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

EJNMMI Research
Ralf BergmannFrank 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 p...Continue Reading

References

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Citations

Mar 24, 2017·Journal of Peptide Science : an Official Publication of the European Peptide Society·Ralf BergmannInes Neundorf
Jul 22, 2018·IEEE Transactions on Nanobioscience·Nafiseh SalekMohammad Ghannadi-Maragheh
Jun 18, 2017·Scientific Reports·Ralf BergmannHolger Stephan
Aug 30, 2020·Current Osteoporosis Reports·Jeffery J Nielsen, Stewart A Low
Oct 9, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jeffery J NielsenPhilip S Low
Aug 6, 2021·Frontiers in Medicine·Michiel Van de VoordeAndrew R Burgoyne

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Methods Mentioned

BETA
nuclear magnetic resonance
neutron capture
column chromatography

Software Mentioned

GraphPad
GraphPad Prism

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