Preclinical studies of [61Cu]ATSM as a PET radiopharmaceutical for fibrosarcoma imaging

Acta Pharm. 2009 Mar;59(1):45-55. doi: 10.2478/v10007-009-0008-9.

Abstract

[61Cu]diacetyl-bis(N4-methylthiosemicarbazone) ([61Cu] ATSM) was prepared using in house-made diacetyl-bis(N4-methylthiosemicarbazone) (ATSM) ligand and [61Cu]CuCl2 produced via the natZn(p, x)61Cu (180 muA proton irradiation, 22 MeV, 3.2 h) and purified by a ion chromatography method. [61Cu]ATSM radiochemical purity was >98 %, as shown by HPLC and RTLC methods. [61Cu]ATSM was administered into normal and tumor bearing rodents for up to 210 minutes, followed by biodistribution and co-incidence imaging studies. Significant tumor/non-tumor accumulation was observed either by animal sacrification or imaging. [61Cu]ATSM is a positron emission tomography (PET) radiotracer for tumor hypoxia imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Hypoxia
  • Chromatography, High Pressure Liquid
  • Chromatography, Thin Layer
  • Coordination Complexes
  • Copper Radioisotopes / pharmacokinetics
  • Drug Evaluation, Preclinical
  • Fibrosarcoma / diagnosis*
  • Male
  • Neoplasms, Experimental / diagnosis
  • Organometallic Compounds* / pharmacokinetics
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals / pharmacokinetics
  • Rats
  • Thiosemicarbazones* / pharmacokinetics
  • Tissue Distribution

Substances

  • Coordination Complexes
  • Copper Radioisotopes
  • Organometallic Compounds
  • Radiopharmaceuticals
  • Thiosemicarbazones
  • copper (II) diacetyl-di(N(4)-methylthiosemicarbazone)