Production, quality control and pharmacokinetic studies of 177Lu–zoledronate for bone pain palliation therapy

Radiolabeling, quality control, biodistribution, and imaging studies of 177Lu‐ibandronate

“…Finally, TLC technique was used to analyze radiochemical purity. A mixture of NH 4 OH (25.28%)/MeOH (100%)/H 2 O (1:5:9.5 v / v / v ) was used for the eluting solvent …”

Development of 166Ho-pamidronate for bone pain palliation therapy

“…The protein binding for the PMD ligand has been reported in different references from 54 % in free form [12], however no protein biding for metal PMD complexes were available in the literature.…”

“…The search for the development of new ligands with higher stability, better pharmacokinetics properties and lower unwanted tissue uptakes (liver and GI) is still ongoing [11].…”

“…Considering the inhibitory binding affinity constant (Ki) of bisphosphonates used in clinics including etidronate (Ki: 91 lM), ibandronate (116 lM), pamidronate (83 lM), risedronate (85 lM) and zoledronate (81 lM), the idea 66 of developing bone avid agents based on these ligands is of great interest, however in one study with 177 Lu-zoledronate, the resulting complex was not stable in vivo compared to other therapeutic bisphosphonates due to the existence an imidazole ring [12]. Thus another interesting ligand based on affinity constants was considered pamidronic acid while containing an amino group which possibly could increase the complex stability.…”

Chelating agents for radiolanthanides: Applications to imaging and therapy

“…The complex showed good bone uptake in rat studies, but was not superior to the performance of 177 Lu-EDTMP. 53 Interestingly, the combined use of zoledronic acid and 153 Sm-EDTMP has been investigated in hormone-refractory prostate cancer patients with bone metastases. 54 In terms of the Ln(III) coordination chemistry, there do not appear to be any specific reports on the structural properties of zoledronate complexes.…”