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Nucl Med Biol. 2011 Apr;38(3):381-92. doi: 10.1016/j.nucmedbio.2010.09.008. Epub 2010 Dec 3.

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

Author information

  • 1Radiopharmacy, KULeuven, Belgium. matthias.bauwens@pharm.kuleuven.be

Abstract

PURPOSE:

Two variants of Annexin A5 (Cys2-AnxA5 and Cys165-AnxA5) were labelled with Gallium-68 in order to evaluate their biological properties.

PROCEDURES:

Biodistribution and pharmacokinetics of the radiotracers were studied with μPET in healthy mice and in a mouse model of hepatic apoptosis. μPET imaging after IV injection of the tracers in combination with μMRI was performed in Daudi tumor bearing mice before and after treatment with a combination of chemotherapy and radiotherapy.

RESULTS:

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.

CONCLUSION:

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.

Copyright © 2011 Elsevier Inc. All rights reserved.

PMID:
21492787
[PubMed - indexed for MEDLINE]
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