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: Radhia El Aissi, Imen Miladi, Jean-Michel Chezal, Olivier Chavignon, Elisabeth Miot-Noirault, Emmanuel Moreau
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 120 Pg. 304-12 (Sep 14 2016) ISSN: 1768-3254 [Electronic] France
• PMID: 27214141 (Publication Type: Journal Article)
• Copyright: Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Chemical References

• Iodine Radioisotopes
• Prodrugs
• Radiopharmaceuticals
• Idoxuridine

Topics

• Animals
• Humans
• Idoxuridine (pharmacokinetics)
• Iodine Radioisotopes (administration & dosage, pharmacokinetics)
• Melanoma (drug therapy)
• Mice
• Prodrugs (administration & dosage, pharmacokinetics)
• Radiopharmaceuticals (administration & dosage, pharmacokinetics)
• Tissue Distribution
• Xenograft Model Antitumor Assays