31 results match your criteria radiolabelled bisphosphonates


Imaging with radiolabelled bisphosphonates.

Authors:
Gary J R Cook

Bone 2020 08 28;137:115372. Epub 2020 Apr 28.

Department of Cancer Imaging, School of Biomedical Engineering and Imaging Sciences, King's College London, London, UK. Electronic address:

Radiolabeled bisphosphonates were developed in the 1970s for scintigraphic functional imaging of the skeleton in benign and malignant disease. Tracers such as Tc-methylene diphosphonate, that map focal or global changes in mineralization in the skeleton qualitatively and quantitatively, have been the backbone of nuclear medicine imaging for decades. While competing technologies are evolving, new indications and improvements in scanner hardware, in particular hybrid imaging (e. Read More

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Organ Biodistribution of Radiolabelled γδ T Cells Following Liposomal Alendronate Administration in Different Mouse Tumour Models.

Nanotheranostics 2020 6;4(2):71-82. Epub 2020 Feb 6.

School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, United Kingdom.

Vγ9Vδ2 T cell immunotherapy has been shown to be effective in delaying tumour growth in both pre-clinical and clinical studies. It has been pointed out the importance of the ability of cells to accumulate within tumours and the association with therapeutic efficacy in clinical studies of adoptive T cell transfer. We have previously reported that alendronate liposomes (L-ALD) increase the efficacy of this therapy after localised or systemic injection of γδ T cells in mice, inoculated with ovarian, melanoma, pancreatic or experimental lung metastasis tumour models, respectively. Read More

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Dual-radiolabelling of an injectable hyaluronan-tyramine-bisphosphonate hybrid gel for in vitro and in vivo tracking.

Carbohydr Polym 2020 Mar 21;231:115652. Epub 2019 Nov 21.

Institute of Nuclear Physics and Chemistry, China Academy of Engineering Physics, 621900, Mianyang, PR China; Collaborative Innovation Center of Radiation Medicine of Jiangsu, Higher Education Institutions, 215123, Suzhou, PR China; Key Laboratory of Nuclear Medicine and Molecular Imaging of Sichuan Province, 621999, Mianyang, PR China. Electronic address:

Hyaluronan (HA) have been widely used as the ideal biomaterials. It is important to understand their degradation and distribution for better optimization. From a new aspect of using radiotracers, we designed the HA-tyramine-bisphosphonate derivative for dual-labelling with two radionuclides (Tc and I) simultaneously for in vitro and in vivo tracking. Read More

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Evaluation of the inverse electron demand Diels-Alder reaction in rats using a scandium-44-labelled tetrazine for pretargeted PET imaging.

EJNMMI Res 2019 May 28;9(1):49. Epub 2019 May 28.

Department of Clinical Physiology, Nuclear Medicine & PET, Rigshospitalet, Blegdamsvej 9, 2100, Copenhagen, Denmark.

Background: Pretargeted imaging allows the use of short-lived radionuclides when imaging the accumulation of slow clearing targeting agents such as antibodies. The biotin-(strept)avidin and the bispecific antibody-hapten interactions have been applied in clinical pretargeting studies; unfortunately, these systems led to immunogenic responses in patients. The inverse electron demand Diels-Alder (IEDDA) reaction between a radiolabelled tetrazine (Tz) and a trans-cyclooctene (TCO)-functionalized targeting vector is a promising alternative for clinical pretargeted imaging due to its fast reaction kinetics. Read More

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Optimized Production and Biological Evaluation of Ga-PDTMP as a New Agent for PET Bone Scanning.

J Med Imaging Radiat Sci 2019 Mar 15;50(1):142-148. Epub 2018 Nov 15.

Energy Engineering and Department of Physics, Amir Kabir, University of Technology, Tehran, Iran.

Introduction: In this study, Ga-PDTMP was introduced as a novel agent for PET bone scanning.

Methods: Ga-PDTMP was prepared with radiochemical purity of higher than 98% at the optimized conditions.

Results: Stability tests showed no decrease in radiochemical purity, even after 120 min. Read More

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Evaluation of [Ac]Ac-DOTA for α-Therapy of Bone Metastases.

Curr Radiopharm 2018 ;11(3):223-230

Institute of Nuclear Chemistry, Johannes Gutenberg University, Mainz, Germany.

Background: Conjugates of bisphosphonates with macrocyclic chelators possess high potential in bone targeted radionuclide imaging and therapy. DOTAZOL, zoledronic acid conjugated to DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), demonstrated promising results in vivo in small animals as well as in first patient applications using 68Ga for diagnosis via PET and the lowenergy β-emitter 177Lu for therapy of painful bone metastases. In consideration of the fact that targeted α-therapy probably offers various advantages over the use of β--emitters, the 225Ac-labelled derivative [225Ac]Ac-DOTAZOL was synthesized and evaluated in vivo. Read More

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January 2019

The value of 99mTc-MDP bone SPECT/CT in evaluation of patients with painful knee prosthesis.

Nucl Med Commun 2018 May;39(5):397-404

Department of Nuclear Medicine, Guy's and St Thomas' NHS Foundation Trust.

Objective: The purpose of this study was to assess the incremental value of technetium-99m-methyl diphosphonate (Tc-MDP) single-photon emission computed tomography/computed tomography (SPECT/CT) over Tc-MDP two-phase bone scan (TPBS) in the assessment of the patients with pain following knee arthroplasty.

Patients And Methods: Tc-MDP TPBS and Tc-MDP SPECT/CT were performed in 49 patients with knee pain after knee arthroplasty. The scans were reviewed by two readers (nuclear medicine physician and musculoskeletal radiologist). Read More

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Suitability of liposomal carriers for systemic delivery of risedronate using the pulmonary route.

Drug Deliv 2013 Nov 30;20(8):311-8. Epub 2013 Sep 30.

Faculty of Pharmacy, Ain Shams University, Pharmaceutics and Industrial Pharmacy , Cairo , Egypt and.

Objective: This study aims at testing the hypothesis that reversed phase evaporation liposomes (REVs) are suitable for systemic delivery of an anti-osteporotic drug (risedronate sodium (RS)) via pulmonary nebulization.

Materials And Methods: RS REVs were prepared using phospholipids and cholesterol with or without stearylamine, and were characterized for morphology, entrapment efficiency (EE%), in vitro release, particle size and aerosolization behavior from an actively vibrating mesh nebulizer. RS accumulation in rat bones following intra-tracheal administration of the selected formulation was assessed using a radiolabelling-based technique, and histological examination of rat lung tissue was performed to assess its safety. Read More

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November 2013

Bone scan in metabolic bone diseases. Review.

Nucl Med Rev Cent East Eur 2012 Aug 25;15(2):124-31. Epub 2012 Aug 25.

Department of Nuclear Medicine Medical University of Bialystok, Poland.

Metabolic bone disease encompasses a number of disorders that tend to present a generalized involvement of the whole skeleton. The disorders are mostly related to increased bone turnover and increased uptake of radiolabelled diphosphonate. Skeletal uptake of 99mTc-labelled diphosphonate depends primarily upon osteoblastic activity, and to a lesser extent, skeletal vascularity. Read More

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Design and synthesis of novel bone-targeting dual-action pro-drugs for the treatment and reversal of osteoporosis.

Bioorg Med Chem 2012 Mar 31;20(6):2131-40. Epub 2012 Jan 31.

Department of Chemistry, Simon Fraser University, Burnaby, British Columbia, Canada V5A 1S6.

There is an important medical need for effective therapies to redress the general bone loss associated with advanced osteoporosis. Prostaglandin E(2) and related EP4 receptor agonists have been shown to stimulate bone regrowth but their use has been limited by systemic side effects. Herein is described the design and synthesis of novel dual-action bone-targeting conjugate pro-drugs where two classes of active agents, a bone growth stimulating prostaglandin E(2) EP4 receptor subtype agonist (5 or 6) and a bone resorption inhibitor bisphosphonate, alendronic acid (1), are coupled using metabolically labile carbamate or 4-hydroxyphenylacetic acid based linkers. Read More

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[Systemic therapy approaches in patients with bone metastases of urogenital malignancies].

Urologe A 2007 Aug;46(8):904, 906-12

Klinik für Urologie und Kinderurologie, Universitätsklinikum Ulm, 89075, Ulm.

Bone metastases develop commonly in patients with a variety of urogenital malignancies and are a major cause of morbidity and diminished quality of life in a significant proportion of urogenital carcinoma patients. For example, bone metastases occur in approximately 80% of patients with hormone-refractory prostate cancer and in approximately 25% of patients with renal cell carcinoma. A sufficient and early therapy is crucial since adequate therapy can lead to significant improvements in pain control and function and maintain skeletal integrity. Read More

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Uptake of bone-seekers is solely associated with mineralisation! A study with 99mTc-MDP, 153Sm-EDTMP and 18F-fluoride on osteoblasts.

Eur J Nucl Med Mol Imaging 2006 Apr 17;33(4):491-4. Epub 2006 Jan 17.

Department of Nuclear Medicine, Medical University of Vienna, AKH Wien, Waehringer Guertel 18-20, 1090 Vienna, Austria.

Purpose: Although polyphosphonates (PPs) were introduced as bone imaging agents in nuclear medicine in the early 1970s, the mechanisms involved in their uptake still remain unclear. Suggested mechanisms range from mineral adsorption with disputed binding to the organic phase, over incorporation into the mineralisation process to a combination of both mechanisms. Thus, our investigations aimed to: (1) evaluate adsorption parameters of (99m)Tc-MDP, (153)Sm-EDTMP and (18)F-fluoride on mineralising osteoblast cultures, (2) correlate the radiotracer binding measured in the cell cultures with binding values from our previously presented mineral model and (3) compare binding with cell number. Read More

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Determination of inflammation of reflex sympathetic dystrophy at early stages with Tc-99m HIG scintigraphy: preliminary results.

Rheumatol Int 2006 Mar 16;26(5):404-8. Epub 2005 Jul 16.

Department of Nuclear Medicine, Ankara Numune Research and Training Hospital, Ankara, Turkey.

The pathogenesis of reflex sympathetic dystrophy (RSD) is not completely understood. However, an excessive regional inflammation, sensitization of primary somatosensory afferents, and sensitization of spinal neurons are considered to have a role in the pathogenesis of RSD. The underlying pathophysiology relating the clinical picture may help to determine the pharmacotherapeutic approach for an individual patient. Read More

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Binding studies of [(18)F]-fluoride and polyphosphonates radiolabelled with [(111)In], [(99m)Tc], [(153)Sm], and [(188)Re] on bone compartments: a new model for the pre vivo evaluation of bone seekers?

Bone 2004 May;34(5):835-44

Department of Nuclear Medicine, Medical University of Vienna, Vienna, Austria.

Introduction: Although the first polyphosphonates were already introduced in the early 1970s, mechanisms involved in uptake still remain speculative. The present work aimed to establish a new method to rate the influence of various factors on the uptake and to evaluate new bone-seekers on these bone compartments.

Methods: Radioactive-labelled diphosphonates and [(18)F]-fluoride were added to a vial containing hydroxyapatite (HA), collagen, or amorphous calcium phosphate (ACP) in 3 ml of Hanks' Balanced Salt Solution (HBSS). Read More

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Scintigraphy using a technetium 99m-labelled anti-E-selectin Fab fragment in rheumatoid arthritis.

Rheumatology (Oxford) 2002 Jan;41(1):53-61

Centre of Nuclear Medicine, University of Louvain Medical School, Brussels, Belgium.

Objective: We previously described a novel radiolabelled monoclonal antibody (1.2B6), which reacts with porcine E-selectin, for targeting activated endothelium as a means of imaging inflammatory disorders, and presented initial clinical work based on (111)In-labelled antibody. The aim of the present study was to evaluate a Fab fragment of 1. Read More

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January 2002

Chronic post-traumatic osteomyelitis of the lower extremity: comparison of magnetic resonance imaging and combined bone scintigraphy/immunoscintigraphy with radiolabelled monoclonal antigranulocyte antibodies.

Skeletal Radiol 2000 Jul;29(7):378-86

Department of Diagnostic Radiology, University Hospital Basel, Switzerland.

Objective: A retrospective study of the validity of combined bone scintigraphy (BS) and immunoscintigraphy (IS) using (99m)Tc-labelled murine antigranulocyte antibodies (MAB) and magnetic resonance imaging (MRI) in chronic posttraumatic osteomyelitis.

Design And Patients: The results of MRI and combined BS/IS of 19 lesions in 18 patients (13 men, 5 women; mean age 45 years, range 27-65 years) were independently evaluated by two radiologists and one nuclear medicine physician with regard to bone infection activity and extent. The patient group was a highly selective collection of clinical cases: the average number of operations conducted because of relapsing infection was eight (range 2-27), the average time interval between the last surgical intervention and the present study was 6. Read More

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Pharmacokinetics of alendronate.

Clin Pharmacokinet 1999 May;36(5):315-28

Merck Research Laboratories, Clinical Pharmacology and Drug Metabolism, Rahway, New Jersey, USA.

Alendronate (alendronic acid; 4-amino-1-hydroxybutylidene bisphosphonate) has demonstrated effectiveness orally in the treatment and prevention of postmenopausal osteoporosis, corticosteroid-induced osteoporosis and Paget's disease of the bone. Its primary mechanism of action involves the inhibition of osteoclastic bone resorption. The pharmacokinetics and pharmacodynamics of alendronate must be interpreted in the context of its unique properties, which include targeting to the skeleton and incorporation into the skeletal matrix. Read More

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Effects of polyethylene on macrophages.

J Orthop Res 1997 Jan;15(1):50-6

McKay Laboratories, Department of Orthopaedic Surgery, Hospital of the University of Pennsylvania, Philadelphia, USA.

A system was developed to expose macrophages to polyethylene in vitro. Exposure of macrophages to these particles in isolation led to the release of tumor necrosis factor alpha and prostaglandin E2. Exposure of macrophages in co-culture with osteoblasts to polyethylene particles increased the release of prostaglandin E2 and also led to the release of interleukin-6. Read More

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January 1997

Disturbances of fluid balance reduce the image quality of bone scintigraphy. Experimental studies in mice.

Nucl Med Commun 1994 Jun;15(6):469-74

Department of Diagnostic Radiology, Karolinska Hospital, Stockholm, Sweden.

The effects of hydration, dehydration and osmotic diuresis on the activity distribution of bone-seeking radiopharmaceuticals have been studied in an experimental mouse system. It was found that any change of the water balance impairs the activity distribution of the radiolabelled phosphonate in the potential bone scintigraphic image. The findings suggest that in order to maintain image quality, elderly patients should not be instructed to drink a large volume of fluid after the administration of a bone-seeking radiopharmaceutical. Read More

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The effect of portal venous flow on the washout of a regionally injected marker substance 99mTc-methylene diphosphonate after hepatic arterial blockade with degradable starch microspheres.

Eur J Surg Oncol 1992 Aug;18(4):347-52

University Department of Surgery, Royal Liverpool Hospital, UK.

Patients with hepatic metastases derived from colorectal carcinoma have a poor prognosis. Regional chemotherapy, either alone, or combined with agents such as degradable starch microspheres (DSM) that reduce or abolish intrahepatic arterial flow and potentiate the delivery of cytotoxics to hepatic metastases, have not significantly improved survival. We have investigated one positive mechanism, namely the effect of portal venous washout of cytotoxics, for the poor efficacy of drugs administered either alone or in combination with DSM via the hepatic artery in the rat. Read More

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Soft-tissue localization of 99mTc-hydroxymethylene diphosphonate due to interaction with calcium.

Clin Radiol 1992 May;45(5):326-30

Radiopharmacy Unit, Bristol General Hospital.

Soft tissue localization of 99mTc-labelled bone imaging agents is often associated with high calcium levels either locally or systemically. This could be due to the formation of a large molecular complex after administration of the radiopharmaceutical. We have investigated the formation of such a complex between 99mTc-hydroxymethylene diphosphonate (HMDP) and calcium by a number of techniques. Read More

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A method of computerised isotope dynamic proctography.

Eur J Nucl Med 1992 ;19(6):431-5

Department of Surgery, Western General Hospital, Edinburgh, UK.

Patients with long-standing constipation were examined by radioisotope proctography. A radiolabelled synthetic potato mash was inserted intrarectally and the dynamic changes during simulated defaecation recorded using a gamma-camera. Computer images from the stored data illustrate changes in the anorectal angle and pelvic floor. Read More

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Clinical experience with pamidronate in the treatment of Paget's disease of bone.

Ann Rheum Dis 1991 Dec;50(12):930-3

University Department of Medicine, Glasgow Royal Infirmary, UK.

Bisphosphonates have been shown to be effective in treating the increased bone turnover associated with Paget's disease of bone. In this study two groups of patients were treated with pamidronate by intravenous infusion. In group 1 (n = 15) 30 mg of pamidronate was given once a week for six weeks. Read More

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December 1991

The effects of intra-arterial vasoconstrictors on the distribution of a radiolabelled low molecular weight marker in an experimental model of liver tumour.

Br J Cancer 1991 Apr;63(4):495-8

University Department of Surgery, Royal Infirmary, Glasgow, UK.

Regional chemotherapy for colorectal liver metastases has not demonstrated a convincing survival benefit over systemic chemotherapy. This may be due to poor delivery of chemotherapeutic drugs to hypovascular liver tumour. Since vasoactive agents may influence hepatic blood flow this study investigated the effects of systemic and regional vasoconstrictors on the delivery of a regionally delivered marker in an experimental model of liver tumour. Read More

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Radiolabelled stripped mucin, SM3, monoclonal antibody for immunoscintigraphy of ovarian tumours.

Int J Biol Markers 1990 Apr-Jun;5(2):89-96

Department of Nuclear Medicine, St. Bartholomew's Hospital, London, England.

A new monoclonal antibody, SM3, against stripped mucin core protein has been evaluated for the radioimmunoscintigraphy of ovarian cancer. It was radiolabelled with In-111, I-123 and Tc-99m and results showed a sensitivity of 95%, 100% and 100% and an accuracy of 73%, 86% and 100% for malignancy; respectively. Read More

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Relapse of osteoporosis circumscripta as a lytic ring after treatment of Paget's disease with intravenous 3-amino-1-hydroxypropylidene-1,1-bisphosphonate.

Br J Radiol 1988 Nov;61(731):996-1001

University of Manchester Department of Medicine, Hope Hospital, Salford.

Two patients with osteoporosis circumscripta of the skull are presented who have each been treated with a 3-month course of intravenous infusions of (3-amino-1-hydroxypropylidene)-1,1-bisphosphonate (APD) (total dose of 185 and 375 mg), which in both cases was associated with rapid and dramatic remineralization of the porotic bone and marked clinical and biochemical remission. However, osteolytic disease reappeared (after 9 and 18 months, respectively) in both cases as an osteolytic ring showing high uptake of radiolabelled bisphosphonate on bone scan, in formerly unaffected bone just distal to the original leading edge of osteolysis. Further treatment was associated with healing of these new lesions. Read More

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November 1988

Effect of portal blood flow and intra-arterially injected starch microspheres on the passage of a labelled tracer through the liver. An experimental study in pigs.

Acta Oncol 1987 ;26(3):217-21

Department of Oncology, University Hospital, Linköping, Sweden.

Pig liver was used to study the influence of portal blood flow and degradable starch microspheres (DSM) on the passage of radiolabelled methylene-di-phosphonate from the hepatic artery to the systemic circulation. When the portal vein was clamped abut 70 per cent of the labelled marker injected into the hepatic artery passed to the systemic circulation and the remaining 30 per cent passed when the portal vein was opened. When the flow of the hepatic artery was stopped, the portal blood flow alone drained about 65 per cent of the marker, which was given as a small volume injection into the hepatic artery. Read More

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November 1987

Does radiolabelled diphosphonate retention reflect bone metabolism in the elderly?

Age Ageing 1986 May;15(3):164-8

The 24-h whole-body retention of diphosphonates (WBR), a useful measure of bone metabolism in young subjects, was measured in 27 elderly subjects (19 from home and eight in-patients). WBR rose with increasing age (r = 0.55, P less than 0. Read More

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Disposition of radiolabelled suppositories in humans.

J Pharm Pharmacol 1985 Apr;37(4):266-8

The disposition of Witepsol H 15 suppositories radiolabelled with [99mTc] technetium hydroxymethyldiphosphonate was studied after rectal administration in volunteers. The migration of the radiolabel was monitored continuously by external scintigraphy. The resulting scintiphotos were superimposed on lower GI radiographs to determine the extent of spreading of the dosage form in the rectum. Read More

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