177Lu labelled polyaminophosphonates as potential agents for bone pain palliation.

Abstract	Polyphosphonate ligands labelled with radioisotopes decaying by moderate energy beta emission have shown utility as palliative agents for painful bone metastasis. 177Lu (T(1/2)=6.71 d, Ebetamax=497 keV) has radionuclidic properties suitable for use in palliative therapy of bone metastasis. 177Lu was produced at a high specific activity and excellent radionuclidic purity by thermal neutron bombardment of a target prepared from natural Lu. Three polyaminomethylene phosphonate ligands, abbreviated as EDTMP, DTPMP and TTHMP, were synthesized and radiolabelled with 177Lu. Complexation parameters were optimized to achieve maximum yields (97-99.5%). All the complexes were found to retain their stability at room temperature even 14 days after preparation. Biodistribution studies of the complexes were carried out in Wistar rats. All the complexes showed significant bone uptake (6-6.5%/g in tibia at 3 h post-injection (p.i.)) with rapid clearance from blood and minimum uptake in soft tissues. These studies reveal that 177Lu complexes with the synthesized ligands have a potential use in palliative treatment of painful bone metastasis.
Authors	S Chakraborty, T Das, P R Unni, H D Sarma, G Samuel, S Banerjee, M Venkatesh, N Ramamoorthy, M R A Pillai
Journal	Nuclear medicine communications (Nucl Med Commun) Vol. 23 Issue 1 Pg. 67-74 (Jan 2002) ISSN: 0143-3636 [Print] England
PMID	11748440 (Publication Type: Journal Article)
Chemical References	Ligands Organophosphonates Phosphoramides Polyamines Radioisotopes Radiopharmaceuticals lutetium aminophosphonate Lutetium
Topics	Animals Bone Neoplasms (physiopathology, secondary) Isotope Labeling Ligands Lutetium (chemistry, pharmacokinetics, therapeutic use) Magnetic Resonance Spectroscopy Organophosphonates (chemical synthesis, pharmacokinetics, therapeutic use) Pain, Intractable (etiology, radiotherapy) Palliative Care Phosphoramides Polyamines (chemical synthesis, pharmacokinetics, therapeutic use) Quality Control Radioisotopes (therapeutic use) Radiopharmaceuticals (chemical synthesis, pharmacokinetics, therapeutic use) Rats Rats, Wistar Spectrophotometry, Infrared Tissue Distribution

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