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This study was aimed at the preparation of 177Lu-CHX-A″-DTPA-Rituximab injection at the hospital pharmacy for non-Hodgkin lymphoma. Rituximab was conjugated with CHX-A″-DTPA-NCS and the CHX-A″-DTPA-Rituximab conjugate was radiolabeled with 177Lu in > 95% purity. The product exhibited excellent in vitro stability up to 5 days at 37 °C. In vitro cell binding studies in Raji cells confirmed the specificity of 177Lu-CHX-A″-DTPA-Rituximab to CD20 antigen. The radioimmunoconjugate exhibited predominantly hepatobiliary clearance and low bone uptake in Swiss mice. Preliminary clinical studies corroborated the usefulness of 177Lu-CHX-A″-DTPA-Rituximab for therapy of non-Hodgkin lymphoma. [ABSTRACT FROM AUTHOR]

While neutron activation of natural TmO is the convenient strategy for producing Tm for use in palliative care of painful bone metastases, the coproduction of Tm ( t = 1.92 years) is as an impediment towards its clinical utility. The production strategy has been optimized to obtain Tm with adequate specific activity and radionuclidic purity. Preliminary clinical studies carried out using the Tm-labeled ethylenediaminetetramethylene phosphonic acid (Tm-EDTMP) showed site specific localization of the radiopharmaceutical in skeleton with preferential accumulation in metastatic lesions along with almost no accumulation in non-target organs, a distribution pattern comparable to that of Tc-labeled methylene diphosphonate (Tc-MDP). [ABSTRACT FROM AUTHOR]

Hydroxyapatite (HA) [Ca(PO)(OH)] particles radiolabeled with a variety of β emitting lanthanide radionuclides and also pseudolanthanide Y have been proposed for the treatment of arthritis. A ready-to-use cold kit of HA particles (1-10 µm size) was developed for fast and convenient formulation of radiolanthanide-labeled HA particles at hospital radiopharmacy. Six radionuclides namely, Er, Lu, Sm, Ho, Pr and Y, having β emissions of a wide range of energy [E = 0.34-2.28 MeV] were identified and produced by thermal neutron activation. Clinical doses of HA particles labeled with these radionuclides were prepared in high yield (>97 %) and radiochemical purity (>99 %) using the cold kits. Pre-clinical studies of Lu-HA carried out in Wistar rats bearing arthritis in knee joints revealed no leakage of the activity from the joints. In preliminary clinical investigation using 333 ± 46 MBq doses of the same preparation, significant improvement in the disease conditions was reported in patients with chronic rheumatoid arthritis of knee joints. [ABSTRACT FROM AUTHOR]

The objective of the present work is to prepare freeze-dried DOTA-TATE and DOTA-NOC kits for the easy and convenient preparation of patient doses of Lu-DOTA-TATE and Lu-DOTA-NOC, respectively at the hospital radiopharmacy and to compare the radio-peptides with respect to their radiochemical and biological behaviors. Freeze-dried kits of DOTA-TATE and DOTA-NOC, comprising a lyophilized mixture of 200 μg of DOTA-peptide, 80 mg of gentisic acid and 13.9 mg of ammonium acetate were prepared. Therapeutic doses of Lu-labeled peptides (up to 200 mCi, 7.4 GBq) were prepared using these kits and Lu, produced in-house, with >99 % radiochemical purity and high stability following an easy and convenient protocol. Comparative pharmacokinetic behavior of the radio-peptides was studied by carrying out biodistribution studies in normal Wistar rats which revealed higher retention of activity in several major organs and slower renal clearance for Lu-DOTA-NOC compared to that of Lu-DOTA-TATE. Preliminary pharmacokinetic studies, carried out in limited number of patients suffering from cancers of neuroendocrine origins, showed lower accumulation of activity in vital organs and faster renal clearance of Lu-DOTA-TATE compared to that of Lu-DOTA-NOC. [ABSTRACT FROM AUTHOR]