title: 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.affiliation: Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
authors.forename: S
authors.initials: S
authors.lastname: Chakraborty
authors.forename: T
authors.initials: T
authors.lastname: Das
authors.forename: P R
authors.initials: PR
authors.lastname: Unni
authors.forename: H D
authors.initials: HD
authors.lastname: Sarma
authors.forename: G
authors.initials: G
authors.lastname: Samuel
authors.forename: S
authors.initials: S
authors.lastname: Banerjee
authors.forename: M
authors.initials: M
authors.lastname: Venkatesh
authors.forename: N
authors.initials: N
authors.lastname: Ramamoorthy
authors.forename: M R A
authors.initials: MR
authors.lastname: Pillai
mesh_terms: D000818:Animals; D001859:Bone Neoplasms / Q000503:physiopathology* / Q000556:secondary; D007553:Isotope Labeling; D008024:Ligands; D008187:Lutetium / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D009682:Magnetic Resonance Spectroscopy; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010148:Intractable Pain / Q000209:etiology / Q000532:radiotherapy*; D010166:Palliative Care; D063088:Phosphoramides; D011073:Polyamines / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011786:Quality Control; D011868:Radioisotopes / Q000627:therapeutic use; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared; D014018:Tissue Distribution
chemical_list: D008024:Ligands; D063065:Organophosphonates; D063088:Phosphoramides; D011073:Polyamines; D011868:Radioisotopes; D019275:Radiopharmaceuticals; C449681:lutetium aminophosphonate; D008187:Lutetium