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Absorbed dose assessment of (177)Lu-zoledronate and (177)Lu-EDTMP for human based on biodistribution data in rats.

Yousefnia H, Zolghadri S, Jalilian AR - J Med Phys (2015 Apr-Jun)

Bottom Line: Recently, (177)Lu was successfully labeled with zoledronic acid ((177)Lu-ZLD) as a new generation potential bisphosphonate and demonstrated significant accumulation in bone tissue.The highest absorbed dose for both (177)Lu-ZLD and (177)Lu-EDTMP is observed in trabecular bone surface with 12.173 and 10.019 mSv/MBq, respectively.The results showed that (177)Lu-ZLD has better characteristics compared to (177)Lu-EDTMP and can be a good candidate for bone pain palliation.

View Article: PubMed Central - PubMed

Affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.

ABSTRACT
Over the past few decades, several bone-seeking radiopharmaceuticals including various bisphosphonate ligands and β-emitting radionuclides have been developed for bone pain palliation. Recently, (177)Lu was successfully labeled with zoledronic acid ((177)Lu-ZLD) as a new generation potential bisphosphonate and demonstrated significant accumulation in bone tissue. In this work, the absorbed dose to each organ of human for (177)Lu-ZLD and (177)Lu-ethylenediaminetetramethylene phosphonic acid ((177)Lu-EDTMP;as the only clinically bone pain palliation agent) was investigated based on biodistribution data in rats by medical internal radiation dosimetry (MIRD) method. (177)Lu-ZLD and (177)Lu-EDTMP were prepared in high radiochemical purity (>99%, instant thin layer chromatography (ITLC)) at the optimized condition. The biodistribution of the complexes demonstrated fast blood clearance and major accumulation in the bone tissue. The highest absorbed dose for both (177)Lu-ZLD and (177)Lu-EDTMP is observed in trabecular bone surface with 12.173 and 10.019 mSv/MBq, respectively. The results showed that (177)Lu-ZLD has better characteristics compared to (177)Lu-EDTMP and can be a good candidate for bone pain palliation.

No MeSH data available.


Related in: MedlinePlus

Chemical structure for zoledronic acid monohydrate
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Figure 1: Chemical structure for zoledronic acid monohydrate

Mentions: According to the results of three randomized phase III clinical trials enrolling more than 3,000 patients; zoledronic acid (1-hydroxy-2-(imidazol-1-yl-amino)-ethylidene-biphosphonic acid) [Figure 1] has showed its high potential as a new-generation bisphosphonate that is effective in the treatment of bone metastases secondary to all solid tumor types and bone lesions from multiple myeloma.[4567]


Absorbed dose assessment of (177)Lu-zoledronate and (177)Lu-EDTMP for human based on biodistribution data in rats.

Yousefnia H, Zolghadri S, Jalilian AR - J Med Phys (2015 Apr-Jun)

Chemical structure for zoledronic acid monohydrate
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4478643&req=5

Figure 1: Chemical structure for zoledronic acid monohydrate
Mentions: According to the results of three randomized phase III clinical trials enrolling more than 3,000 patients; zoledronic acid (1-hydroxy-2-(imidazol-1-yl-amino)-ethylidene-biphosphonic acid) [Figure 1] has showed its high potential as a new-generation bisphosphonate that is effective in the treatment of bone metastases secondary to all solid tumor types and bone lesions from multiple myeloma.[4567]

Bottom Line: Recently, (177)Lu was successfully labeled with zoledronic acid ((177)Lu-ZLD) as a new generation potential bisphosphonate and demonstrated significant accumulation in bone tissue.The highest absorbed dose for both (177)Lu-ZLD and (177)Lu-EDTMP is observed in trabecular bone surface with 12.173 and 10.019 mSv/MBq, respectively.The results showed that (177)Lu-ZLD has better characteristics compared to (177)Lu-EDTMP and can be a good candidate for bone pain palliation.

View Article: PubMed Central - PubMed

Affiliation: Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.

ABSTRACT
Over the past few decades, several bone-seeking radiopharmaceuticals including various bisphosphonate ligands and β-emitting radionuclides have been developed for bone pain palliation. Recently, (177)Lu was successfully labeled with zoledronic acid ((177)Lu-ZLD) as a new generation potential bisphosphonate and demonstrated significant accumulation in bone tissue. In this work, the absorbed dose to each organ of human for (177)Lu-ZLD and (177)Lu-ethylenediaminetetramethylene phosphonic acid ((177)Lu-EDTMP;as the only clinically bone pain palliation agent) was investigated based on biodistribution data in rats by medical internal radiation dosimetry (MIRD) method. (177)Lu-ZLD and (177)Lu-EDTMP were prepared in high radiochemical purity (>99%, instant thin layer chromatography (ITLC)) at the optimized condition. The biodistribution of the complexes demonstrated fast blood clearance and major accumulation in the bone tissue. The highest absorbed dose for both (177)Lu-ZLD and (177)Lu-EDTMP is observed in trabecular bone surface with 12.173 and 10.019 mSv/MBq, respectively. The results showed that (177)Lu-ZLD has better characteristics compared to (177)Lu-EDTMP and can be a good candidate for bone pain palliation.

No MeSH data available.


Related in: MedlinePlus