Site-specific Ga-68-labeled Annexin A5 as a PET imaging agent for apoptosis

Matthias Bauwens*, Marijke De Saint-Hubert, Ellen Devos, Niko Deckers, Chris P. M. Reutelingsperger, Luc Mortelmans, Uwe Himmelreich, Felix M. Mottaghy, Alfons M. Verbruggen

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Two variants of Annexin A5 (Cys2-AnxA5 and Cys165-AnxA5) were labelled with Gallium-68 in order to evaluate their biological properties.Biodistribution and pharmacokinetics of the radiotracers were studied with ?PET in healthy mice and in a mouse model of hepatic apoptosis. ?PET imaging after IV injection of the tracers in combination with ?MRI was performed in Daudi tumor bearing mice before and after treatment with a combination of chemotherapy and radiotherapy.The biodistribution data indicated a fast urinary clearance with only minor hepatobilliary clearance, although a high retention in the kidneys was observed. Animals treated with anti-Fas showed a 3 to 8 times higher liver uptake as compared to healthy animals. Tumor uptake of (68)Ga-Cys2-AnxA5 and (68)Ga-Cys165-AnxA5 was low but significantly increased after therapy.Both (68)Ga-Cys2-AnxA5 and (68)Ga-Cys165-AnxA5 show a clear binding to apoptotic cells and are promising tracers for rapid evaluation of cancer therapy.
Original languageEnglish
Pages (from-to)381-392
JournalNuclear Medicine and Biology
Volume38
Issue number3
DOIs
Publication statusPublished - Apr 2011

Keywords

  • [Ga-68]
  • Annexin A5
  • Apoptosis
  • Therapy evaluation
  • PET

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