rhenium(v)dimercaptosuccinic-acid and 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

[186Re]Re(V)DMSA, a beta-emitting analogue of the tumour imaging radiopharmaceutical pentavalent [99mTc]Tc(V)DMSA of possible value in tumour therapy, is readily prepared by stannous reduction of [186Re]ReO4 in the presence of dimercaptosuccinic acid at 100 degrees C using a commercial DMSA kit as used for renal imaging with 99mTc, and purified using a disposable sample preparation column. The complex has been identified as [ReO(DMSA)2] by NMR, optical and i.r., spectroscopy and elemental analysis.

Topics: Humans; Indicators and Reagents; Isomerism; Molecular Structure; Neoplasms; Organometallic Compounds; Radioisotopes; Rhenium; Succimer