succimer and Liver-Neoplasms

Rhenium-188 is one of the most readily available generator derived and useful radionuclides for therapy emitting β(-) particles (2.12 MeV, 71.1% and 1.965 MeV, 25.6%) and imageable gammas (155 keV, 15.1%). The (188)W/(188)Re generator is an ideal source for the long term (4-6 months) continuous availability of no carrier added (nca) (188)Re suitable for the preparation of radiopharmaceuticals for radionuclide therapy. The challenges associated with the double neutron capture route of production of the parent (188)W radionuclide have been a major impediment in the progress of application of (188)Re. Tungsten-188 of adequate specific activity can be prepared only in 2-3 of the high flux reactors operating in the World. Several useful technologies have been developed for the preparation of clinical grade (188)W/(188)Re generators. Since the specific activity of (188)W used in the generator is relatively low 185 GBq( < 5 Ci)/g], the eluted (188)ReO(4)(-) can have low radioactive concentration often insufficient for radiopharmaceutical preparation. However, several efficient post elution concentration techniques have been developed that yield clinically useful (188)ReO(4)(-) solutions. Rhenium-188 has been used for the preparation of therapeutic radiopharmaceuticals for the management of diseases such as bone metastasis, rheumatoid arthritis and primary cancers. Several early phase clinical studies using radiopharmaceuticals based on (188)Re-labeled phosphonates, antibodies, peptides, lipiodol and particulates have been reported. This article reviews the availability and use of (188)Re including a discussion of why broader use of (188)Re has not progressed as expected as a popular radionuclide for therapy.

Topics: Adsorption; Antibodies, Monoclonal; Arthritis, Rheumatoid; Bone Neoplasms; Carcinoma, Hepatocellular; Chromatography; Coronary Disease; Drug Combinations; Equipment Design; Humans; Iodized Oil; Liver Neoplasms; Musculoskeletal Pain; Neoplasms; Organometallic Compounds; Palliative Care; Peptides; Radioimmunotherapy; Radioisotopes; Radionuclide Generators; Radiopharmaceuticals; Rhenium; Skin Neoplasms; Succimer

To investigate the targeting activity of the peptide (named P1c) derived from connective tissue growth factor (CTGF) to αvβ3-rich tumor cells.. P1c was synthesized and conjugated with ultrasuperparamagnetic iron oxide particles (USPIOs) coated with meso-2,3-dimercaptosuccinic acid (DMSA). The specific binding activity of P1c-USPIOs to αvβ3 was verified by solid phase binding assay. The combination of P1c-USPIOs with a human primary liver cancer cell (Bel 7402) with αvβ3-positive expression and uptake of P1c-USPIOs by cells was investigated by Prussian blue staining, transmission electron microscopy (TEM), and magnetic resonance imaging (MRI). The targeting activity of the probe in vivo was also evaluated using a small-animal tumor model by MRI.. The cell uptake of P1c-USPIOs was observed in a dose-dependent manner, whereas no significant particle uptake was found in the plain USPIOs group. The differences on T2*-weighted imaging were also found by MRI and the signal intensity (SI) was statistically reduced after coculture of Bel 7402 cells with P1c-USPIOs at a concentration of 20-80 μg/mL compared with plain USPIOs (P < 0.05). The in vivo study showed that the signal reduction was distributed mainly in the periphery and some central areas of the tumor. The tumor-to-muscle CNR (contrast-to-noise ratio) at 12 hours after the administration of the P1c-USPIOs was statistically significantly different compared to those at 0 hour, 1 hour, or the plain USPIO group (P < 0.05).. The peptide P1c might be a good candidate as a targeting carrier for drugs or tracers.

Topics: Cell Line, Tumor; Coloring Agents; Disease Progression; Ferric Compounds; Ferrocyanides; Humans; Integrin alphaVbeta3; Liver Neoplasms; Magnetic Resonance Imaging; Microscopy, Electron, Transmission; Neoplasm Metastasis; Peptides; Succimer

For this study, 24 patients with medullary thyroid cancer (MTC) and 10 with carcinoid-/GEP-tumours underwent scintigraphy with 123I-Tyr3-octreotide or 111In-DTPA-D-Phe1-octreotide (Octreoscan) or 99mTc-V-DMSA. Calcitonin and CEA were elevated in MTC patients, the other had tumour lesions on CT. Octreoscan-scintigraphy was positive in 68% of all suspicious cases. On the other hand, 123I-Tyr3-octreotide showed only rarely positive results. 99mTc-V-DMSA-scans in MTC patients were positive in 23%. Liver metastases could be seen only with Octreoscan in the non-MTC-group. These results showed better sensitivity of 111In-labelled octreotide.

Topics: Adult; Aged; Calcitonin; Carcinoembryonic Antigen; Carcinoid Tumor; Carcinoma, Medullary; False Positive Reactions; Female; Gastrointestinal Neoplasms; Humans; Indium Radioisotopes; Iodine Radioisotopes; Liver Neoplasms; Male; Middle Aged; Octreotide; Organotechnetium Compounds; Pancreatic Neoplasms; Pentetic Acid; Radionuclide Imaging; Receptors, Somatostatin; Sensitivity and Specificity; Succimer; Technetium Tc 99m Dimercaptosuccinic Acid; Thyroid Neoplasms

Topics: Hemangioma; Humans; Liver Neoplasms; Middle Aged; Organotechnetium Compounds; Radionuclide Imaging; Succimer; Technetium Tc 99m Dimercaptosuccinic Acid; Technetium Tc 99m Medronate; Thallium Radioisotopes; Ultrasonography

This case report describes the localization and categorization of tumors using 99mTc(V)-dimercaptosuccinic acid and [131I]metaiodobenzylguanidine scans in a very uncommon case of medullary thyroid carcinoma associated with pheochromocytoma (Sipple's syndrome) and hepatocellular carcinoma. Technetium-99m(V)-dimercaptosuccinic acid showed accumulation only in medullary thyroid carcinoma, but [131I]metaiodobenzylguanidine scans were positive in both medullary thyroid carcinoma and pheochromocytoma. In advanced Sipple's syndrome, combined use of [99mTc(V)]dimercaptosuccinic acid and [131I]metaiodobenzylguanidine may be useful for the categorization of tumor mass lesions and planning appropriate therapy.

Topics: 3-Iodobenzylguanidine; Adrenal Gland Neoplasms; Aged; Carcinoma; Carcinoma, Hepatocellular; Humans; Iodine Radioisotopes; Iodobenzenes; Liver Neoplasms; Male; Multiple Endocrine Neoplasia; Neoplasms, Multiple Primary; Organometallic Compounds; Pheochromocytoma; Radionuclide Imaging; Succimer; Sulfhydryl Compounds; Technetium; Technetium Tc 99m Dimercaptosuccinic Acid; Thyroid Neoplasms