Development of acetylated HDD kit for preparation of 188Re-HDD/lipiodol

Appl Radiat Isot. 2007 Jan;65(1):64-9. doi: 10.1016/j.apradiso.2006.07.008. Epub 2006 Sep 28.

Abstract

A lipiodol solution of (188)Re-4-hexadecyl-2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol ((188)Re-HDD/lipiodol) is in clinical study for liver cancer therapy. However, formulation of it is difficult due to highly active and unstable sulfhydryl groups. We produced new kits using diacetylated HDD (AHDD), in which sulfhydryl groups are protected. We found that AHDD kit can replace HDD kit due to an increased stability for formulation, the better radiolabeling efficiency (78%) and the equivalent biodistribution pattern in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation
  • Animals
  • Equipment Design
  • Equipment Failure Analysis
  • Iodized Oil / chemical synthesis*
  • Iodized Oil / pharmacokinetics*
  • Iodized Oil / therapeutic use
  • Isotope Labeling / instrumentation*
  • Isotope Labeling / methods
  • Metabolic Clearance Rate
  • Mice
  • Organ Specificity
  • Organometallic Compounds / chemical synthesis*
  • Organometallic Compounds / pharmacokinetics*
  • Organometallic Compounds / therapeutic use
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use
  • Reagent Kits, Diagnostic*
  • Tissue Distribution

Substances

  • 188Re-4-hexadecyl-1,2,9,9-tetramethyl-4,7-diaza-1,10-decanethiol lipiodol conjugate
  • Organometallic Compounds
  • Radiopharmaceuticals
  • Reagent Kits, Diagnostic
  • Iodized Oil