title: Melanoma-targeted delivery system (part 2): Synthesis, radioiodination and biological evaluation in B16F0 bearing mice.
abstract: Here we report the synthesis and radiolabelling with iodine-125 of a melanoma-selective prodrug (17a*) and its parent drug IUdR. The in vivo and ex vivo biodistributions of [(125)I](17a*) and [(125)I]IUdR were evaluated in a model of melanoma B16F0-bearing mice. The pharmacokinetic profile of [(125)I](17a*) suggests rapid release of the active drug [(125)I]IUdR after i.v. administration of [(125)I](17a*). Preliminary metabolism studies in dedicated compartments (i.e. blood, urine and tumour) yielded results consistent with this hypothesis.
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
authors.forename: Radhia
authors.initials: R
authors.lastname: El Aissi
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
authors.forename: Imen
authors.initials: I
authors.lastname: Miladi
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Chezal
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
authors.forename: Olivier
authors.initials: O
authors.lastname: Chavignon
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France.
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Miot-Noirault
authors.affiliation: INSERM - Université d'Auvergne, UMR 990, IMTV, BP 184, F-63005 Clermont-Ferrand Cedex, France; Clermont Université, Université d'Auvergne, Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63005 Clermont-Ferrand Cedex, France. Electronic address: emmanuel.moreau@udamail.fr.
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Moreau
mesh_terms: D000818:Animals; D006801:Humans; D007065:Idoxuridine / Q000493:pharmacokinetics; D007457:Iodine Radioisotopes / Q000008:administration & dosage / Q000493:pharmacokinetics; D008545:Melanoma / Q000188:drug therapy*; D051379:Mice; D011355:Prodrugs / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000493:pharmacokinetics; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D007457:Iodine Radioisotopes; D011355:Prodrugs; D019275:Radiopharmaceuticals; D007065:Idoxuridine
keywords: Biodistribution; IUdR; Melanoma-targeted delivery system; Prodrug; Radioiodination