Treatment of painful bone metastases in prostate and breast cancer patients with the therapeutic radiopharmaceutical rhenium-188-HEDP

Lange, Rogier; Overbeek, Floor; Klerk, John M. H. de; Jong, P.C.M. Pasker-de; Berk, A. M. van den; Heine, Rob ter; Rodenburg, C. J.; Kooistra, A.; Hendrikse, N. Harry; Bloemendal, Haiko J.

doi:10.3413/nukmed-0828-16-05

Cited by 30 publications

(9 citation statements)

References 36 publications

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“…Additionally, the short physical half-life of 188 Re ( T 1/2 = 16.9 h) is an important property for repeated treatment 32 . 188 Re-HEDP has been applied for pain relief therapy of bone metastases secondary to breast cancer and prostate cancer 33 . The results of clinical trials suggest that the use of 188 Re-conjugated radiopharmaceuticals with repeated doses for cancer treatment should be feasible.…”

Section: Discussionmentioning

confidence: 99%

PEGylated liposome-encapsulated rhenium-188 radiopharmaceutical inhibits proliferation and epithelial–mesenchymal transition of human head and neck cancer cells in vivo with repeated therapy

Chang

Chen

Lin

et al. 2018

Cell Death Discovery

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Human head and neck squamous cell carcinoma (HNSCC) is usually treated with chemoradiotherapy, but the therapeutic efficacy could be hampered by intrinsic radioresistance and early relapse. Repeated administrations of rhenium-188 (188Re)-conjugated radiopharmaceutical has been reported to escalate the radiation doses for better control of advanced human cancers. Here we found that high dosage of 188Re-liposome, the liposome-encapsulated 188Re nanoparticles exhibited significant killing effects on HNSCC FaDu cells and SAS cells but not on OECM-1 cells. To investigate the biological and pharmaceutical responses of high 188Re-liposomal dosage in vivo, repeated doses of 188Re-liposome was injected into the orthotopic tumor model. FaDu cells harboring luciferase reporter genes were implanted in the buccal positions of nude mice followed by intravenous injection of 188Re-liposome. The Cerenkov luminescence imaging (CLI) was performed to demonstrate an increased accumulation of 188Re-liposome in the tumor lesion of nude mice with repeated doses compared to a single dose. Repeated doses also enhanced tumor growth delay and elongated the survival of tumor-bearing mice. These observations were associated with significant loss of Ki-67 proliferative marker and epithelial–mesenchymal transition (EMT) markers in excised tumor cells. The body weights of mice were not significantly changed using different doses of 188Re-liposome, yet repeated doses led to lower blood counts than a single dose. Furthermore, the pharmacokinetic analysis showed that the internal circulation of repeated 188Re-liposomal therapy was elongated. The biodistribution analysis also demonstrated that accumulations of 188Re-liposome in tumor lesions and bone marrow were increased using repeated doses. The absorbed dose of repeated doses over a single dose was about twofold estimated for a 1 g tumor. Together, these data suggest that the radiopharmacotherapy of 188Re-liposome can enhance tumor suppression, survival extension, and internal circulation without acute toxicity using repeated administrations.

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Section: Discussionmentioning

confidence: 99%

PEGylated liposome-encapsulated rhenium-188 radiopharmaceutical inhibits proliferation and epithelial–mesenchymal transition of human head and neck cancer cells in vivo with repeated therapy

Chang

Chen

Lin

et al. 2018

Cell Death Discovery

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“…Results were not detailed according to the primary tumor (Figure 4). Lange et al specifically studied the impact on quality of life, proving the routine clinical benefit of 188 Re-HEDP therapy (106). A small study by Sabet et al on 6 patients, failed to demonstrate the usefulness of salvage therapy with 188 Re-HEDP for patients with progressive bone metastases after 177 Lu-octreotate therapy (107).…”

Section: Re-labeled Small Moleculesmentioning

confidence: 99%

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

et al. 2019

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Rhenium-188 ( 188 Re) is a high energy beta-emitting radioisotope with a short 16.9 h physical half-life, which has been shown to be a very attractive candidate for use in therapeutic nuclear medicine. The high beta emission has an average energy of 784 keV and a maximum energy of 2.12 MeV, sufficient to penetrate and destroy targeted abnormal tissues. In addition, the low-abundant gamma emission of 155 keV (15%) is efficient for imaging and for dosimetric calculations. These key characteristics identify 188 Re as an important therapeutic radioisotope for routine clinical use. Moreover, the highly reproducible on-demand availability of 188 Re from the 188 W/ 188 Re generator system is an important feature and permits installation in hospital-based or central radiopharmacies for cost-effective availability of no-carrier-added (NCA) 188 Re. Rhenium-188 and technetium-99 m exhibit similar chemical properties and represent a “theranostic pair.” Thus, preparation and targeting of 188 Re agents for therapy is similar to imaging agents prepared with 99m Tc, the most commonly used diagnostic radionuclide. Over the last three decades, radiopharmaceuticals based on 188 Re-labeled small molecules, including peptides, antibodies, Lipiodol and particulates have been reported. The successful application of these 188 Re-labeled therapeutic radiopharmaceuticals has been reported in multiple early phase clinical trials for the management of various primary tumors, bone metastasis, rheumatoid arthritis, and endocoronary interventions. This article reviews the use of 188 Re-radiopharmaceuticals which have been investigated in patients for cancer treatment, demonstrating that 188 Re represents a cost effective alternative for routine clinical use in comparison to more expensive and/or less readily available therapeutic radioisotopes.

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“…The response rate of 70–80% has been reported in painful bone metastases in various malignancies [ 90 , 91 , 92 , 93 , 94 ]. In addition, an increase in Karnofsky performance score and improved quality of life have been noticed after treatment with [ 188 Re]Re–HEDP [ 28 , 93 , 94 , 95 ]. Generally, serious hematological side-effects are not expected [ 92 , 95 , 96 ].…”

Section: [188 Re]rhenium-hydroxyethylidene Diphosphonate ([ mentioning

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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Treatment of painful bone metastases in prostate and breast cancer patients with the therapeutic radiopharmaceutical rhenium-188-HEDP

Abstract: The clinically relevant response on pain and quality of life and the limited adverse events prove clinical benefit of treatment with (188)Re-HEDP and support its use in routine clinical care. Its effectiveness appears comparable to that of external beam radiotherapy.

Cited by 30 publications

References 36 publications

PEGylated liposome-encapsulated rhenium-188 radiopharmaceutical inhibits proliferation and epithelial–mesenchymal transition of human head and neck cancer cells in vivo with repeated therapy

PEGylated liposome-encapsulated rhenium-188 radiopharmaceutical inhibits proliferation and epithelial–mesenchymal transition of human head and neck cancer cells in vivo with repeated therapy

Rhenium-188 Labeled Radiopharmaceuticals: Current Clinical Applications in Oncology and Promising Perspectives

Targeted Palliative Radionuclide Therapy for Metastatic Bone Pain

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