title: Potential (166)Ho radiopharmaceuticals for intravascular radiation therapy (IVRT)-I: [(166)Ho] holmium labeled ethylene dicysteine.
abstract: The use of beta(-) emitting radionuclides in the control of restenosis in post angioplasty patients is currently under intense investigation at many leading cardiovascular research centers. (32)P coated metallic stents, (192)Ir wire source and balloons filled with an appropriate radionuclide solution such as of (188)Re, attached to catheter are being studied. (166)Ho has comparable radionuclidic properties to that of (188)Re, can be more easily produced and hence is an attractive alternative to (188)Re. Ethylene dicysteine complex of (166)Ho was prepared and its pharmacological behavior studied. Optimum conditions for the preparation of complex with respect to the reaction time, ligand concentration, pH of the reaction mixture as well as reaction temperature were standardized. The stability of the labeled complex at room temperature as well as at 4 degrees C was determined. Biodistribution pattern of the injected complex in Wistar rats was estimated at 10 min, 30 min and 3 h post injection. This study indicated that >90% of the injected (166)Ho-EC complex was excreted in urine within 3 h post injection, with insignificant retention in any major organ. These studies reveal that (166)Ho-EC could be a viable substitute for (188)Re compounds in radioactive liquid-filled balloon IVRT.
authors.affiliation: Radiopharmaceuticals Division, Bhabha Atomic Research Centre, 400085, Mumbai, India.
authors.forename: S
authors.initials: S
authors.lastname: Chakraborty
authors.forename: P R
authors.initials: PR
authors.lastname: Unni
authors.forename: S
authors.initials: S
authors.lastname: Banerjee
authors.forename: G
authors.initials: G
authors.lastname: Samuel
authors.forename: T
authors.initials: T
authors.lastname: Das
authors.forename: H D
authors.initials: HD
authors.lastname: Sarma
authors.forename: N
authors.initials: N
authors.lastname: Ramamoorthy
authors.forename: M R
authors.initials: MR
authors.lastname: Pillai
mesh_terms: D000818:Animals; D002854:Chromatography, Paper; D003327:Coronary Disease / Q000532:radiotherapy; D003545:Cysteine / Q000031:analogs & derivatives / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006695:Holmium / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006801:Humans; D008657:Metabolic Clearance Rate; D051379:Mice; D011868:Radioisotopes; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D011868:Radioisotopes; D019275:Radiopharmaceuticals; C109063:ethylene dicysteine; D003545:Cysteine; D006695:Holmium