title: In vivo biodistribution and pharmacokinetics of 18F-labelled Spiegelmers: a new class of oligonucleotidic radiopharmaceuticals.
abstract: OBJECTIVE
  Single-stranded mirror-image oligonucleotides (Spiegelmers) are highly resistant to nuclease degradation and are capable of tightly and specifically binding to protein targets. Here we explored the potential of Spiegelmers as in vivo imaging probes for positron emission tomography (PET).
  
  
  METHODS
  We investigated the biodistribution and pharmacokinetics of [18F]-L-DNA and [18F]-L-RNA Spiegelmers by dynamic quantitative whole-body PET imaging after intravenous administration in non-human primates. Their metabolic profile was explored in primates and rats, and ex vivo autoradiography of [(125)I]-L-RNA was performed in rat kidneys, the major organ for Spiegelmer uptake.
  
  
  RESULTS
  Both [18F]-L-DNA and [18F]-L-RNA Spiegelmers were metabolically stable in plasma during 2 h after injection. No evidence of non-specific binding was found with either type of Spiegelmer in any tissue.
  
  
  CONCLUSIONS
  The biodistribution and metabolic profiles of [18F]-L-DNA and [18F]-L-RNA Spiegelmers highlight their potential as radiotracers for in vivo imaging applications.
authors.affiliation: Laboratoire d'Imagerie de l'Expression des Gènes, CEA, Service Hospitalier Frédéric Joliot, INSERM ERM 103, Orsay, France.
authors.forename: Raphaël
authors.initials: R
authors.lastname: Boisgard
authors.forename: Bertrand
authors.initials: B
authors.lastname: Kuhnast
authors.forename: Stefan
authors.initials: S
authors.lastname: Vonhoff
authors.forename: Chéraz
authors.initials: C
authors.lastname: Younes
authors.forename: Françoise
authors.initials: F
authors.lastname: Hinnen
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Verbavatz
authors.forename: Bernard
authors.initials: B
authors.lastname: Rousseau
authors.forename: Jens Peter
authors.initials: JP
authors.lastname: Fürste
authors.forename: Britta
authors.initials: B
authors.lastname: Wlotzka
authors.forename: Frédéric
authors.initials: F
authors.lastname: Dollé
authors.forename: Sven
authors.initials: S
authors.lastname: Klussmann
authors.forename: Bertrand
authors.initials: B
authors.lastname: Tavitian
mesh_terms: D000818:Animals; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics*; D008297:Male; D008657:Metabolic Clearance Rate; D009841:Oligonucleotides / Q000493:pharmacokinetics*; D009928:Organ Specificity; D010215:Papio; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D013045:Species Specificity; D014018:Tissue Distribution
chemical_list: D005462:Fluorine Radioisotopes; D007457:Iodine Radioisotopes; D009841:Oligonucleotides; D019275:Radiopharmaceuticals