Iodine-131-labeled diphosphonates for the palliative treatment of bone metastases—III. Considerations of interaction, binding and absorbed dose

Eisenhut, Michael; Fritz, P.; Kimmig, B.; Wingen, F.; Krempien, B.

doi:10.1016/0883-2889(86)90269-8

Cited by 8 publications

(3 citation statements)

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“…The various radiopharmaceuticals that are used for palliative treatment of bone metastases include strontium-89 (Pecher, 1942) phosphorus-32 (Friedell and Storaassli, 1950), iodine-131-BDP3 (Eisenhut et al, 1986), yttrium-90 (Kutzner et al, 1991), rhenium-186-HEDP (Maxon et al, 1990) and samarium-153-EDTMP (Turner et al, 1989). More recently, tin-17m-DTPA (Atkins et al, 1995) rhenium-188-HEDP (Palmedo et al, 2000 and rhenium-188-DMSA (Blower et al, 2000) have been reported to be effective for bone pain palliation.…”

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confidence: 99%

Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

et al. 2003

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Rhenium-188-HEDP (Re generator, it is convenient for clinical therapeutic use with a short physical half-life of 16.9 h and a maximal b-energy of 2.1 MeV. We investigated the effect of 188 Re-HEDP on pain relief, analgesic intake and impairment of bone marrow function in 27 patients with bone metastases induced from prostate cancer. All patients were interviewed using a standardised set of questions before, and after therapy for 12 weeks. The patients were treated with 2700 -3459 MBq of 188 Re-HEDP. Blood samples were taken weekly for 12 weeks, and a blood count was performed. Patients described an improvement on the Karnofsky performance scale from 7477 to 8579% 12 weeks after therapy (P ¼ 0.001). The pain score showed a maximum decrease from 44718 to 27720% in the third to the eight week after therapy (P ¼ 0.009). Seventy-six percent of the patients described a pain relief without increase of analgesic intake. Twenty percent of the patients could discontinue their analgesics and were pain free. Mean platelet count decreased from (286775) * 10 3 ml À1 to (215792) * 10 3 ml À1, and mean leucocyte count from (7.771.5) * 10 3 ml À1 to (6.071.9) * 10 3 ml À1 in the second to the fourth week after therapy. The maximal differences between the values of platelets and leucocytes before and after therapy were not statistically significant (P ¼ 0.021 and 0.094). In conclusion, 188Re-HEDP is an effective radiopharmaceutical used in the palliative treatment of metastatic bone pain in prostate cancer and shows minimal bone marrow toxicity.

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Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

et al. 2003

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“…Because this new labelled BP is taken up also by osteoclasts, it may be very interesting to monitor osteoclastic lesions. Drug delivery systems based on avidity of BPs to hydroxyapatite have been also envisaged [12][13][14] especially for the treatment of patient with inoperable osteosarcoma [15]. Fig.…”

Section: Imaging Of Osteoblastic Bone Tumours By Modified Bisphosphonmentioning

confidence: 99%

Therapeutic Approach of Primary Bone Tumours by Bisphosphonates

Moriceau¹,

Ory²,

Gobin³

et al. 2010

CPD

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Bone tumours can be dissociated in two main categories: i) primary bone tumours (benign or malignant) including mainly osteosarcoma and other sarcomas.ii)and giant cell tumour and bone metastases originate from others cancer (Breast, prostate, kidney cancer, etc). These tumours are able to destroy or/and induce a new calcified matrix. However, the first step of bone tumour development is associated with an induction of bone resorption and the establishment of a vicious cycle between the osteoclasts and the tumour growth. Indeed, bone resorption contributes to the pathogenesis of bone tumour by the release of cytokines (IL6, TNFα) which govern the bone tumour's development and which are trapped into the bone matrix. Bisphosphonates (BPs) are chemical compounds of P-C-P structure with a high affinity for bone hydroxyapatite crystals. Thus, they have been used as a carrier for radio nucleotides to develop novel approaches of bone imaging. BPs exert also indirect anti-tumour activities in vivo. Indeed, BPs directly interfere with the bone microenvironment and target osteoclasts, endothelial cells and immune cells (tumour-associated macrophages, γ9δ2 T cells). BPs induce tumour cell death in vitro and same activity is suspected in vivo. The present review summarizes the mechanisms of actions of BPs as well as their clinical interests in bone primary tumours.

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“…Eisenhut was first to report the potential use of 131 I-labeled bisphosphonates for palliative treatment of bone-related cancer. , In these studies, several benzylidenebisphosphonates ( 5 , Chart ) were synthesized and evaluated. The bone affinity and selectivity of the compounds were found to be comparable to that of other bone-seeking radiopharmaceuticals; however, because of their low in vivo stability these compounds have not been used clinically.…”

Section: Introductionmentioning

confidence: 99%

Studies on the Synthesis and Biological Properties of Non-Carrier-Added [¹²⁵I and ¹³¹I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions

et al. 2003

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Arylalkylidenebisphosphonates labeled with nca [(125)I or (131)I] have been synthesized and their biological function investigated. The label was attached to the aromatic group in high yield and under mild conditions by means of iododesilylation. The bone affinities of the radioactive compounds were investigated in normal Balb/C mice. The compound 1-hydroxy(m-iodo[(125,131)I]-phenylethylidene)-1,1-bisphosphonate was found to possess superior bone affinity compared to others, and its in vivo deiodination was insignificant. The uptake in femur 24h after injection was 850 +/- 265% and 986 +/- 118% of injected dose per gram tissue times gram body weight in mice and rats, respectively. The therapeutic potential of the compound was investigated in two tumor models in athymic (nude) rats, one model for mixed lytic/sclerotic metastatic bone-lesions originating from breast cancer and the other model simulating osseous osteosarcoma. The effects in these models compare favorably to those observed for established treatment modalities. The experiments demonstrate that radioiodinated bisphosphonates may have a potential for diagnosis and therapy of malignant osseous lesions.

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Iodine-131-labeled diphosphonates for the palliative treatment of bone metastases—III. Considerations of interaction, binding and absorbed dose

Cited by 8 publications

References 2 publications

Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

Therapeutic Approach of Primary Bone Tumours by Bisphosphonates

Studies on the Synthesis and Biological Properties of Non-Carrier-Added [¹²⁵I and ¹³¹I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions

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Iodine-131-labeled diphosphonates for the palliative treatment of bone metastases—III. Considerations of interaction, binding and absorbed dose

Cited by 8 publications

References 2 publications

Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

Therapeutic efficiency of rhenium-188-HEDP in human prostate cancer skeletal metastases

Therapeutic Approach of Primary Bone Tumours by Bisphosphonates

Studies on the Synthesis and Biological Properties of Non-Carrier-Added [125I and 131I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions

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Studies on the Synthesis and Biological Properties of Non-Carrier-Added [¹²⁵I and ¹³¹I]-Labeled Arylalkylidenebisphosphonates: Potent Bone-Seekers for Diagnosis and Therapy of Malignant Osseous Lesions