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  • Title: Site-specific 68Ga-labeled Annexin A5 as a PET imaging agent for apoptosis.
    Author: Bauwens M, De Saint-Hubert M, Devos E, Deckers N, Reutelingsperger C, Mortelmans L, Himmelreich U, Mottaghy FM, Verbruggen A.
    Journal: Nucl Med Biol; 2011 Apr; 38(3):381-92. PubMed ID: 21492787.
    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.
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