Preparation and preliminary biological evaluation of a 177Lu labeled nitroimidazole derivative for possible use in targeted tumor therapy
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Tapas Das
Summary
The preparation and preliminary biological evaluation of a metronidazole-BFCA (bifunctional chelating agent) conjugate labeled with 177Lu is reported. Metronidazole, a well known hypoxia marker has been suitably derivatized and coupled with a polyazamacrocyclic BFCA, namely, para-aminobenzyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (p-amino-benzyl-DOTA). 177Lu, which is presently being considered as one of the pivotal radionuclides for targeted therapy was produced in adequate specific activity (∼185 TBq/g) and high radionuclidic purity (99.99%) by irradiating enriched (60.6% 176Lu) Lu2O3 target at a moderate thermal neutron flux of 3×1013 n/cm2/s. The metronidazole-BFCA conjugate was radiolabeled with 177Lu in high radiochemical purity (97%). Preliminary biodistribution studies carried out in Swiss mice bearing fibrosarcoma tumors revealed good tumor uptake (1.30% ID/g at 30 min post-injection) with rapid renal clearance (94.48% ID at 30 min post-injection) and significant tumor to blood (28.00 at 3 h post-injection) and tumor to muscle (14.00 at 3 h post-injection) ratios.
© by Oldenbourg Wissenschaftsverlag, München
Artikel in diesem Heft
- Preface - Special Issue: NUCAR 2005
- Incomplete fusion mechanism in 16O + 93Nb reaction at 6 MeV/nucleon: Recoil range measurements
- Extraction of actinides using N, N, N′, N′-tetraoctyl diglycolamide (TODGA): a thermodynamic study
- Extraction of neptunium(IV) by a mixture of 3-phenyl-4-acetyl-5-isoxazolone and tri-n-octyl phosphine oxide
- Third phase formation in the extraction of Th(NO3)4 by tri-2-methyl butyl phosphate from nitric acid media
- Solvent extraction behaviour of some fission product elements with N,N-dihexyl octanamide and tri-n-butyl phosphate under simulated PUREX process conditions
- Transport of uranium from nitric acid solution by non-dispersive solvent extraction using a hollow fibre contactor
- Fixation of some major fission products in NaZr2P3O12 ceramic employing microwave heating
- Synthesis, characterization and structural refinement of polycrystalline uranium substituted zirconolite CaZr0.9U0.1Ti2O7
- Effect of glass composition on diffusion of cesium in borosilicate glass
- Studies on diffusional mobility and selectivity of I− ion in plasticized anion-exchange membrane using radiotracer
- BEHSA grafted polymer for selective extraction of U(VI), Th(IV) and La(III) from acidic matrices and environmental samples – a green process
- Studies on the dissolution behaviour of ThO2 and (U,Th)O2 by a solid state reaction method
- Studies on some divalent metal α-isosaccharinic acid complexes
- Effect of humic acid on cesium sorption on silica colloids
- Preparation and preliminary biological evaluation of a 177Lu labeled nitroimidazole derivative for possible use in targeted tumor therapy
Artikel in diesem Heft
- Preface - Special Issue: NUCAR 2005
- Incomplete fusion mechanism in 16O + 93Nb reaction at 6 MeV/nucleon: Recoil range measurements
- Extraction of actinides using N, N, N′, N′-tetraoctyl diglycolamide (TODGA): a thermodynamic study
- Extraction of neptunium(IV) by a mixture of 3-phenyl-4-acetyl-5-isoxazolone and tri-n-octyl phosphine oxide
- Third phase formation in the extraction of Th(NO3)4 by tri-2-methyl butyl phosphate from nitric acid media
- Solvent extraction behaviour of some fission product elements with N,N-dihexyl octanamide and tri-n-butyl phosphate under simulated PUREX process conditions
- Transport of uranium from nitric acid solution by non-dispersive solvent extraction using a hollow fibre contactor
- Fixation of some major fission products in NaZr2P3O12 ceramic employing microwave heating
- Synthesis, characterization and structural refinement of polycrystalline uranium substituted zirconolite CaZr0.9U0.1Ti2O7
- Effect of glass composition on diffusion of cesium in borosilicate glass
- Studies on diffusional mobility and selectivity of I− ion in plasticized anion-exchange membrane using radiotracer
- BEHSA grafted polymer for selective extraction of U(VI), Th(IV) and La(III) from acidic matrices and environmental samples – a green process
- Studies on the dissolution behaviour of ThO2 and (U,Th)O2 by a solid state reaction method
- Studies on some divalent metal α-isosaccharinic acid complexes
- Effect of humic acid on cesium sorption on silica colloids
- Preparation and preliminary biological evaluation of a 177Lu labeled nitroimidazole derivative for possible use in targeted tumor therapy
