Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose
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Sudipta Chakraborty
Abstract
The work reported in this paper provides a systematic study towards the development of an optimized strategy for preparation of a clinically relevant dose of 90Y-labeled dimeric RGD peptide derivative, DOTA-E[c(RGDfK)]2 [DOTA-(RGD)2] for in vivo targeted therapy utilizing 90Y obtained from a novel electrochemical 90Sr/90Y generator. The performance of the generator was evaluated to ensure its suitability for providing 90Y in adequate quantity and purity required for formulation of clinically relevant dose for PRRT. 90Y-DOTA-(RGD)2 was synthesized in high yield (86.2 ± 2.5%) and radiochemical purity (98.4 ± 0.5%) using clinically relevant dose (∼3.8 GBq) of 90Y. In vitro stability studies revealed that the radiolabeled conjugate retained its radiochemical purity in normal saline and human serum. Preliminary biodistribution studies carried out in C57/BL6 mice bearing melanoma tumors showed that the preparation exhibited significant tumor uptake (5.30 ± 0.78% of injected activity at 30 min post-injection) with good tumor to background ratio. The optimized radiolabeling protocol seems to be an attractive strategy which is largely viewed as a springboard to realize scope of developing 90Y labeled cyclic RGD peptides for targeted therapy of tumors over-expressing integrin-αvβ3 receptors.
©2014 Walter de Gruyter Berlin/Boston
Artikel in diesem Heft
- Frontmatter
- Excitation function of (p, α) nuclear reaction on enriched 67Zn: possibility of production of 64Cu at low energy cyclotron
- Radiochemical measurement of neutron-spectrum averaged cross sections for the formation of 64Cu and 67Cu via the (n,p) reaction at a TRIGA Mark-II reactor: Feasibility of simultaneous production of the theragnostic pair 64Cu/67Cu
- A novel dipicolinamide-dicarbollide synergistic solvent system for actinide extraction
- Plutonium sorption to nanocast mesoporous carbon
- Retrieval and purification of an aged 231Pa source from its decay daughters
- Natural radioactivity measurements in agricultural soil, fertilizer and crops in some specific areas of Kingdom of Saudi Arabia
- Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose
- Radiochemical synthesis and biological evaluation of 3-[4-(4-[18F]fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine as dopamine D4 receptor radioligand
- Synthesis and initial biological evaluation of a novel Tc-99m radioligand as a potential agent for 5-HT1A receptor imaging
- Clinical scale preparation and evaluation of 131I-Rituximab for Non-Hodgkin's Lymphoma
Artikel in diesem Heft
- Frontmatter
- Excitation function of (p, α) nuclear reaction on enriched 67Zn: possibility of production of 64Cu at low energy cyclotron
- Radiochemical measurement of neutron-spectrum averaged cross sections for the formation of 64Cu and 67Cu via the (n,p) reaction at a TRIGA Mark-II reactor: Feasibility of simultaneous production of the theragnostic pair 64Cu/67Cu
- A novel dipicolinamide-dicarbollide synergistic solvent system for actinide extraction
- Plutonium sorption to nanocast mesoporous carbon
- Retrieval and purification of an aged 231Pa source from its decay daughters
- Natural radioactivity measurements in agricultural soil, fertilizer and crops in some specific areas of Kingdom of Saudi Arabia
- Utilization of a novel electrochemical 90Sr/90Y generator for the preparation of 90Y-labeled RGD peptide dimer in clinically relevant dose
- Radiochemical synthesis and biological evaluation of 3-[4-(4-[18F]fluorobenzyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine as dopamine D4 receptor radioligand
- Synthesis and initial biological evaluation of a novel Tc-99m radioligand as a potential agent for 5-HT1A receptor imaging
- Clinical scale preparation and evaluation of 131I-Rituximab for Non-Hodgkin's Lymphoma
