetics of the injection can satisfy the clinical demands. The drug dose recommended for clinical use was 27.75 MBq of the injection for each kg of human body.

Targeting radioimmunotherapy of hepatocellular carcinoma with iodine (131I) metuximab injection: clinical phase I/II trials.

PURPOSE: 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. METHODS AND MATERIALS: 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. RESULTS: 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). CONCLUSION: Iodine (131I) metuximab injection is safe and active for HCC patients.

[Application study of JPEG2000 image compression in nuclear medicine].

To study the usefulness of JPEG2000 compression for nuclear medicine (NM) image, normal and abnormal static images were compressed using a JPEG2000 plug-in. For lossless algorithm, the compressing ratio (CR) was calculated. For lossy algorithm, images were visually analyzed by NM physicians and ROC curves were generated. The area under ROC curve (AUC) was used as the index of image diagnostic quality. Paired sample t tests were performed to compare the AUCs. It was found that the lossless CR was (1.34+/-0.05) : 1. For lossy algorithm, the AUC decreased with the increase of CR. Comparison between the original and the compressed images revealed no significant difference for 10:1 CR but significant difference for bigger CRs. It was concluded that lossless compression has little usefulness for NM image because of very low CR. While lossy compression isused, the diagnostic quality of static NM images is preserved at CRs 50 : 1,40 : 1, 30 : 1,20 : 1 up to 10 : 1. For other types of NM image, CR should be increased or decreased according to their characteristics, especially the level of intrinsic statistical noise of NM image.

Biodistribution and localization of iodine-131-labeled metuximab in patients with hepatocellular carcinoma.

PURPOSE: Radioimmunotherapy may improve the outcome of hepatocellular carcinoma (HCC) patients by delivering targeted radiation to liver lesion tissue while relatively sparing nontarget tissues. This study was designed to observe the biodistribution, localization and imaging characteristics of 131I -labeled Metuximab in 24 patients with HCC to determine the diagnostic and therapeutic potential of this antibody. METHODS: Twenty-four HCC patients were randomly divided into three groups to receive 18.5, 27.75 and 37 MBq/kg of 131I-labeled Metuximab per kilogram of body weight, respectively. 99mTc-sodium phytate was administered intravenously and the single photon emission computed tomography (SPECT) scanning was performed. After 48 h, 131I -labeled Metuximab was injected by hepatic artery intubation, and SPECT scan performed at 7 d. The percentage of absorbed 131I (%ID) and the time-dependent 131I tumor:nontumor tissue (T/NT) ratios were calculated at 12, 48, 96 and 192 h after injection. RESULTS: The positive Imaging result of MAb scanning in 24 patients showed that the iodine 131 conjugated to Metuximab was apparently accumulated more in hepatoma. Biodistribution studies of 131I-Metuximab in trial I demonstrated that the comparable % ID uptake in tumor (with a T/NT ratio at 12, 48, 96 and 192 h) to that in such normal organs, as thyroid, heart, lung, spleen and intestines were all more than one. The optimal imaging time for the highest T/NT ratio in liver was at 192 h. CONCLUSION: 131I-labeled Metuximab could deliver relatively selective radiation to tumor tissues and may have potential efficacy in relieving hepatocellular carcinoma.

[Biological distribution of 131I-HAb18F(ab')2 in patients with hepatocellular carcinoma].

Before 131I-HAb18F(ab')2 administration, 24 cases of mid-term or advanced hepatocellular carcinoma(HCC) were given Lugol's Liquid to block the thyroid gland, and submitted to hepatic colloid imaging. The cases were randomly divided into 3 groups. Then 131I-HAb18F(ab')2 was injected into the target hepatic artery with doses of 0.5, 0.75, 1.0 mCi/kg, respectively. At the followed 10, 48, 96 and 192 hours, 131I-HAb18F(ab')2 distribution in human body was acquired by whole body dynamic image with Single photon emission computed tomography(SPECT). The results showsed that 131I-HAb18F(ab')2 in tumor tissue was significantly higher than that in normal liver tissue and other organs. This difference became obvious as time passed. 131I-HAb18F(ab')2 is stable in human body and it can combine with HCC tissue specifically. So it is a new medicine deserving further research for the treatment of HCC.

[The primary applications of ¹5³Sm-EDTMP plus chemotherapy in the treatment of bone metastasis of lung cancer].

BACKGROUND: To study the clinical effects of ¹5³Sm-EDTMP plus chemotherapy in the treatment of bone metastasis of lung cancer. METHODS: One hundred and ten lung cancer patients with one metastasis [male 82 and female 28, aged from 32 to 76 yrs; squamous cell carcinoma 28, adenocarcinoma 27, small cell lung cancer (SCLC) 7, mix type 41, alveolar carcinoma 7] who did not undergo an operation were entered into this study. The patients were divided into 3 groups: ¹5³Sm-EDTMP therapy only (37 cases), ¹5³Sm-EDTMP plus chemotherapy after 3 days (42 cases), 30 days after chemotherapy plus ¹5³Sm-EDTMP (31 cases). The dosages of ¹5³Sm-EDTMP ranged from 1 111 to 2 660 MBq. The patients with SCLC were adapted CCNU, MTX and CTX; those with non-small cell lung cancer (NSCLC) were adapted MMC, VCR and DDP. Statistic analysis of the data was performed by Chi-square test. RESULTS: Total pain relief rate for ¹5³Sm-EDTMP only was 89.2% , for ¹5³Sm-EDTMP plus chemotherapy was 92.8%, and for chemotherapy plus 153 Sm EDTMP was 90.3% . The foci disappeared in 9 cases with ¹5³Sm-EDTMP only, in 12 cases with ¹5³Sm-EDTMP plus chemotherapy, and in 9 cases with chemotherapy plus ¹5³Sm-EDTMP. The 1 year survival rate was 29.7%(11/37) by 153 Sm only, 40.5%(17/42) by 153 Sm plus chemotherapy, 38.7%(12/31) by chemotherapy plus ¹5³Sm-EDTMP. CONCLUSIONS: ¹5³Sm-EDTMP plus chemotherapy is effective in the treatment of bone metastasis of lung cancer.