Preparation of 166Dy/166Ho-EDTMP: a potential in vivo generator system for bone marrow ablation

Pedraza-López, Martha; Ferro-Flores, Guillermina; Murphy, Consuelo Arteaga de; Tendilla, J. I.; Villanueva-Sanchez, Octavio

doi:10.1097/01.mnm.0000126516.57329.07

Cited by 17 publications

(6 citation statements)

References 8 publications

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“…As a comparable 166 Ho bone pain palliation agent, 166 Ho-EDTMP has been proposed as a potential clinically used radiopharmaceutical by different groups [7,10]. A low liver uptake has been reported for 166 Ho-EDTMP which is considered a disadvantage as a bone pain palliative agent leading to less unwanted liver dose in patients (Fig.…”

Section: Biodistribution Of 166 Ho Cation and 166 Ho-pmd In Wild-typementioning

confidence: 96%

“…The use of bisphosphonates has made a significant change in the therapeutic approach to management of bone metastasis and pain prevention in breast cancer and multiple myeloma [4]. Various therapeutic 166 Ho bone-seeking agents have been reported such as 166 Ho-DOTMP [5,6], 166 Ho-EDTMP [7,8], 166 Ho-AP-DDMP [9], as well as 166 Dy/ 166 Ho-EDTMP demonstrating adequate properties as a stable in vivo generator system for bone marrow ablation [10].…”

Section: Introductionmentioning

confidence: 99%

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Development of 166Ho-pamidronate for bone pain palliation therapy

Fakhari

Jalilian²,

Yousefnia³

et al. 2014

J Radioanal Nucl Chem

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Section: Biodistribution Of 166 Ho Cation and 166 Ho-pmd In Wild-typementioning

confidence: 96%

Section: Introductionmentioning

confidence: 99%

Development of 166Ho-pamidronate for bone pain palliation therapy

Fakhari

Jalilian²,

Yousefnia³

et al. 2014

J Radioanal Nucl Chem

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“…Different phosphonate complexes have been labelled with [ 166 Ho]holmium targeting bone and bone marrow lesions [ 111 , 112 , 113 , 114 ]. [ 166 Ho]holmium is an inexpensive β¯-emitter, majorly used in the treatment of multiple myeloma [ 112 , 115 ].…”

Section: [166 Ho]holmium-ethylene Diamine Tetramethylene Phosphonmentioning

confidence: 99%

“…In a pilot study, [ 166 Ho]Ho–DOTMP was used for the treatment of bone metastases in breast cancer patients showing median time to progression of 10.4 months [ 118 ]. In addition, owing to the remarkably higher radiation dose to the bone marrow, combination of [ 166 Dy]dysprosium/[ 166 Ho]Ho-EDTMP is proposed as an agent for bone marrow ablation [ 113 ].…”

Section: [166 Ho]holmium-ethylene Diamine Tetramethylene Phosphonmentioning

confidence: 99%

Targeted Palliative Radionuclide Therapy for Metastatic Bone Pain

Manafi‐Farid

Masoumi

Divband

et al. 2020

JCM

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Bone metastasis develops in multiple malignancies with a wide range of incidence. The presence of multiple bone metastases, leading to a multitude of complications and poorer prognosis. The corresponding refractory bone pain is still a challenging issue managed through multidisciplinary approaches to enhance the quality of life. Radiopharmaceuticals are mainly used in the latest courses of the disease. Bone-pain palliation with easy-to-administer radionuclides offers advantages, including simultaneous treatment of multiple metastatic foci, the repeatability and also the combination with other therapies. Several β¯- and α-emitters as well as pharmaceuticals, from the very first [89Sr]strontium-dichloride to recently introduced [223Ra]radium-dichloride, are investigated to identify an optimum agent. In addition, the combination of bone-seeking radiopharmaceuticals with chemotherapy or radiotherapy has been employed to enhance the outcome. Radiopharmaceuticals demonstrate an acceptable response rate in pain relief. Nevertheless, survival benefits have been documented in only a limited number of studies. In this review, we provide an overview of bone-seeking radiopharmaceuticals used for bone-pain palliation, their effectiveness and toxicity, as well as the results of the combination with other therapies. Bone-pain palliation with radiopharmaceuticals has been employed for eight decades. However, there are still new aspects yet to be established.

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“…Animal studies showed a fast blood clearance of [ 166 Dy]Dy/[ 166 Ho]Ho EDTMP and a skeletal uptake of 22.32 ± 1.86% ID/g at 2 h and 20.12 ± 1.94% ID/g after 10 days. Theoretical bone marrow absorbed dose calculations indicate that the [ 166 Dy]Dy/[ 166 Ho]Ho EDTMP in vivo generator system produced 3.47 times more dose than [ 166 Ho]Ho DOTMP per unit of initial activity in the skeleton (Pedraza-Lopez et al 2004a). The same group also demonstrated that the [ 166 Dy]Dy/[ 166 Ho]Ho EDTMP system induced considerable cytotoxicity, genotoxicity and severe myelosuppression in mice at bone marrow absorbed doses of 18–23 Gy, suggesting that this system could potentially be a good agent for use in humans (Pedraza-Lopez et al 2004b).…”

Section: Intravenous Applicationsmentioning

confidence: 99%

The various therapeutic applications of the medical isotope holmium-166: a narrative review

Klaassen¹,

Arntz²,

Arranja

et al. 2019

EJNMMI radiopharm. chem.

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Over the years, a broad spectrum of applications of the radionuclide holmium-166 as a medical isotope has been established. The isotope holmium-166 is attractive as it emits high-energy beta radiation which can be used for a therapeutic effect and gamma radiation which can be used for nuclear imaging purposes. Furthermore, holmium-165 can be visualized by MRI because of its paramagnetic properties and by CT because of its high density. Since holmium-165 has a natural abundance of 100%, the only by-product is metastable holmium-166 and no costly chemical purification steps are necessary for production of nuclear reactor derived holmium-166. Several compounds labelled with holmium-166 are now used in patients, such Ho 166 -labelled microspheres for liver malignancies, Ho 166 -labelled chitosan for hepatocellular carcinoma (HCC) and [ 166 Ho]Ho DOTMP for bone metastases. The outcomes in patients are very promising, making this isotope more and more interesting for applications in interventional oncology. Both drugs as well as medical devices labelled with radioactive holmium are used for internal radiotherapy. One of the treatment possibilities is direct intratumoural treatment, in which the radioactive compound is injected with a needle directly into the tumour. Numerous other applications have been developed, like patches for treatment of skin cancer and holmium labelled antibodies and peptides. The second major application that is currently clinically applied is selective internal radiation therapy (SIRT, also called radioembolization), a novel treatment option for liver malignancies. This review discusses medical drugs and medical devices based on the therapeutic radionuclide holmium-166.

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Preparation of 166Dy/166Ho-EDTMP: a potential in vivo generator system for bone marrow ablation

Abstract: The prepared radiolabelled EDTMP has adequate properties as a stable in vivo generator system for bone marrow ablation.

Cited by 17 publications

References 8 publications

Development of 166Ho-pamidronate for bone pain palliation therapy

Development of 166Ho-pamidronate for bone pain palliation therapy

Targeted Palliative Radionuclide Therapy for Metastatic Bone Pain

The various therapeutic applications of the medical isotope holmium-166: a narrative review

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