Preparation and pharmacokinetics of samarium(III)-153-labeled DTPA-bis-biotin. Characterization and theoretical studies of the samarium(III)-152 conjugate.

The complex(153)Sm(III)DTPA-bis-biotin was prepared with a 99% radiochemical purity and a specific activity of 370 MBq/mg employing a molar ratio of DTPA-bis-biotin/Sm from 2 to 4 at pH 8.0. In vitro studies demonstrated that the complex is stable after dilution in saline and in human serum. Avidity of labeled biotin for avidin was not affected by the labeling procedure. Pharmacokinetic data of (153)Sm(III)DTPA-bis-biotin in normal mice showed that blood clearance is biexponential during the time interval from 0 to 24 h and that 3 h postinjection 92 +/- 4.32% of the dose is eliminated in the urine. To have further evidence which could sustain that (153)Sm(III)DTPA-bis-biotin is stable in solution as a real coordination complex, (152)Sm(III)DTPA-bis-biotin was obtained in macroscopic quantities and its characterization was done by IR, TGA, and conductivity measurements. The results indicated that the complex was chemically pure, where the Sm(3+) ion is neutralized by three carboxylate groups of the DTPA-bis-biotin ligand and coordinated to it. Using the Force Field method followed by ab initio calculations, the DTPA-bis-biotin and the Sm(III)DTPA-bis-biotin molecules were done. Accordingly, the coordination sphere of Sm(III) was totally satisfied with nitrogen and oxygen donors; the best coordination number was 9. The conformation geometry of both compounds is presented.

[Radionuclide study of cutaneous melanomas with 99m Tc-HMPAO: visualization of metastases and recurrence]. / Estudio gammagráfico de los melanomas cutáneos con 99m Tc-HMPAO: visualización de metástasis y recidivas.

Malignant cutaneous melanoma (MCM) is a very aggressive disease that becomes in a true problem of health because of the increase in the last 5 years. In the present paper, authors report the detection of the tumor, metastases and recurrences mean 99mTc HMPAO. We presented 5 cases of MCM patients and observed the radiopharmaceutical uptake in skin, nodules and recurrent tumor lesions. Because of the number of patients was limited, authors recommended the research with a lot of patients. The gammagraphic studies could be very important for the staging of the disease and early detection of metastases and recurrent lesions.

Preparation, biodistribution, and dosimetry of 188Re-labeled MoAb ior cea1 and its F(ab')2 fragments by avidin-biotin strategy.

The biotinylated monoclonal antibody (MoAb) ior cea1 and its F(ab')2 fragments were labeled with Re-188 by combination of avidin-biotin strategy. 188Re-MoAb, 188Re-MoAb-biotin, 188Re-F(ab')2, and 188Re-F(ab')2-biotin preparations were produced for these studies with specific activities of 1.30+/-0.18 GBq/mg and from instant freeze-dried kit formulations using ethane-1-hydroxy-1,1-diphosphonic acid (EHDP) as a weak competing ligand. There were no significant differences (p > 0.05) between the biodistribution in mice of biotinylated and unbiotinylated 188Re-labeled immunoconjugates. When avidin was injected as a chase after injection of 188Re-MoAb-biotin or 188Re-F(ab')2-biotin, the blood radioactivity level decreased approximately 75% (cumulated activity) and the effective dose decreased almost 25% with respect to that of the radioimmunoconjugates in which the chase effect was not used. Our results suggest that 188Re-labeled biotinylated MoAb ior ceal and its F(ab')2 fragments prepared by this method are stable complexes in vivo.

[Radiolabeling of a new agent for the study of colorectal tumors]. / Radiomarcaje de un nuevo agente para el estudio de tumores colorrectales.

A new Monoclonal Antibody (AcMo) ior-C5, highly specific for the most part of colorectal adenocarcinomas has been developed. The AcMo was labeled with 99mTc by the Schwarz's direct method using molar ratios MAb: reductant of 1:1,000 and 1:2,000. The first molar ratio was the most adequate for the preparation of the radiopharmaceutical. A labeling yield greater than 95% was obtained. Several <> assays were carried out in order to evaluate the stability of the preparation, whose results reflected the presence of the stable complex 99mTc-IgG. The biodistribution patterns for both preparations were similar. The excreting organs behaved like normal. Nevertheless, a greater renal excretion was observed for the preparation of the molar ratio of 1:2.000, which could be due to the presence of low affinity sites observed in this preparation. They are vulnerable to the trans-chelation of the 99mTc toward cysteine or glutathione present in plasma and tissues.