Bone seeking radiopharmaceuticals

Ligny, C.L. De; Gelsema, W.J.; Tji, T.G.; Huigen, Y.M.; Vink, Henk A.

doi:10.1016/0883-2897(90)90144-p

Cited by 29 publications

(34 citation statements)

References 65 publications

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“…177 Lu with considerable characteristics has been recognized as one of the most promising radionuclides. The significant advantage of using 177 Lu is its b -particle energies which are adequately low, therefore the bone marrow suppression is minimum when it accumulates in skeletal lesions [20]. On the other hand, 177 Lu can be produced with high specific activity via the indirect method by neutron irradiation of 176 Yb.…”

Section: Discussionmentioning

confidence: 99%

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Yousefnia

Zolghadri

Sadeghi

et al. 2015

J Radioanal Nucl Chem

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In this study, 177 Lu-(4-{[(bis(phosphonomethyl))-carbamoyl]methyl}-7,10-bis(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid ( 177 Lu-BPAMD) was successfully prepared. The quality control, partition coefficient, hydroxyapatite binding assay and stability of the complex were determined. For better comparison, biodistribution patterns of 177 Lu-BPAMD and 177 Lu-EDTMP complexes were compared in same animal model. 177 Lu-BPAMD was prepared with high radiochemical purity ([93 %) and specific activity of 534 GBq/mmol at the optimal conditions. Comparative study between 177 Lu-BPAMD and 177 Lu-EDTMP indicated higher bone uptake and lesser accumulation in the other organs for 177 Lu-BPAMD. 177 Lu-BPAMD can be considered as a promising agent for bone pain palliation in the near future.

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Section: Discussionmentioning

confidence: 99%

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Yousefnia

Zolghadri

Sadeghi

et al. 2015

J Radioanal Nucl Chem

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“…The high bone affinity of BPs is due to their common diphosphonate moiety, { 2 ( 2 HO)(O)P-C-P(O)-(OH 2 ) 2 }, whereas the varying pharmacological activity of the BPs is due to different chemical moieties attached to the central C-atom of BPs. The high bone-affinity of BPs was initially utilized to target radioactive metal ions, such as technetium (3,4), to bone for diagnostic and therapeutic purposes. The BPs typically bind to metal ions through electrostatic interactions and deliver the radioactive ion to bone sites.…”

Section: Introductionmentioning

confidence: 99%

Targeting Systemically Administered Proteins to Bone by Bisphosphonate Conjugation

Uludağ

Yang

2002

Biotechnology Progress

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To develop a methodology for bone-specific delivery of proteins, a bone-seeking aminobisphosphonate (aminoBP) was previously conjugated to a model protein, bovine serum albumin (BSA). The conjugates were shown to exhibit a high affinity to bone in vitro and in vivo. This study was conducted to determine whether the systemic delivery of proteins to bone can be increased by aminoBP conjugation. Two model proteins used for this study were BSA and lysozyme (LYZ). For each protein, an unmodified (i.e., control) and aminoBP-conjugated protein were (125)I-labeled and injected into rats, and the organ delivery of the proteins were determined. Intravenous (IV) injection of aminoBP-BSA resulted in a 2.0- to 3.7-fold increased delivery to bones as compared to the control protein in young rats. In osteopenic, ovariectomized rats, aminoBP conjugation enhanced the bone delivery of BSA by 2.2- to 7.5-fold. A 3.7- to 5.6-fold increased delivery was also observed for LYZ after IV injection in normal rats. In addition to IV route of administration, subcutaneous injection was also effective in delivering a higher amount of aminoBP-conjugated proteins to bone. We conclude that conjugating bone-seeking aminoBPs to proteins improved their delivery to mineralized tissues. The proposed targeting approach has the potential to improve the efficacy of recombinant proteins capable of stimulating bone formation by enhancing their localization to bones.

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“…177 Lu with considerable characteristics has been recognized as one of the most promising radionuclides. The significant advantage of using 177 Lu is its β -particle energies which are adequately low; therefore the bone marrow suppression is minimum when it accumulates in skeletal lesions (Deligny et al, 1990). However, different complexes of 177 Lu with bisphosphonates have been developed; the only clinically used Lu-177 bone pain palliation therapeutic agent is 177 Lu-EDTMP.…”

Section: Dosimetric Studiesmentioning

confidence: 99%

“…177 Lu with considerable characteristics [t 1/2 =6.73 d, E βmax = 497 MeV, Eγ=112 keV (6.4%), 208 keV (11%)] has been recognized as one of the most promising radionuclides. The significant advantage of using 177 Lu is its  -particle energies which are adequately low, therefore the bone marrow suppression is minimum when it accumulates in skeletal lesions (Deligny et al 1990). …”

Section: Introductionmentioning

confidence: 98%

Estimated human absorbed dose of 177Lu–BPAMD based on mice data: Comparison with 177Lu–EDTMP

Yousefnia

Zolghadri

Shanehsazzadeh

2015

Applied Radiation and Isotopes

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Bone seeking radiopharmaceuticals

Cited by 29 publications

References 65 publications

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Preparation and biological assessment of 177Lu-BPAMD as a high potential agent for bone pain palliation therapy: comparison with 177Lu-EDTMP

Targeting Systemically Administered Proteins to Bone by Bisphosphonate Conjugation

Estimated human absorbed dose of 177Lu–BPAMD based on mice data: Comparison with 177Lu–EDTMP

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