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. 2015 Winter;3(1):35-42.

Production, biodistribution assessment and dosimetric evaluation of (177)Lu-TTHMP as an agent for bone pain palliation

Samaneh Zolghadri  1 , Hassan Yousefnia  1 , Amir Reza Jalilian  1 , Mohammad Ghannadi-Maragheh  1
Affiliations

Production, biodistribution assessment and dosimetric evaluation of (177)Lu-TTHMP as an agent for bone pain palliation

Samaneh Zolghadri et al. Asia Ocean J Nucl Med Biol. 2015 Winter.

Abstract

Objectives: Recently, bone-avid radiopharmaceuticals have been shown to have potential benefits for the treatment of widespread bone metastases. Although (177)Lu-triethylene tetramine hexa methylene phosphonic acid (abbreviated as (177)Lu-TTHMP), as an agent for bone pain palliation, has been evaluated in previous studies, there are large discrepancies between the obtained results. In this study, production, quality control, biodistribution, and dose evaluation of (177)Lu-TTHMP have been investigated and compared with the previously reported data.

Methods: TTHMP was synthesized and characterized, using spectroscopic methods. Radiochemical purity of the (177)Lu-TTHMP complex was determined using instant thin-layer chromatography (ITLC) and high performance liquid chromatography (HPLC) methods. The complex was injected to wild-type rats and biodistribution was studied for 7 days. Preliminary dose evaluation was investigated based on biodistribution data in rats.

Results: (177)Lu was prepared with 2.6-3 GBq/mg specific activity and radionuclide purity of 99.98%. (177)Lu-TTHMP was successfully prepared with high radiochemical purity (>99%). The complex showed rapid bone uptake, while accumulation in other organs was insignificant. Dosimetric results showed that all tissues received almost insignificant absorbed doses in comparison with bone tissues.

Conclusion: Based on the obtained results, this radiopharmaceutical can be a good candidate for bone pain palliation therapy in skeletal metastases.

Keywords: Bone pain palliation; Dosimetry; Lu-177; TTHMP.

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Figures

Figure 1
Figure 1
The chemical structure of TTHMP
Figure 2
Figure 2
Effect of pH variation on complexation yield of 177Lu-TTHMP at room temperature
Figure 3
Figure 3
(a) ITLC chromatograms of 177LuCl3 solution, and (b) 177Lu-TTHMP in a NH4OH: MeOH: H2O (0.2:2:4) solution, using Whatman 3 MM
Figure 4
Figure 4
Biodistribution of 177Lu-TTHMP in different organs of wild-type rats
Figure 5
Figure 5
The clearance curves of each organ of rats
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