All

What are you looking for?

All
Projects
Results
Organizations

Quick search

  • Projects supported by TA ČR
  • Excellent projects
  • Projects with the highest public support
  • Current projects

Smart search

  • That is how I find a specific +word
  • That is how I leave the -word out of the results
  • “That is how I can find the whole phrase”

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

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    CA - Inorganic chemistry

  • OECD FORD branch

Result continuities

  • Project

  • 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

  • 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

  • UT code for WoS article

    000369486700002

  • EID of the result in the Scopus database

    2-s2.0-84954458116