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177Lu-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment

Overview of attention for article published in EJNMMI Research, January 2016
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Title
177Lu-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment
Published in
EJNMMI Research, January 2016
DOI 10.1186/s13550-016-0161-3
Pubmed ID
Authors

Ralf Bergmann, Marian Meckel, Vojtěch Kubíček, Jens Pietzsch, Jörg Steinbach, Petr Hermann, Frank Rösch

Abstract

Metastatic bone lesion is a common syndrome of many cancer diseases in an advanced state. The major symptom is severe pain, spinal cord compression, and pathological fracture, associated with an obvious morbidity. Common treatments including systemic application of bisphosphonate drugs aim on pain reduction and on improving the quality of life of the patient. Particularly, patients with multiple metastatic lesions benefit from bone-targeting therapeutic radiopharmaceuticals. Agents utilizing beta-emitting radionuclides in routine clinical praxis are, for example, [(89)Sr]SrCl2 and [(153)Sm]Sm-EDTMP. No-carrier-added (n.c.a.) (177)Lu is remarkably suitable for an application in this scope. Five 1,4,7,10-tetraazacyclododecane N,N',N'',N''-tetra-acetic acid (DOTA)- and DO2A-based bisphosphonates, including monomeric and dimeric structures and one 1,4,7-triazacyclononane-1,4-diacetic acid (NO2A) derivative, were synthesized and labelled with n.c.a. (177)Lu. Radio-TLC and high-performance liquid chromatography (HPLC) methods were successfully established for determining radiochemical yields and for quality control. Their binding to hydroxyapatite was measured in vitro. Ex vivo biodistribution experiments and dynamic in vivo single photon computed tomography (SPECT)/CT measurements were performed in healthy rats for 5 min and 1 h periods. Data on %ID/g or standard uptake value (SUV) for femur, blood, and soft-tissue organs were analyzed and compared with [(177)Lu]citrate. Radiolabelling yields for [(177)Lu]Lu-DOTA and [(177)Lu]Lu-NO2A monomeric bisphosphonate complexes were >98 % within 15 min. The dimeric macrocyclic bisphosphonates showed a decelerated labelling kinetics, reaching a plateau after 30 min of 60 to 90 % radiolabelling yields. All (177)Lu-bisphosphonate complexes showed exclusive accumulation in the skeleton. Blood clearance and renal elimination were fast. SUV data (all for 1 h p.i.) in the femur ranged from 3.34 to 5.67. The bone/blood ratios were between 3.6 and 135.6, correspondingly. (177)Lu-bisphosphonate dimers showed a slightly higher bone accumulation (SUVfemur = 4.48 ± 0.38 for [(177)Lu]Lu-DO2A(P(BP))2; SUVfemur = 5.41 ± 0.46 for [(177)Lu]Lu-DOTA(M(BP))2) but a slower blood clearance (SUVblood = 1.25 ± 0.09 for [(177)Lu]Lu-DO2A(P(BP))2; SUVblood = 1.43 ± 0.32 for [(177)Lu]Lu-DOTA(M(BP))2). Lu-complexes of macrocyclic bisphosphonates might become options for the therapy of skeletal metastases in the near future, since they show high uptake in bone together with a very low soft-tissue accumulation.

Twitter Demographics

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Mendeley readers

The data shown below were compiled from readership statistics for 31 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 31 100%

Demographic breakdown

Readers by professional status Count As %
Professor 5 16%
Student > Ph. D. Student 5 16%
Researcher 4 13%
Student > Bachelor 4 13%
Student > Doctoral Student 3 10%
Other 5 16%
Unknown 5 16%
Readers by discipline Count As %
Chemistry 11 35%
Pharmacology, Toxicology and Pharmaceutical Science 4 13%
Medicine and Dentistry 4 13%
Biochemistry, Genetics and Molecular Biology 3 10%
Engineering 2 6%
Other 2 6%
Unknown 5 16%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 25 January 2016.
All research outputs
#6,037,928
of 7,028,853 outputs
Outputs from EJNMMI Research
#82
of 152 outputs
Outputs of similar age
#260,938
of 317,380 outputs
Outputs of similar age from EJNMMI Research
#2
of 3 outputs
Altmetric has tracked 7,028,853 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 152 research outputs from this source. They receive a mean Attention Score of 1.2. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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