Lu-177-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F16%3A10323194" target="_blank" >RIV/00216208:11310/16:10323194 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1186/s13550-016-0161-3" target="_blank" >http://dx.doi.org/10.1186/s13550-016-0161-3</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1186/s13550-016-0161-3" target="_blank" >10.1186/s13550-016-0161-3</a>
Alternative languages
Result language
angličtina
Original language name
Lu-177-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment
Original language description
Metastatic bone lesion is a common syndrome of many cancer diseases in an advanced state. 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. No-carrier-added Lu-177 is remarkably suitable for an application in this scope. Five DOTA-and DO2A-based bisphosphonates, including monomeric and dimeric structures and one NO2A-derivative, were synthesized and labelled with Lu-177. Radiolabelling yields for [Lu-177]Lu-DOTA and [Lu-177]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 Lu-177-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. Lu-177-bisphosphonate dimers showed a slightly higher bone accumulation (SUVfemur = 4.48 +/- 0.38 for [Lu-177] Lu-DO2A(P-BP)(2); SUVfemur = 5.41 +/- 0.46 for [Lu-177]Lu-DOTA(M-BP)(2)) but a slower blood clearance (SUVblood = 1.25 +/- 0.09 for [Lu-177]Lu-DO2A(P-BP)(2); SUVblood = 1.43 +/- 0.32 for [Lu-177]Lu-DOTA(M-BP)(2)). Conclusions: 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.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CA - Inorganic chemistry
OECD FORD branch
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Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
EJNMMI Research
ISSN
2191-219X
e-ISSN
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Volume of the periodical
6
Issue of the periodical within the volume
neuveden
Country of publishing house
DE - GERMANY
Number of pages
12
Pages from-to
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UT code for WoS article
000369486700002
EID of the result in the Scopus database
2-s2.0-84954458116